Identification
NameSitagliptin
Accession NumberDB01261  (DB07214)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Sitagliptin is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 diabetes mellitus. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin.

Structure
Thumb
Synonyms
(2R)-4-OXO-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
MK-0431
Sitagliptan
Sitagliptin phosphate
Sitagliptina
Sitagliptine
Sitagliptinum
External IDs LEZ-763 / LEZ763 / MK-0431
Product Ingredients Not Available
Product Images
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralCardinal Health2006-10-16Not applicableUs
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralA S Medication Solutions2006-10-162017-06-20Us
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-09Not applicableUs
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mg/1OralPhysicians Total Care, Inc.2009-05-06Not applicableUs00006 0112 54 nlmimage10 131609e0
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet50 mgOralMerck Ltd.2012-09-17Not applicableCanada
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mg/1OralAvera Mc Kennan Hospital2016-01-11Not applicableUs
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralMerck Sharp & Dohme Limited2006-10-16Not applicableUs
JanuviaTablet, film coated50 mg/1OralCardinal Health2006-10-16Not applicableUs
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet100 mgOralMerck Ltd.2008-01-02Not applicableCanada
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralA S Medication Solutions2006-10-162017-06-20Us
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mg/1OralRemedy Repack2014-03-032017-06-20Us
JanuviaTablet, film coated50 mg/1OralMerck Sharp & Dohme Limited2006-10-16Not applicableUs
JanuviaTablet, film coated50 mg/1OralCardinal Health2006-10-162017-04-27Us
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated50 mg/1OralCardinal Health2006-10-16Not applicableUs
JanuviaTablet, film coated100 mg/1OralCardinal Health2006-10-16Not applicableUs
JanuviaTablet, film coated100 mg/1OralPhysicians Total Care, Inc.2007-12-13Not applicableUs
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet25 mgOralMerck Ltd.2012-09-17Not applicableCanada
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated25 mg/1OralAvera Mc Kennan Hospital2016-10-20Not applicableUs
JanuviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
JanuviaTablet, film coated25 mg/1OralMerck Sharp & Dohme Limited2006-10-16Not applicableUs00006 0221 31 nlmimage10 da15ed0f
JanuviaTablet, film coated100 mg/1OralCardinal Health2006-10-162017-04-27Us00006 0277 54 nlmimage10 16160b30
JanuviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated25 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
RistabenTablet, film coated100 mgOralMerck Sharp & Dohme Limited2010-03-15Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated50 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
TesavelTablet, film coated25 mgOralMerck Sharp & Dohme Limited2008-01-10Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated50 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
XeleviaTablet, film coated100 mgOralMerck Sharp & Dohme Limited2007-03-21Not applicableEu
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
JanuviaTablet, film coated100 mg/1OralClinical Solutions Wholsesale2006-10-162017-06-24Us
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
XeleviaNot Available
Brand mixtures
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
JanumetTablet, film coatedOralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2012-03-09Not applicableUs00006 0575 61 nlmimage10 19160ce0
Janumet XRTablet, film coated, extended releaseOralMerck Sharp & Dohme Limited2012-02-02Not applicableUs
VelmetiaTablet, film coatedOralMerck Sharp & Dohme Limited2008-07-16Not applicableEu
Categories
UNIIQFP0P1DV7Z
CAS number486460-32-6
WeightAverage: 407.3136
Monoisotopic: 407.118079357
Chemical FormulaC16H15F6N5O
InChI KeyMFFMDFFZMYYVKS-SECBINFHSA-N
InChI
InChI=1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1
IUPAC Name
(3R)-3-amino-1-[3-(trifluoromethyl)-5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
SMILES
N[[email protected]@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC1=CC(F)=C(F)C=C1F
Pharmacology
Indication

For use as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Also for use in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin or a PPARγ agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Structured Indications
Pharmacodynamics

Sitagliptin is an orally-active member of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. The benefit of this medicine is expected to be its lower side-effects of hypoglycemia in the control of blood glucose values. The drug works to diminish the effects of a protein/enzyme (by the inhibition of this protein/enzyme) on the pancreas at the level of release of glucagon (diminishes its release) and at the level of insulin (increases its synthesis and release) until blood glucose levels are restored toward normal, in which case the protein/enzyme-enzyme inhibitor becomes less effective and the amounts of insulin released diminishes thus diminishing the "overshoot" of hypoglycemia seen in other oral hypoglycemic agents.

Mechanism of action

Sitagliptin is a highly selective DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones, thereby increasing the concentration and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. These changes lead to a decrease in hemoglobin A1c (HbA1c)levels, as well as a lower fasting and postprandial glucose concentration. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

TargetKindPharmacological actionActionsOrganismUniProt ID
Dipeptidyl peptidase 4Proteinyes
inhibitor
HumanP27487 details
Related Articles
Absorption

Rapidly absorbed following oral administration, with an absolute bioavailability of 87%.

Volume of distribution
  • 198 L [healthy subjects]
Protein binding

The fraction of sitagliptin reversibly bound to plasma proteins is low (38%).

Metabolism

Sitagliptin does not undergo extensive metabolism. In vitro studies indicate that the primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4 (oxidation), with contribution from CYP2C8.

Route of elimination

Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Following administration of an oral [14C]sitagliptin dose to healthy subjects, approximately 100% of the administered radioactivity was eliminated in feces (13%) or urine (87%) within one week of dosing. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion.

Half life

12.4 hours

Clearance
  • renal cl=350 mL/min [Healthy subjects receiving 100 mg oral dose]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Sitagliptin.Experimental
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Sitagliptin.Approved, Investigational
AbirateroneThe serum concentration of Sitagliptin can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Sitagliptin can be increased when it is combined with Acetaminophen.Approved
AcetohexamideSitagliptin may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Sitagliptin.Approved, Vet Approved
AfatinibThe serum concentration of Sitagliptin can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Sitagliptin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Sitagliptin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Sitagliptin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Sitagliptin can be increased when it is combined with Alfentanil.Approved, Illicit
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Sitagliptin.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Sitagliptin.Approved, Illicit, Investigational
AmantadineThe serum concentration of Sitagliptin can be increased when it is combined with Amantadine.Approved
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Sitagliptin.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Sitagliptin.Illicit, Withdrawn
Aminohippuric acidThe serum concentration of Sitagliptin can be increased when it is combined with Aminohippuric acid.Approved
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Sitagliptin.Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Sitagliptin.Approved
AmiodaroneThe metabolism of Sitagliptin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Sitagliptin.Approved
AmlodipineThe serum concentration of Sitagliptin can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Sitagliptin can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Sitagliptin can be increased when it is combined with Amsacrine.Approved
AprepitantThe serum concentration of Sitagliptin can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Aripiprazole.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Asenapine.Approved
AstemizoleThe serum concentration of Sitagliptin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Sitagliptin can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Sitagliptin can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Sitagliptin can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Sitagliptin.Approved
AzelastineThe serum concentration of Sitagliptin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Sitagliptin can be increased when it is combined with Azithromycin.Approved
BalsalazideBalsalazide may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
BenazeprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Benazepril.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Sitagliptin.Withdrawn
BenzocaineThe serum concentration of Sitagliptin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Sitagliptin can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BexaroteneThe serum concentration of Sitagliptin can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Sitagliptin can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Sitagliptin can be decreased when it is combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Sitagliptin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Sitagliptin can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Sitagliptin can be increased when it is combined with Bosutinib.Approved
BrexpiprazoleThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Brexpiprazole.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Sitagliptin.Approved, Investigational
BumetanideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Bumetanide.Approved
BuprenorphineThe serum concentration of Sitagliptin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuserelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Buserelin.Approved
BuspironeThe serum concentration of Sitagliptin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Sitagliptin can be increased when it is combined with Cabazitaxel.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Sitagliptin.Approved
CaffeineThe serum concentration of Sitagliptin can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Sitagliptin can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Sitagliptin can be increased when it is combined with Candesartan.Approved
CandoxatrilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Candoxatril.Experimental
CaptoprilThe serum concentration of Sitagliptin can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Sitagliptin can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypoglycemic activities of Sitagliptin.Withdrawn
CarvedilolThe serum concentration of Sitagliptin can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Sitagliptin can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Sitagliptin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Sitagliptin can be increased when it is combined with Ceritinib.Approved
ChloroquineThe serum concentration of Sitagliptin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Sitagliptin.Withdrawn
ChlorpromazineThe serum concentration of Sitagliptin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideSitagliptin may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Sitagliptin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
ChlorthalidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Chlorthalidone.Approved
CholesterolThe serum concentration of Sitagliptin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Sitagliptin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Sitagliptin can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Sitagliptin can be decreased when it is combined with Cimetidine.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Withdrawn
CiprofloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Sitagliptin.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Sitagliptin can be increased when it is combined with Citalopram.Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Sitagliptin.Approved
ClemastineThe metabolism of Sitagliptin can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Sitagliptin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Sitagliptin.Approved, Vet Approved
ClopidogrelThe metabolism of Sitagliptin can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Sitagliptin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Clozapine.Approved
CobicistatThe metabolism of Sitagliptin can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Sitagliptin can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Sitagliptin can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Sitagliptin can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Sitagliptin.Approved
CorticotropinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Cortisone acetate.Approved
CrizotinibThe metabolism of Sitagliptin can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Sitagliptin.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Sitagliptin.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Sitagliptin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Sitagliptin can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Sitagliptin can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Sitagliptin can be increased when it is combined with Dactinomycin.Approved
DanazolThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Sitagliptin.Investigational
DarunavirThe metabolism of Sitagliptin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Sitagliptin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Sitagliptin can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Sitagliptin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Sitagliptin.Approved
dersalazinedersalazine may increase the hypoglycemic activities of Sitagliptin.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Sitagliptin.Approved
DesloratadineThe serum concentration of Sitagliptin can be increased when it is combined with Desloratadine.Approved, Investigational
DesogestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Sitagliptin.Approved
DexamethasoneThe serum concentration of Sitagliptin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Sitagliptin can be increased when it is combined with Dextromethorphan.Approved
DiazoxideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Diazoxide.Approved
DiclofenacThe serum concentration of Sitagliptin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Sitagliptin.Approved
DienogestThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Sitagliptin.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Sitagliptin.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Sitagliptin.Approved
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Sitagliptin.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Sitagliptin.Illicit
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Sitagliptin.Approved
DipyridamoleThe serum concentration of Sitagliptin can be increased when it is combined with Dipyridamole.Approved
DisopyramideSitagliptin may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Sitagliptin.Approved
DoxazosinThe serum concentration of Sitagliptin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Sitagliptin.Approved
DoxorubicinThe serum concentration of Sitagliptin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Sitagliptin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Sitagliptin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Sitagliptin can be decreased when combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Sitagliptin.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Sitagliptin.Approved
EfavirenzThe serum concentration of Sitagliptin can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Sitagliptin can be increased when it is combined with Elbasvir.Approved
EnalaprilThe serum concentration of Sitagliptin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Sitagliptin.Approved, Investigational
EnoxacinEnoxacin may increase the hypoglycemic activities of Sitagliptin.Approved
EnzalutamideThe serum concentration of Sitagliptin can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Sitagliptin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Sitagliptin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Sitagliptin.Approved
ErythromycinThe metabolism of Sitagliptin can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Sitagliptin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Sitagliptin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Sitagliptin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Sitagliptin.Approved
EstriolThe serum concentration of Sitagliptin can be decreased when it is combined with Estriol.Approved, Vet Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Sitagliptin.Approved
EstroneThe serum concentration of Sitagliptin can be decreased when it is combined with Estrone.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Sitagliptin.Approved
Etacrynic acidThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Sitagliptin.Approved
Ethynodiol diacetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Sitagliptin.Approved
EtoposideThe serum concentration of Sitagliptin can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Sitagliptin.Approved
EverolimusThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Everolimus.Approved
FelodipineThe serum concentration of Sitagliptin can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Sitagliptin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Sitagliptin can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Sitagliptin can be increased when it is combined with Fidaxomicin.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Sitagliptin.Approved
FluconazoleThe metabolism of Sitagliptin can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
FluoxetineThe serum concentration of Sitagliptin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Sitagliptin.Approved, Illicit
FlupentixolThe serum concentration of Sitagliptin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Sitagliptin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Sitagliptin can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Sitagliptin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Sitagliptin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Sitagliptin can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Fosinopril.Approved
FosphenytoinThe metabolism of Sitagliptin can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Sitagliptin.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Fusidic Acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Sitagliptin.Investigational
GarlicThe serum concentration of Sitagliptin can be decreased when it is combined with Garlic.Approved
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
GefitinibThe serum concentration of Sitagliptin can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe metabolism of Sitagliptin can be decreased when combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
GenisteinThe serum concentration of Sitagliptin can be increased when it is combined with Genistein.Investigational
GlibornurideSitagliptin may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideSitagliptin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideSitagliptin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideSitagliptin may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneSitagliptin may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideSitagliptin may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideSitagliptin may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Goserelin.Approved
Gramicidin DThe serum concentration of Sitagliptin can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Sitagliptin can be increased when it is combined with Haloperidol.Approved
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Sitagliptin.Withdrawn
HistrelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Sitagliptin.Experimental
HydrochlorothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe serum concentration of Sitagliptin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IdelalisibThe serum concentration of Sitagliptin can be increased when it is combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Iloperidone.Approved
ImatinibThe metabolism of Sitagliptin can be decreased when combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Sitagliptin.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Sitagliptin.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Indapamide.Approved
IndinavirThe metabolism of Sitagliptin can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Sitagliptin can be increased when it is combined with Indomethacin.Approved, Investigational
Insulin AspartSitagliptin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirSitagliptin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineSitagliptin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineSitagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanSitagliptin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproSitagliptin may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin PorkSitagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Sitagliptin.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Sitagliptin.Withdrawn
IrbesartanThe metabolism of Sitagliptin can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Sitagliptin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Sitagliptin.Approved
IsradipineThe metabolism of Sitagliptin can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Sitagliptin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Sitagliptin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Sitagliptin can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Sitagliptin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe metabolism of Sitagliptin can be decreased when combined with Ketoconazole.Approved, Investigational
LanreotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lanreotide.Approved
LansoprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Sitagliptin can be increased when it is combined with Lapatinib.Approved, Investigational
LeuprolideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Sitagliptin.Approved
LevonorgestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LevothyroxineThe serum concentration of Sitagliptin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Sitagliptin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Sitagliptin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Sitagliptin can be decreased when it is combined with Liotrix.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Sitagliptin.Approved, Nutraceutical
LisinoprilThe serum concentration of Sitagliptin can be increased when it is combined with Lisinopril.Approved, Investigational
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Sitagliptin.Approved
LomitapideThe serum concentration of Sitagliptin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Sitagliptin can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Sitagliptin can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Sitagliptin can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Sitagliptin can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Sitagliptin.Approved, Investigational
LuliconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Sitagliptin can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lurasidone.Approved
MaprotilineThe serum concentration of Sitagliptin can be increased when it is combined with Maprotiline.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
MebendazoleThe serum concentration of Sitagliptin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MecaserminSitagliptin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
MefloquineThe serum concentration of Sitagliptin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Sitagliptin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Sitagliptin can be increased when it is combined with Meprobamate.Approved, Illicit
MesalazineMesalazine may increase the hypoglycemic activities of Sitagliptin.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Sitagliptin.Approved
MethadoneThe serum concentration of Sitagliptin can be increased when it is combined with Methadone.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Sitagliptin.Experimental
MethotrimeprazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Sitagliptin.Investigational
MethylprednisoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Sitagliptin.Approved
MetolazoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Metolazone.Approved
MetoprololThe serum concentration of Sitagliptin can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Sitagliptin can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Sitagliptin.Approved, Illicit
MifepristoneThe serum concentration of Sitagliptin can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Sitagliptin.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Sitagliptin.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Sitagliptin.Approved
MitomycinThe serum concentration of Sitagliptin can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Sitagliptin can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Sitagliptin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideMoclobemide may increase the hypoglycemic activities of Sitagliptin.Approved
ModafinilThe serum concentration of Sitagliptin can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Moexipril.Approved
MorphineThe serum concentration of Sitagliptin can be increased when it is combined with Morphine.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
NafcillinThe serum concentration of Sitagliptin can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Sitagliptin.Approved
NaltrexoneThe serum concentration of Sitagliptin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Sitagliptin can be increased when it is combined with Naringenin.Experimental
NateglinideSitagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Sitagliptin.Approved, Withdrawn
NelfinavirThe metabolism of Sitagliptin can be decreased when combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Sitagliptin.Investigational
NeostigmineThe serum concentration of Sitagliptin can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Sitagliptin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Sitagliptin can be increased when combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Sitagliptin.Withdrawn
NicardipineThe serum concentration of Sitagliptin can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Sitagliptin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Sitagliptin can be decreased when combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Sitagliptin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Sitagliptin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Sitagliptin can be increased when it is combined with Nitrendipine.Approved
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Sitagliptin.Investigational
NorethisteroneThe serum concentration of Sitagliptin can be decreased when it is combined with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Sitagliptin.Approved
NorgestimateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Norgestimate.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Sitagliptin.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Sitagliptin.Withdrawn
OctreotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinOfloxacin may increase the hypoglycemic activities of Sitagliptin.Approved
OlanzapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Sitagliptin can be decreased when combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Sitagliptin.Approved
OmapatrilatThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Omapatrilat.Investigational
OmeprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Sitagliptin.Investigational
OsimertinibThe serum concentration of Sitagliptin can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Sitagliptin.Approved, Illicit
P-NitrophenolThe serum concentration of Sitagliptin can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Sitagliptin can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Sitagliptin can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Paliperidone.Approved
Palmitic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Pantoprazole.Approved
PargylinePargyline may increase the hypoglycemic activities of Sitagliptin.Approved
ParoxetineThe serum concentration of Sitagliptin can be increased when it is combined with Paroxetine.Approved, Investigational
PasireotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Sitagliptin.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Sitagliptin.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Sitagliptin.Approved
PentamidineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pentamidine.Approved
PentobarbitalThe metabolism of Sitagliptin can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Sitagliptin can be increased when it is combined with Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Pethidine.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Sitagliptin.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
PhenobarbitalThe metabolism of Sitagliptin can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
PhenytoinThe metabolism of Sitagliptin can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Sitagliptin.Approved
PioglitazoneThe metabolism of Sitagliptin can be decreased when combined with Pioglitazone.Approved, Investigational
PiperazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pipotiazine.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Sitagliptin.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
Platelet Activating FactorThe serum concentration of Sitagliptin can be decreased when it is combined with Platelet Activating Factor.Experimental
PolythiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Polythiazide.Approved
PonatinibThe serum concentration of Sitagliptin can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Sitagliptin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Sitagliptin can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Sitagliptin can be increased when it is combined with Prazosin.Approved
PrednisoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Sitagliptin can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Sitagliptin can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Sitagliptin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Sitagliptin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Sitagliptin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Sitagliptin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Sitagliptin can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Sitagliptin.Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Sitagliptin.Investigational
QuercetinThe serum concentration of Sitagliptin can be increased when it is combined with Quercetin.Experimental
QuetiapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Quetiapine.Approved
QuinacrineThe serum concentration of Sitagliptin can be increased when it is combined with Quinacrine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Quinapril.Approved, Investigational
QuinethazoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Quinethazone.Approved
QuinidineThe serum concentration of Sitagliptin can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Sitagliptin can be increased when it is combined with Quinine.Approved
RabeprazoleThe metabolism of Sitagliptin can be decreased when combined with Rabeprazole.Approved, Investigational
RamiprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Ramipril.Approved
RanitidineThe serum concentration of Sitagliptin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Sitagliptin can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Sitagliptin.Approved
ReboxetineThe serum concentration of Sitagliptin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Sitagliptin can be increased when it is combined with Regorafenib.Approved
RepaglinideSitagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Rescinnamine.Approved
ReserpineThe serum concentration of Sitagliptin can be decreased when it is combined with Reserpine.Approved
RifabutinThe metabolism of Sitagliptin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Sitagliptin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Sitagliptin can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Sitagliptin can be increased when it is combined with Rilpivirine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Sitagliptin.Approved
RisperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe metabolism of Sitagliptin can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Sitagliptin can be increased when it is combined with Rolapitant.Approved
RosiglitazoneThe metabolism of Sitagliptin can be decreased when combined with Rosiglitazone.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Sitagliptin.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Sitagliptin.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Sitagliptin.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Sitagliptin.Approved, Vet Approved
SaquinavirThe metabolism of Sitagliptin can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Sitagliptin can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Sitagliptin can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Sitagliptin can be increased when it is combined with Sertraline.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Sitagliptin.Approved, Investigational
SiltuximabThe serum concentration of Sitagliptin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Sitagliptin.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Sitagliptin.Approved
SirolimusThe serum concentration of Sitagliptin can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Sitagliptin can be increased when it is combined with Sorafenib.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Sitagliptin.Approved
SpiraprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Spirapril.Approved
SpironolactoneThe serum concentration of Sitagliptin can be increased when it is combined with Spironolactone.Approved
St. John's WortThe metabolism of Sitagliptin can be increased when combined with St. John's Wort.Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Sitagliptin.Approved, Vet Approved
StaurosporineThe serum concentration of Sitagliptin can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Sitagliptin can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Sitagliptin can be decreased when it is combined with Streptozocin.Approved
SulfadiazineSitagliptin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sitagliptin can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Sitagliptin can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Sitagliptin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Sitagliptin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Sitagliptin can be increased when it is combined with Sunitinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Sitagliptin.Approved
TacrineThe serum concentration of Sitagliptin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Sitagliptin.Approved, Investigational
TacrolimusThe serum concentration of Sitagliptin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Sitagliptin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe metabolism of Sitagliptin can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Sitagliptin can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Sitagliptin can be increased when it is combined with Telmisartan.Approved, Investigational
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Sitagliptin.Withdrawn
TemocaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Sitagliptin can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Sitagliptin can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe metabolism of Sitagliptin can be decreased when combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Sitagliptin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Sitagliptin can be increased when it is combined with Testosterone.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Sitagliptin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Sitagliptin.Approved
TicagrelorThe serum concentration of Sitagliptin can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Sitagliptin can be decreased when combined with Ticlopidine.Approved
TipranavirThe serum concentration of Sitagliptin can be decreased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Sitagliptin can be decreased when it is combined with Tocilizumab.Approved
TolazamideSitagliptin may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideSitagliptin may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Sitagliptin.Approved
TolvaptanThe serum concentration of Sitagliptin can be increased when it is combined with Tolvaptan.Approved
TorasemideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Torasemide.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Sitagliptin.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Sitagliptin.Approved
TrazodoneThe serum concentration of Sitagliptin can be decreased when it is combined with Trazodone.Approved, Investigational
TriamcinoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Sitagliptin.Approved
TrichlormethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrifluoperazineThe serum concentration of Sitagliptin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Sitagliptin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Sitagliptin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Sitagliptin.Approved
TriptorelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Sitagliptin.Approved, Investigational
VenlafaxineThe metabolism of Sitagliptin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Sitagliptin.Approved
VinblastineThe serum concentration of Sitagliptin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Sitagliptin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Sitagliptin can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Sitagliptin can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Vorinostat.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Sitagliptin.Approved
ZimelidineThe serum concentration of Sitagliptin can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Sitagliptin can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Can be administered without regard to food
References
Synthesis Reference

Nurit Perlman, Marina Etinger, Valerie Niddam-Hildesheim, Mili Abramov, "Preparation of sitagliptin intermediate." U.S. Patent US20090192326, issued July 30, 2009.

US20090192326
General References
  1. Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 Dec;78(6):675-88. [PubMed:16338283 ]
  2. Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA: Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 Aug;46(8):876-86. [PubMed:16855072 ]
  3. Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP: Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 Feb;24(2):489-96. doi: 10.1185/030079908X261069 . [PubMed:18182122 ]
  4. Pratley RE, Salsali A: Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes. Curr Med Res Opin. 2007 Apr;23(4):919-31. [PubMed:17407649 ]
  5. Bergman A, Ebel D, Liu F, Stone J, Wang A, Zeng W, Chen L, Dilzer S, Lasseter K, Herman G, Wagner J, Krishna R: Absolute bioavailability of sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, in healthy volunteers. Biopharm Drug Dispos. 2007 Sep;28(6):315-22. [PubMed:17575559 ]
  6. Richter B, Bandeira-Echtler E, Bergerhoff K, Lerch C: Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes. Vasc Health Risk Manag. 2008;4(4):753-68. [PubMed:19065993 ]
External Links
ATC CodesA10BD12 — Pioglitazone and sitagliptinA10BH51 — Sitagliptin and simvastatinA10BH01 — SitagliptinA10BD07 — Metformin and sitagliptin
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceHealthy Volunteers1
0CompletedTreatmentCongestive Heart Failure (CHF)1
0WithdrawnTreatmentType 2 Diabetes Mellitus1
1CompletedNot AvailableBMI >30 kg/m21
1CompletedNot AvailableDiabetes Mellitus (DM)1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of ASP19411
1CompletedNot AvailableType 2 Diabetes Mellitus1
1CompletedDiagnosticCystic Fibrosis (CF)1
1CompletedDiagnosticType 2 Diabetes Mellitus2
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentDiabetes Mellitus (DM) / Gastroparesis1
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
1CompletedTreatmentDiabetes, Diabetes Mellitus Type 1 / Type 2 Diabetes Mellitus1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentLiver Insufficiency1
1CompletedTreatmentType 2 Diabetes Mellitus23
1CompletedTreatmentType2 Diabetes Mellitus1
1Not Yet RecruitingBasic ScienceType 2 Diabetes Mellitus1
1RecruitingBasic ScienceHealthy Volunteers1
1RecruitingTreatmentHepato Carcinoma1
1TerminatedTreatmentChronic Hepatitis C Infection1
1Unknown StatusTreatmentType 2 Diabetes Mellitus1
1, 2CompletedTreatmentType 2 Diabetes Mellitus1
1, 2Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
2Active Not RecruitingTreatmentAcute Lymphocytic Leukemia (ALL) / Acute Myeloid Leukaemias (AML) / Hematopoetic Myelodysplasia / Leukemia, Myelogenous, Chronic / Non-Hodgkin's Lymphoma (NHL)1
2CompletedNot AvailableType 2 Diabetes Mellitus1
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia, Myelogenous, Chronic / Leukemia, Myeloid, Acute / Myelodysplasia / Non-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentDiabetes1
2CompletedTreatmentDiabetes Mellitus (DM)1
2CompletedTreatmentDiabetes Mellitus (DM) / Gastroparesis1
2CompletedTreatmentDiabetes Mellitus, Non Insulin Dependent / Type 2 Diabetes Mellitus1
2CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
2CompletedTreatmentGlucose tolerance impaired1
2CompletedTreatmentInfection, Human Immunodeficiency Virus I1
2CompletedTreatmentNon- Alcoholic Fatty Liver Disease / Non-Alcoholic Fatty Liver Disease (NAFLD)1
2CompletedTreatmentPsoriasis1
2CompletedTreatmentPsoriasis / Type 2 Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus22
2Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
2RecruitingPreventionPosttransplant Diabetes Mellitus1
2RecruitingTreatmentAtherosclerosis / Inflammatory Reaction1
2RecruitingTreatmentGraft Versus Host Disease (GVHD) / Hematopoietic Stem Cell Transplantation (HSCT)1
2TerminatedBasic ScienceType 2 Diabetes Mellitus1
2TerminatedTreatmentCystic Fibrosis (CF)1
2TerminatedTreatmentDiabetes, Autoimmune / Diabetes, Diabetes Mellitus Type 11
2Unknown StatusHealth Services ResearchGlucose Homeostasis1
2Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
2Unknown StatusTreatmentImpaired Glucose Tolerance (IGT)1
2Unknown StatusTreatmentPre-Diabetic1
2WithdrawnTreatmentType 2 Diabetes Mellitus1
2, 3CompletedNot AvailableDiabetes / Insulin Resistance1
2, 3CompletedBasic ScienceHyperlipidemias1
2, 3CompletedTreatmentDiabetes1
2, 3CompletedTreatmentType 2 Diabetes Mellitus2
2, 3Not Yet RecruitingTreatmentDiabetes Mellitus (DM) / Gastroduodenal Ulcers / Iron Metabolism Disorders / Optic Atrophy / Platelets Dysfunction / Sensorineural Hearing Loss1
2, 3Unknown StatusTreatmentAcute Myocardial Infarction (AMI)1
3Active Not RecruitingTreatmentDiabetes / Type 2 Diabetes Mellitus2
3Active Not RecruitingTreatmentType 2 Diabetes Mellitus5
3CompletedBasic ScienceType 2 Diabetes Mellitus1
3CompletedTreatmentCardiovascular Disease (CVD) / Inflammatory Reaction / Macrophage Infiltration1
3CompletedTreatmentChronic Renal Insufficiency / Type 2 Diabetes Mellitus1
3CompletedTreatmentDiabetes Mellitus (DM) / Postprandial Lipaemia1
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent3
3CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Type 2 Diabetes Mellitus, Non Insulin Dependent1
3CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus5
3CompletedTreatmentEnd-Stage Kidney Disease / Type 2 Diabetes Mellitus1
3CompletedTreatmentHyperlipidemias / Type 2 Diabetes Mellitus1
3CompletedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
3CompletedTreatmentRenal Insufficiency,Chronic / Type 2 Diabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus71
3Not Yet RecruitingTreatmentType 2 Diabetes Mellitus2
3RecruitingPreventionHealthy Volunteers1
3RecruitingTreatmentCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
3RecruitingTreatmentComparative Effectiveness of Glycemia-lowering Medications / Type 2 Diabetes Mellitus1
3RecruitingTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
3RecruitingTreatmentDiabetes / Type 2 Diabetes Mellitus1
3RecruitingTreatmentType 2 Diabetes Mellitus3
3TerminatedPreventionCystic Fibrosis (CF) / Pre-Diabetic1
3TerminatedTreatmentGlycemic Control1
3TerminatedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
3TerminatedTreatmentType 2 Diabetes Mellitus5
3Unknown StatusTreatmentIslet Transplantation1
3Unknown StatusTreatmentType 2 Diabetes Mellitus1
3WithdrawnPreventionType 2 Diabetes Mellitus1
3WithdrawnTreatmentDiabetic Foot1
3WithdrawnTreatmentType 2 Diabetes Mellitus2
4Active Not RecruitingBasic ScienceHealthy Volunteers1
4Active Not RecruitingTreatmentDisorder of Glucose Regulation1
4CompletedNot AvailableHealthy Volunteers1
4CompletedBasic ScienceAtherosclerosis / Diabetes1
4CompletedBasic ScienceHealthy Volunteers / Type 2 Diabetes Mellitus1
4CompletedBasic ScienceHypertensive / Metabolic Syndromes1
4CompletedBasic ScienceType 2 Diabetes Mellitus3
4CompletedOtherBMI >30 kg/m21
4CompletedPreventionCoronary Artery Disease1
4CompletedPreventionPolycystic Ovarian Syndrome1
4CompletedTreatmentBody Weights / Polycystic Ovaries Syndrome1
4CompletedTreatmentCoronary Artery Disease / Newly Diagnosed Type 2 Diabetes1
4CompletedTreatmentDIABETES Mellitus Type 2 Not Well Controlled1
4CompletedTreatmentDiabetes3
4CompletedTreatmentDiabetes Ketoacidosis / Hyperglycemias / Ketosis Prone Diabetes1
4CompletedTreatmentDiabetes Mellitus (DM)2
4CompletedTreatmentDiabetes Mellitus (DM) / Impaired Glucose Tolerance (IGT) / Myocardial Infarction (MI) / Unstable Angina Pectoris1
4CompletedTreatmentDiabetes, Diabetes Mellitus Type 13
4CompletedTreatmentDiabetes / Pancreatitis1
4CompletedTreatmentDiabetes / Type 2 Diabetes Mellitus3
4CompletedTreatmentGlucose tolerance impaired1
4CompletedTreatmentHospitalization / Hyperglycemias / Type 2 Diabetes Mellitus1
4CompletedTreatmentPre-Diabetic1
4CompletedTreatmentReactive Hypoglycemia1
4CompletedTreatmentType 2 Diabetes Mellitus25
4Enrolling by InvitationTreatmentBMI >30 kg/m2 / General Surgery / Hypoglycemia1
4Enrolling by InvitationTreatmentType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentCoronary Heart Disease (CHD) / Diabetes Mellitus (DM)1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4RecruitingNot AvailablePolycystic Ovaries Syndrome1
4RecruitingNot AvailableType 2 Diabetes Mellitus1
4RecruitingBasic ScienceBMI >30 kg/m2 / Pre-Diabetic1
4RecruitingBasic ScienceType 2 Diabetes Mellitus1
4RecruitingHealth Services ResearchType 2 Diabetes Mellitus1
4RecruitingPreventionHyperglycemias2
4RecruitingSupportive CareAcromegaly / Cushing's Disease1
4RecruitingTreatmentAcute Coronary Syndromes (ACS) / Type 2 Diabetes Mellitus1
4RecruitingTreatmentAtherosclerosis / Type 2 Diabetes Mellitus1
4RecruitingTreatmentCholesterol, LDL / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Dipeptidyl-Peptidase 4 Inhibitors / Glycosylated Hemoglobin1
4RecruitingTreatmentDiabetes Mellitus (DM)1
4RecruitingTreatmentHeart Failure, Systolic / Type 2 Diabetes Mellitus1
4RecruitingTreatmentHeart Failure, Unspecified / Type 2 Diabetes Mellitus1
4RecruitingTreatmentNeoplasms, Adipose Tissue1
4RecruitingTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD)1
4RecruitingTreatmentShort Bowel Syndrome (SBS)1
4RecruitingTreatmentType 2 Diabetes Mellitus9
4RecruitingTreatmentType II Diabetes in Subjects BMI 27 to 32 / Type II Diabetes in the Not so Obese1
4TerminatedTreatmentDiabetes / Hypoglycemia1
4TerminatedTreatmentHyperglycemias / Type 2 Diabetes Mellitus1
4TerminatedTreatmentMicroalbuminuria / Microalbuminuria in Type Two Diabetes / Type 2 Diabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus5
4Unknown StatusNot AvailableType 2 Diabetes Mellitus1
4Unknown StatusBasic ScienceType 2 Diabetes Mellitus1
4Unknown StatusPreventionDiabetes / Transplant, Kidney1
4Unknown StatusTreatmentChronic Liver Diseases (CLD) / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentDiabetes, Diabetes Mellitus Type 11
4Unknown StatusTreatmentType 2 Diabetes Mellitus4
4WithdrawnTreatmentNon-Alcoholic Fatty Liver Disease (NAFLD) / Type 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingTreatmentDiabetes1
Not AvailableCompletedNot AvailableDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
Not AvailableCompletedNot AvailableDiabetes / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus9
Not AvailableCompletedBasic ScienceObesity, Severe1
Not AvailableCompletedPreventionBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
Not AvailableCompletedPreventionBeta-cell Function / Diabetes Mellitus (DM) / Glucocorticoid-induced Diabetes / Steroid Diabetes1
Not AvailableCompletedSupportive CareDiabetes, Diabetes Mellitus Type 11
Not AvailableCompletedTreatmentBMI >30 kg/m21
Not AvailableCompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
Not AvailableCompletedTreatmentHypertensive / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentPre-Diabetic / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus6
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus / Type2 Diabetes Mellitus1
Not AvailableNot Yet RecruitingNot AvailableType 2 Diabetes Mellitus3
Not AvailableNot Yet RecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableRecruitingBasic SciencePhysiology1
Not AvailableRecruitingOtherCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
Not AvailableRecruitingOtherCystic Fibrosis (CF) / Pancreatic Insufficiency1
Not AvailableRecruitingOtherType 2 Diabetes Mellitus1
Not AvailableRecruitingPreventionIncretinomimetics / Pancreas / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentHypertensive / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableTerminatedNot AvailableType 2 Diabetes Mellitus1
Not AvailableTerminatedPreventionPrediabetic State1
Not AvailableTerminatedTreatmentNonalcoholic Steatohepatitis / Type 2 Diabetes Mellitus1
Not AvailableUnknown StatusNot AvailableArterial Stiffness / Diabetes Mellitus (DM)1
Not AvailableUnknown StatusTreatmentDiabetes Type I1
Not AvailableUnknown StatusTreatmentTransplant, Kidney / Type 2 Diabetes Mellitus1
Not AvailableUnknown StatusTreatmentType 2 Diabetes Mellitus3
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
Tablet, extended releaseOral
Tablet, film coated, extended releaseOral
TabletOral100 mg
TabletOral25 mg
TabletOral50 mg
Tablet, film coatedOral100 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral25 mg
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
Tablet, film coatedOral50 mg
Prices
Unit descriptionCostUnit
Januvia 90 25 mg tablet Bottle686.36USD bottle
Januvia 30 100 mg tablet Bottle228.81USD bottle
Januvia 50 mg tablet7.48USD tablet
Januvia 100 mg tablet7.33USD tablet
Januvia 25 mg tablet7.33USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2536251 No2009-08-042024-08-27Canada
CA2450740 No2006-02-142022-07-05Canada
US7326708 No2006-04-112026-04-11Us
US6699871 No2002-07-262022-07-26Us
US7125873 No2002-07-262022-07-26Us
US8414921 No2008-07-212028-07-21Us
US6340475 No1996-09-192016-09-19Us
US6635280 No1996-09-192016-09-19Us
US6303661 No1997-04-242017-04-24Us
US6890898 No1999-02-022019-02-02Us
US7078381 No1999-02-022019-02-02Us
US7459428 No1999-02-022019-02-02Us
US8168637 No2002-06-262022-06-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.034 mg/mLALOGPS
logP1.95ALOGPS
logP1.26ChemAxon
logS-4.1ALOGPS
pKa (Strongest Basic)8.78ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area77.04 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity87.49 m3·mol-1ChemAxon
Polarizability32.66 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9438
Caco-2 permeable-0.6415
P-glycoprotein substrateSubstrate0.6509
P-glycoprotein inhibitor IInhibitor0.7141
P-glycoprotein inhibitor IIInhibitor0.5248
Renal organic cation transporterInhibitor0.592
CYP450 2C9 substrateNon-substrate0.9277
CYP450 2D6 substrateNon-substrate0.7228
CYP450 3A4 substrateSubstrate0.6412
CYP450 1A2 substrateNon-inhibitor0.7178
CYP450 2C9 inhibitorInhibitor0.6111
CYP450 2D6 inhibitorNon-inhibitor0.538
CYP450 2C19 inhibitorInhibitor0.7048
CYP450 3A4 inhibitorInhibitor0.5358
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8336
Ames testNon AMES toxic0.5487
CarcinogenicityNon-carcinogens0.7973
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8093 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7076
hERG inhibition (predictor II)Inhibitor0.6936
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted GC-MSPredicted GC-MS Spectrum - GC-MSNot Available
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-0a4i-0000900000-ce9211ae5927c697618cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-052r-0690500000-c28779e719a0e517d106View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-0076-0930000000-1337dd7fb10ab92722b5View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-00dl-0900000000-91485eb0052ad2f3637aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QTOF , positivesplash10-00di-0900000000-7d92431093315efaed86View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-000i-0390000000-c8853d370b51f01b194bView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-0a4i-0000900000-2895dd4a879799635ae6View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-007c-0970100000-17431cd80097dff5c35fView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-00dl-0910000000-29041ebd42cb7f6026dfView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-00di-0900000000-dc60c3b1e5f0ba0e5e23View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-0umi-0900000000-b1e1f886377c8d9b2a5dView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-004i-0900000000-d9e2b332d0ff3c6e283bView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-0a4i-0000900000-3403c0e74f19a7d0832aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-007c-0970000000-6aa1fc14d171d0102a2cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-00dl-0910000000-62ba59074d19e0d89306View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-00di-0900000000-91600010aa7e80c0e67cView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-0fmi-0900000000-d38f8b74df088a3b8232View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-004i-0900000000-08cf9f4ac284f2cd9057View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT , positivesplash10-000i-0390000000-b6e5cd73f4ff7abd2747View in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as beta amino acids and derivatives. These are amino acids having a (-NH2) group attached to the beta carbon atom.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentBeta amino acids and derivatives
Alternative ParentsAmphetamines and derivatives / Triazolopyrazines / Aralkylamines / Fluorobenzenes / Pyrazines / Aryl fluorides / Triazoles / Tertiary carboxylic acid amides / Heteroaromatic compounds / Azacyclic compounds
SubstituentsBeta amino acid or derivatives / Amphetamine or derivatives / Triazolopyrazine / Fluorobenzene / Halobenzene / Aralkylamine / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Pyrazine
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptorstrifluorobenzene, triazolopyrazine (CHEBI:40237 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Virus receptor activity
Specific Function:
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also ...
Gene Name:
DPP4
Uniprot ID:
P27487
Uniprot Name:
Dipeptidyl peptidase 4
Molecular Weight:
88277.935 Da
References
  1. Herman GA, Stevens C, Van Dyck K, Bergman A, Yi B, De Smet M, Snyder K, Hilliard D, Tanen M, Tanaka W, Wang AQ, Zeng W, Musson D, Winchell G, Davies MJ, Ramael S, Gottesdiener KM, Wagner JA: Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 Dec;78(6):675-88. [PubMed:16338283 ]
  2. Bergman AJ, Stevens C, Zhou Y, Yi B, Laethem M, De Smet M, Snyder K, Hilliard D, Tanaka W, Zeng W, Tanen M, Wang AQ, Chen L, Winchell G, Davies MJ, Ramael S, Wagner JA, Herman GA: Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther. 2006 Jan;28(1):55-72. [PubMed:16490580 ]
  3. Gallwitz B: Therapies for the treatment of type 2 diabetes mellitus based on incretin action. Minerva Endocrinol. 2006 Jun;31(2):133-47. [PubMed:16682937 ]
  4. Herman GA, Bergman A, Liu F, Stevens C, Wang AQ, Zeng W, Chen L, Snyder K, Hilliard D, Tanen M, Tanaka W, Meehan AG, Lasseter K, Dilzer S, Blum R, Wagner JA: Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 Aug;46(8):876-86. [PubMed:16855072 ]
  5. Miller S, St Onge EL: Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Ann Pharmacother. 2006 Jul-Aug;40(7-8):1336-43. [PubMed:16868220 ]
  6. Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP: Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 Feb;24(2):489-96. doi: 10.1185/030079908X261069 . [PubMed:18182122 ]
  7. Pratley RE, Salsali A: Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes. Curr Med Res Opin. 2007 Apr;23(4):919-31. [PubMed:17407649 ]
  8. Lyseng-Williamson KA: Sitagliptin. Drugs. 2007;67(4):587-97. [PubMed:17352516 ]
  9. Hermansen K, Kipnes M, Luo E, Fanurik D, Khatami H, Stein P: Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin. Diabetes Obes Metab. 2007 Sep;9(5):733-45. Epub 2007 Jun 26. [PubMed:17593236 ]
  10. Gallwitz B: Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes. Drugs Today (Barc). 2007 Jan;43(1):13-25. [PubMed:17315049 ]
  11. Richter B, Bandeira-Echtler E, Bergerhoff K, Lerch C: Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes. Vasc Health Risk Manag. 2008;4(4):753-68. [PubMed:19065993 ]
  12. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da
References
  1. Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [PubMed:20590741 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Uniprot Name:
Cytochrome P450 2C8
Molecular Weight:
55824.275 Da
References
  1. Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [PubMed:20590741 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Uniprot Name:
Multidrug resistance protein 1
Molecular Weight:
141477.255 Da
References
  1. Scheen AJ: Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab. 2010 Aug;12(8):648-58. doi: 10.1111/j.1463-1326.2010.01212.x. [PubMed:20590741 ]
Drug created on May 16, 2007 11:36 / Updated on September 01, 2017 10:38