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Identification
NameSitagliptin
Accession NumberDB01261  (DB07214)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionSitagliptin 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 Identifiers
  • MK-0431
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Januviatablet, film coated50 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated50 mg/1oralMerck Sharp & Dohme Corp.2006-10-16Not applicableUs
Januviatablet25 mgoralMerck Canada Inc2012-09-17Not applicableCanada
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralREMEDYREPACK INC.2014-03-03Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated25 mg/1oralMerck Sharp & Dohme Corp.2006-10-16Not applicableUs
Januviatablet50 mgoralMerck Canada Inc2012-09-17Not applicableCanada
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated50 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralPhysicians Total Care, Inc.2007-12-13Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated50 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralMerck Sharp & Dohme Corp.2006-10-16Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralClinical Solutions Wholesale2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated50 mg/1oralPhysicians Total Care, Inc.2009-05-06Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralCardinal Health2006-10-16Not applicableUs
JanuviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet100 mgOral use Page 2 of 2Merck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet, film coated100 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-09Not applicableUs
JanuviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Januviatablet100 mgoralMerck Canada Inc2008-01-02Not applicableCanada
JanuviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
RistabenFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2010-03-15Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
TesavelFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2008-01-10Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet50 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet100 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
XeleviaFilm-coated tablet25 mgOral useMerck Sharp & Dohme Ltd2007-03-21Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
XeleviaNot Available
Brand mixtures
NameLabellerIngredients
JanumetMerck Sharp & Dohme Corp.
Janumet XRMerck Sharp & Dohme Corp.
SaltsNot Available
Categories
UNIIQFP0P1DV7Z
CAS number486460-32-6
WeightAverage: 407.3136
Monoisotopic: 407.118079357
Chemical FormulaC16H15F6N5O
InChI KeyInChIKey=MFFMDFFZMYYVKS-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[C@@H](CC(=O)N1CCN2C(C1)=NN=C2C(F)(F)F)CC1=CC(F)=C(F)C=C1F
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 Parents
Substituents
  • Beta amino acid or derivatives
  • Amphetamine or derivatives
  • Triazolopyrazine
  • Aralkylamine
  • Halobenzene
  • Fluorobenzene
  • Benzenoid
  • Pyrazine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Triazole
  • Tertiary carboxylic acid amide
  • Azole
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor 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.
PharmacodynamicsSitagliptin 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 actionSitagliptin 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.
Related Articles
AbsorptionRapidly absorbed following oral administration, with an absolute bioavailability of 87%.
Volume of distribution
  • 198 L [healthy subjects]
Protein bindingThe 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 eliminationApproximately 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 life12.4 hours
Clearance
  • renal cl=350 mL/min [Healthy subjects receiving 100 mg oral dose]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tablet, film coatedoral
Tablet (extended-release)oral
Tablet, film coated, extended releaseoral
Film-coated tabletOral use100 mg
Film-coated tabletOral use25 mg
Film-coated tabletOral use50 mg
Film-coated tabletOral use Page 2 of 2100 mg
Tabletoral100 mg
Tabletoral25 mg
Tabletoral50 mg
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral50 mg/1
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)
CA2450740 No2006-02-142022-07-05Canada
CA2536251 No2009-08-042024-08-27Canada
US6303661 No1997-04-242017-04-24Us
US6340475 No1996-09-192016-09-19Us
US6635280 No1996-09-192016-09-19Us
US6699871 No2002-07-262022-07-26Us
US6890898 No1999-02-022019-02-02Us
US7078381 No1999-02-022019-02-02Us
US7125873 No2002-07-262022-07-26Us
US7326708 No2006-04-112026-04-11Us
US7459428 No1999-02-022019-02-02Us
US8168637 No2002-06-262022-06-26Us
US8414921 No2008-07-212028-07-21Us
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
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
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 CodesA10BH51A10BD12A10BH01A10BD07
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Sitagliptin.
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Sitagliptin.
AbirateroneThe serum concentration of Sitagliptin can be increased when it is combined with Abiraterone.
AcetaminophenThe serum concentration of Sitagliptin can be increased when it is combined with Acetaminophen.
AcetohexamideSitagliptin may increase the hypoglycemic activities of Acetohexamide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Sitagliptin.
AfatinibThe serum concentration of Sitagliptin can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Sitagliptin can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Sitagliptin can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Sitagliptin can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Sitagliptin can be increased when it is combined with Alfentanil.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Sitagliptin.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Sitagliptin.
AmantadineThe serum concentration of Sitagliptin can be increased when it is combined with Amantadine.
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Sitagliptin.
Aminohippuric acidThe serum concentration of Sitagliptin can be increased when it is combined with Aminohippuric acid.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Sitagliptin.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Sitagliptin.
AmiodaroneThe serum concentration of Sitagliptin can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Sitagliptin.
AmlodipineThe serum concentration of Sitagliptin can be increased when it is combined with Amlodipine.
AmoxapineAmoxapine may increase the hypoglycemic activities of Sitagliptin.
AmprenavirThe serum concentration of Sitagliptin can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Sitagliptin can be increased when it is combined with Amsacrine.
AprepitantThe serum concentration of Sitagliptin can be increased when it is combined with Aprepitant.
AripiprazoleThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Aripiprazole.
Arsenic trioxideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Asenapine.
AstemizoleThe serum concentration of Sitagliptin can be increased when it is combined with Astemizole.
AtazanavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Atazanavir.
AtenololThe serum concentration of Sitagliptin can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Sitagliptin can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Sitagliptin.
AzelastineThe serum concentration of Sitagliptin can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Sitagliptin can be increased when it is combined with Azithromycin.
BenazeprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Benazepril.
BendroflumethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Bendroflumethiazide.
BenmoxinBenmoxin may increase the hypoglycemic activities of Sitagliptin.
BenzocaineThe serum concentration of Sitagliptin can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Sitagliptin can be increased when it is combined with Bepridil.
BetamethasoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Betamethasone.
BexaroteneThe serum concentration of Sitagliptin can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Sitagliptin can be increased when it is combined with Biperiden.
BoceprevirThe serum concentration of Sitagliptin can be decreased when it is combined with Boceprevir.
BortezomibThe metabolism of Sitagliptin can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Sitagliptin can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Sitagliptin can be increased when it is combined with Bosutinib.
BrexpiprazoleThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Brexpiprazole.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Sitagliptin.
BumetanideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Bumetanide.
BuprenorphineThe serum concentration of Sitagliptin can be increased when it is combined with Buprenorphine.
BuserelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Buserelin.
BuspironeThe serum concentration of Sitagliptin can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Sitagliptin can be increased when it is combined with Cabazitaxel.
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Sitagliptin.
CaffeineThe serum concentration of Sitagliptin can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Sitagliptin can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Sitagliptin can be increased when it is combined with Candesartan.
CandoxatrilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Candoxatril.
CaptoprilThe serum concentration of Sitagliptin can be increased when it is combined with Captopril.
CaptoprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Captopril.
CarbamazepineThe serum concentration of Sitagliptin can be decreased when it is combined with Carbamazepine.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Sitagliptin.
CarvedilolThe serum concentration of Sitagliptin can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Sitagliptin can be increased when it is combined with Caspofungin.
CelecoxibThe metabolism of Sitagliptin can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Sitagliptin can be increased when it is combined with Ceritinib.
ChloroquineThe serum concentration of Sitagliptin can be increased when it is combined with Chloroquine.
ChlorothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Chlorothiazide.
ChlorpromazineThe serum concentration of Sitagliptin can be increased when it is combined with Chlorpromazine.
ChlorpropamideSitagliptin may increase the hypoglycemic activities of Chlorpropamide.
ChlorpropamideThe serum concentration of Sitagliptin can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Sitagliptin can be increased when it is combined with Chlorprothixene.
ChlorthalidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Chlorthalidone.
CholesterolThe serum concentration of Sitagliptin can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Sitagliptin can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Sitagliptin can be increased when it is combined with Cilazapril.
CilazaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Cilazapril.
CimetidineThe serum concentration of Sitagliptin can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Ciprofloxacin.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Sitagliptin.
CitalopramCitalopram may increase the hypoglycemic activities of Sitagliptin.
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Sitagliptin.
ClarithromycinThe serum concentration of Sitagliptin can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Sitagliptin can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Sitagliptin can be increased when it is combined with Clofazimine.
ClomipramineClomipramine may increase the hypoglycemic activities of Sitagliptin.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Sitagliptin.
ClopidogrelThe metabolism of Sitagliptin can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Sitagliptin can be decreased when combined with Clotrimazole.
ClozapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Clozapine.
CobicistatThe serum concentration of Sitagliptin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Sitagliptin can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Sitagliptin can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Sitagliptin can be increased when it is combined with Conivaptan.
CorticotropinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Cortisone acetate.
CrizotinibThe metabolism of Sitagliptin can be decreased when combined with Crizotinib.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Sitagliptin.
CyclophosphamideThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Cyclophosphamide.
CyclophosphamideThe serum concentration of Sitagliptin can be increased when it is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Sitagliptin.
CyclosporineThe metabolism of Sitagliptin can be decreased when combined with Cyclosporine.
Cyproterone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Dabrafenib.
DaclatasvirThe serum concentration of Sitagliptin can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Sitagliptin can be increased when it is combined with Dactinomycin.
DanazolThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Danazol.
DapoxetineDapoxetine may increase the hypoglycemic activities of Sitagliptin.
DarunavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Darunavir.
DasatinibThe serum concentration of Sitagliptin can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Sitagliptin can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Sitagliptin can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Sitagliptin.
DelavirdineThe metabolism of Sitagliptin can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Sitagliptin.
DesloratadineThe serum concentration of Sitagliptin can be increased when it is combined with Desloratadine.
DesogestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Dexamethasone.
DextromethorphanThe serum concentration of Sitagliptin can be increased when it is combined with Dextromethorphan.
DiazoxideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Diazoxide.
DiclofenacThe serum concentration of Sitagliptin can be increased when it is combined with Diclofenac.
DienogestThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the hypoglycemic activities of Sitagliptin.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Sitagliptin.
DigoxinThe serum concentration of Sitagliptin can be decreased when it is combined with Digoxin.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Sitagliptin.
DihydroergotamineThe metabolism of Sitagliptin can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Sitagliptin.
DiltiazemThe metabolism of Sitagliptin can be decreased when combined with Diltiazem.
DipyridamoleThe serum concentration of Sitagliptin can be increased when it is combined with Dipyridamole.
DisopyramideSitagliptin may increase the hypoglycemic activities of Disopyramide.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Sitagliptin.
DoxazosinThe serum concentration of Sitagliptin can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Sitagliptin.
DoxorubicinThe serum concentration of Sitagliptin can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Sitagliptin can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Sitagliptin can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Sitagliptin can be decreased when combined with Dronedarone.
DrospirenoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Drospirenone.
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Sitagliptin.
EfavirenzThe serum concentration of Sitagliptin can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Sitagliptin can be increased when it is combined with Elbasvir.
EnalaprilThe serum concentration of Sitagliptin can be increased when it is combined with Enalapril.
EnalaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Enalaprilat.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Sitagliptin.
EnzalutamideThe serum concentration of Sitagliptin can be increased when it is combined with Enzalutamide.
EpinephrineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Epinephrine.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Sitagliptin.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Sitagliptin.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Sitagliptin.
ErythromycinThe metabolism of Sitagliptin can be decreased when combined with Erythromycin.
EscitalopramEscitalopram may increase the hypoglycemic activities of Sitagliptin.
Eslicarbazepine acetateThe serum concentration of Sitagliptin can be decreased when it is combined with Eslicarbazepine acetate.
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Sitagliptin.
EstradiolThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Estradiol.
EstramustineThe serum concentration of Sitagliptin can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Sitagliptin can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Sitagliptin can be decreased when it is combined with Estrone.
Estrone sulfateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Etacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Etonogestrel.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Sitagliptin.
EtoposideThe serum concentration of Sitagliptin can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Sitagliptin.
EverolimusThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Everolimus.
FelodipineThe serum concentration of Sitagliptin can be increased when it is combined with Felodipine.
FenfluramineFenfluramine may increase the hypoglycemic activities of Sitagliptin.
FentanylThe serum concentration of Sitagliptin can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Sitagliptin can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Sitagliptin can be increased when it is combined with Fidaxomicin.
FluconazoleThe metabolism of Sitagliptin can be decreased when combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Fludrocortisone.
FluoxetineFluoxetine may increase the hypoglycemic activities of Sitagliptin.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Sitagliptin.
FlupentixolThe serum concentration of Sitagliptin can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Sitagliptin can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Sitagliptin can be increased when it is combined with Flurazepam.
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Sitagliptin.
FosamprenavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Fosamprenavir.
FosaprepitantThe serum concentration of Sitagliptin can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Fosinopril.
FosphenytoinThe metabolism of Sitagliptin can be increased when combined with Fosphenytoin.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Sitagliptin.
FurosemideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Furosemide.
Fusidic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Fusidic Acid.
GarlicThe serum concentration of Sitagliptin can be decreased when it is combined with Garlic.
GefitinibThe serum concentration of Sitagliptin can be increased when it is combined with Gefitinib.
GemfibrozilThe metabolism of Sitagliptin can be decreased when combined with Gemfibrozil.
GenisteinThe serum concentration of Sitagliptin can be increased when it is combined with Genistein.
GlibornurideSitagliptin may increase the hypoglycemic activities of Glibornuride.
GliclazideSitagliptin may increase the hypoglycemic activities of Gliclazide.
GlimepirideSitagliptin may increase the hypoglycemic activities of Glimepiride.
GlipizideSitagliptin may increase the hypoglycemic activities of Glipizide.
GliquidoneSitagliptin may increase the hypoglycemic activities of Gliquidone.
GlisoxepideSitagliptin may increase the hypoglycemic activities of Glisoxepide.
GlyburideSitagliptin may increase the hypoglycemic activities of Glyburide.
GlyburideThe serum concentration of Sitagliptin can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Sitagliptin can be increased when it is combined with Glycerol.
GoserelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Goserelin.
Gramicidin DThe serum concentration of Sitagliptin can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Sitagliptin can be increased when it is combined with Haloperidol.
HistrelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Histrelin.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Sitagliptin.
HydrochlorothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.
IdelalisibThe serum concentration of Sitagliptin can be increased when it is combined with Idelalisib.
IloperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Iloperidone.
ImatinibThe metabolism of Sitagliptin can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Sitagliptin.
IndalpineIndalpine may increase the hypoglycemic activities of Sitagliptin.
IndapamideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Indinavir.
IndomethacinThe serum concentration of Sitagliptin can be increased when it is combined with Indomethacin.
Insulin AspartSitagliptin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirSitagliptin may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineSitagliptin may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineSitagliptin may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanSitagliptin may increase the hypoglycemic activities of Insulin Human.
Insulin LisproSitagliptin may increase the hypoglycemic activities of Insulin Lispro.
Insulin PorkSitagliptin may increase the hypoglycemic activities of Insulin Pork.
IproclozideIproclozide may increase the hypoglycemic activities of Sitagliptin.
IproniazidIproniazid may increase the hypoglycemic activities of Sitagliptin.
IrbesartanThe metabolism of Sitagliptin can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Sitagliptin can be decreased when combined with Isavuconazonium.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Sitagliptin.
IsradipineThe metabolism of Sitagliptin can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Sitagliptin can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Sitagliptin can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Sitagliptin can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Ketoconazole.
LanreotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lanreotide.
LanreotideSitagliptin may increase the hypoglycemic activities of Lanreotide.
LansoprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Sitagliptin can be increased when it is combined with Lapatinib.
LeuprolideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Leuprolide.
LevofloxacinThe serum concentration of Sitagliptin can be increased when it is combined with Levofloxacin.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Sitagliptin.
LevonorgestrelThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Levonorgestrel.
LevothyroxineThe serum concentration of Sitagliptin can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Sitagliptin can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Sitagliptin can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Sitagliptin can be decreased when it is combined with Liotrix.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Sitagliptin.
LisinoprilThe serum concentration of Sitagliptin can be increased when it is combined with Lisinopril.
LisinoprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Lisinopril.
LomitapideThe serum concentration of Sitagliptin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Sitagliptin can be increased when it is combined with Loperamide.
LopinavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lopinavir.
LoratadineThe serum concentration of Sitagliptin can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Sitagliptin can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Sitagliptin.
LovastatinThe metabolism of Sitagliptin can be decreased when combined with Lovastatin.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Sitagliptin.
LuliconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Sitagliptin can be decreased when it is combined with Lumacaftor.
LurasidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Lurasidone.
MaprotilineThe serum concentration of Sitagliptin can be increased when it is combined with Maprotiline.
MebanazineMebanazine may increase the hypoglycemic activities of Sitagliptin.
MebendazoleThe serum concentration of Sitagliptin can be increased when it is combined with Mebendazole.
MecaserminSitagliptin may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Medroxyprogesterone acetate.
MefloquineThe serum concentration of Sitagliptin can be increased when it is combined with Mefloquine.
Megestrol acetateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Megestrol acetate.
MeprobamateThe serum concentration of Sitagliptin can be increased when it is combined with Meprobamate.
MesalazineMesalazine may increase the hypoglycemic activities of Sitagliptin.
MestranolThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Mestranol.
MethadoneThe serum concentration of Sitagliptin can be increased when it is combined with Methadone.
MethotrimeprazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methyclothiazide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Sitagliptin.
MethylprednisoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Methylprednisolone.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Sitagliptin.
MetolazoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Metolazone.
MetoprololThe serum concentration of Sitagliptin can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Sitagliptin can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Sitagliptin.
MidazolamThe serum concentration of Sitagliptin can be decreased when it is combined with Midazolam.
MifepristoneSitagliptin may increase the hypoglycemic activities of Mifepristone.
MifepristoneThe metabolism of Sitagliptin can be decreased when combined with Mifepristone.
MilnacipranMilnacipran may increase the hypoglycemic activities of Sitagliptin.
MinaprineMinaprine may increase the hypoglycemic activities of Sitagliptin.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Sitagliptin.
MitomycinThe serum concentration of Sitagliptin can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Sitagliptin can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Sitagliptin can be decreased when it is combined with Mitoxantrone.
MoclobemideMoclobemide may increase the hypoglycemic activities of Sitagliptin.
ModafinilThe serum concentration of Sitagliptin can be decreased when it is combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Moexipril.
MorphineThe serum concentration of Sitagliptin can be increased when it is combined with Morphine.
NafcillinThe serum concentration of Sitagliptin can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Sitagliptin can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Sitagliptin can be increased when it is combined with Naringenin.
NateglinideSitagliptin may increase the hypoglycemic activities of Nateglinide.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Sitagliptin.
NefazodoneThe serum concentration of Sitagliptin can be decreased when it is combined with Nefazodone.
NelfinavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Nelfinavir.
NeostigmineThe serum concentration of Sitagliptin can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Sitagliptin can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Sitagliptin can be decreased when combined with Nevirapine.
NiacinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Niacin.
NialamideNialamide may increase the hypoglycemic activities of Sitagliptin.
NicardipineThe serum concentration of Sitagliptin can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Sitagliptin can be decreased when it is combined with Nifedipine.
NilotinibThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Nilotinib.
NisoldipineThe serum concentration of Sitagliptin can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Sitagliptin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Sitagliptin can be increased when it is combined with Nitrendipine.
NorethisteroneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Norgestimate.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Sitagliptin.
OctamoxinOctamoxin may increase the hypoglycemic activities of Sitagliptin.
OctreotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Octreotide.
OctreotideSitagliptin may increase the hypoglycemic activities of Octreotide.
OlanzapineOlanzapine may increase the hypoglycemic activities of Sitagliptin.
OlaparibThe metabolism of Sitagliptin can be decreased when combined with Olaparib.
OmapatrilatThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Omapatrilat.
OmeprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Sitagliptin can be increased when it is combined with Osimertinib.
OxandroloneOxandrolone may increase the hypoglycemic activities of Sitagliptin.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Sitagliptin.
P-NitrophenolThe serum concentration of Sitagliptin can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Sitagliptin can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Sitagliptin can be increased when it is combined with Palbociclib.
PaliperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Paliperidone.
Palmitic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Sitagliptin can be increased when it is combined with Pantoprazole.
PargylinePargyline may increase the hypoglycemic activities of Sitagliptin.
ParoxetineParoxetine may increase the hypoglycemic activities of Sitagliptin.
PasireotideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pasireotide.
PasireotideSitagliptin may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Sitagliptin.
PentamidineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pentamidine.
PentamidineSitagliptin may increase the hypoglycemic activities of Pentamidine.
PentobarbitalThe metabolism of Sitagliptin can be increased when combined with Pentobarbital.
PerindoprilThe serum concentration of Sitagliptin can be increased when it is combined with Perindopril.
PerindoprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Perindopril.
PethidineThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Pethidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Sitagliptin.
PheniprazinePheniprazine may increase the hypoglycemic activities of Sitagliptin.
PhenobarbitalThe serum concentration of Sitagliptin can be decreased when it is combined with Phenobarbital.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Sitagliptin.
PhenytoinThe metabolism of Sitagliptin can be increased when combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Sitagliptin.
PioglitazoneThe metabolism of Sitagliptin can be decreased when combined with Pioglitazone.
PiperazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Pipotiazine.
PirlindolePirlindole may increase the hypoglycemic activities of Sitagliptin.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Sitagliptin.
Platelet Activating FactorThe serum concentration of Sitagliptin can be decreased when it is combined with Platelet Activating Factor.
PolythiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Polythiazide.
PonatinibThe serum concentration of Sitagliptin can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Sitagliptin can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Sitagliptin can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Sitagliptin can be increased when it is combined with Prazosin.
PrednisoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Prednisone.
PrimidoneThe metabolism of Sitagliptin can be increased when combined with Primidone.
ProbenecidThe serum concentration of Sitagliptin can be increased when it is combined with Probenecid.
ProgesteroneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Progesterone.
PromethazineThe serum concentration of Sitagliptin can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Sitagliptin can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Sitagliptin can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Sitagliptin.
QuercetinThe serum concentration of Sitagliptin can be increased when it is combined with Quercetin.
QuetiapineThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Quetiapine.
QuinacrineThe serum concentration of Sitagliptin can be increased when it is combined with Quinacrine.
QuinaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Quinapril.
QuinethazoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Quinethazone.
QuinidineThe serum concentration of Sitagliptin can be increased when it is combined with Quinidine.
QuinineSitagliptin may increase the hypoglycemic activities of Quinine.
QuinineThe serum concentration of Sitagliptin can be increased when it is combined with Quinine.
RabeprazoleThe metabolism of Sitagliptin can be decreased when combined with Rabeprazole.
RamiprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Ramipril.
RanitidineThe serum concentration of Sitagliptin can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Sitagliptin can be increased when it is combined with Ranolazine.
RasagilineRasagiline may increase the hypoglycemic activities of Sitagliptin.
ReboxetineThe serum concentration of Sitagliptin can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Sitagliptin can be increased when it is combined with Regorafenib.
RepaglinideSitagliptin may increase the hypoglycemic activities of Repaglinide.
RescinnamineThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Rescinnamine.
ReserpineThe serum concentration of Sitagliptin can be decreased when it is combined with Reserpine.
RifabutinThe metabolism of Sitagliptin can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Sitagliptin can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Sitagliptin can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Sitagliptin can be increased when it is combined with Rilpivirine.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Sitagliptin.
RisperidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Ritonavir.
RolapitantThe serum concentration of Sitagliptin can be increased when it is combined with Rolapitant.
RosiglitazoneThe metabolism of Sitagliptin can be decreased when combined with Rosiglitazone.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Sitagliptin.
SafrazineSafrazine may increase the hypoglycemic activities of Sitagliptin.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Sitagliptin.
SaquinavirThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Saquinavir.
ScopolamineThe serum concentration of Sitagliptin can be increased when it is combined with Scopolamine.
SecobarbitalThe metabolism of Sitagliptin can be increased when combined with Secobarbital.
SelegilineSelegiline may increase the hypoglycemic activities of Sitagliptin.
SertralineSertraline may increase the hypoglycemic activities of Sitagliptin.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Sitagliptin.
SildenafilThe metabolism of Sitagliptin can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Sitagliptin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Sitagliptin can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Sitagliptin.
SirolimusThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Sirolimus.
SorafenibThe serum concentration of Sitagliptin can be increased when it is combined with Sorafenib.
SpiraprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Spirapril.
SpironolactoneThe serum concentration of Sitagliptin can be increased when it is combined with Spironolactone.
St. John's WortThe metabolism of Sitagliptin can be increased when combined with St. John's Wort.
StanozololStanozolol may increase the hypoglycemic activities of Sitagliptin.
StaurosporineThe serum concentration of Sitagliptin can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Sitagliptin can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Sitagliptin can be decreased when it is combined with Streptozocin.
SulfadiazineSitagliptin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleSitagliptin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfamethoxazoleThe metabolism of Sitagliptin can be decreased when combined with Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Sitagliptin can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleSitagliptin may increase the hypoglycemic activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Sitagliptin can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Sitagliptin can be increased when it is combined with Sumatriptan.
SunitinibSitagliptin may increase the hypoglycemic activities of Sunitinib.
SunitinibThe serum concentration of Sitagliptin can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Sitagliptin can be increased when it is combined with Tacrine.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Sitagliptin.
TacrolimusThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Tacrolimus.
TamoxifenThe serum concentration of Sitagliptin can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Sitagliptin can be increased when it is combined with Taurocholic Acid.
TelaprevirThe metabolism of Sitagliptin can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Sitagliptin can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Sitagliptin can be increased when it is combined with Telmisartan.
TemocaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Temocapril.
TemsirolimusThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Temsirolimus.
TemsirolimusThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Temsirolimus.
TerazosinThe serum concentration of Sitagliptin can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Sitagliptin can be increased when it is combined with Terfenadine.
TeriflunomideThe metabolism of Sitagliptin can be decreased when combined with Teriflunomide.
TesmilifeneThe serum concentration of Sitagliptin can be decreased when it is combined with Tesmilifene.
TestosteroneTestosterone may increase the hypoglycemic activities of Sitagliptin.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Sitagliptin.
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Sitagliptin.
TicagrelorThe serum concentration of Sitagliptin can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Sitagliptin can be decreased when combined with Ticlopidine.
TipranavirThe serum concentration of Sitagliptin can be decreased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Sitagliptin can be decreased when it is combined with Tocilizumab.
TolazamideSitagliptin may increase the hypoglycemic activities of Tolazamide.
TolbutamideSitagliptin may increase the hypoglycemic activities of Tolbutamide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Sitagliptin.
TolvaptanThe serum concentration of Sitagliptin can be increased when it is combined with Tolvaptan.
TorasemideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Trandolapril.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Sitagliptin.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Sitagliptin.
TrazodoneTrazodone may increase the hypoglycemic activities of Sitagliptin.
TriamcinoloneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Triamcinolone.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Sitagliptin.
TrichlormethiazideThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Trichlormethiazide.
TrifluoperazineThe serum concentration of Sitagliptin can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Sitagliptin can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Sitagliptin can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Sitagliptin.
TriptorelinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Triptorelin.
TroleandomycinThe serum concentration of Sitagliptin can be increased when it is combined with Troleandomycin.
VenlafaxineThe metabolism of Sitagliptin can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Sitagliptin can be decreased when combined with Verapamil.
VilazodoneVilazodone may increase the hypoglycemic activities of Sitagliptin.
VinblastineThe serum concentration of Sitagliptin can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Sitagliptin can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Sitagliptin can be increased when it is combined with Vinorelbine.
VoriconazoleThe metabolism of Sitagliptin can be decreased when combined with Voriconazole.
VorinostatThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Vorinostat.
VortioxetineVortioxetine may increase the hypoglycemic activities of Sitagliptin.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Sitagliptin.
ZimelidineZimelidine may increase the hypoglycemic activities of Sitagliptin.
ZiprasidoneThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Ziprasidone.
Food Interactions
  • Can be administered without regard to food

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
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
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
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
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 ]
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Drug created on May 16, 2007 11:36 / Updated on September 30, 2016 02:27