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Identification
NameSaxagliptin
Accession NumberDB06335
TypeSmall Molecule
GroupsApproved
DescriptionSaxagliptin (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. FDA approved on July 31, 2009.
Structure
Thumb
Synonyms
(1S,3S,5S)-2-((2S)-Amino(3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)acetyl)-2-azabicyclo(3.1.0)hexane-3-carbonitrile
BMS 477118
BMS-477118
Onglyza
External Identifiers
  • BMS-477118
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Onglyzatablet5 mgoralAstrazeneca Canada Inc2009-10-29Not applicableCanada
OnglyzaFilm-coated tablet2.5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated2.5 mg/1oralE.R. Squibb & Sons, L.L.C.2009-07-31Not applicableUs
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated5 mg/1oralPhysicians Total Care, Inc.2011-09-22Not applicableUs
OnglyzaFilm-coated tablet2.5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet2.5 mgoralAstrazeneca Canada Inc2011-12-23Not applicableCanada
OnglyzaFilm-coated tablet2.5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated5 mg/1oralE.R. Squibb & Sons, L.L.C.2009-07-31Not applicableUs
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated5 mg/1oralCardinal Health2009-07-31Not applicableUs
OnglyzaFilm-coated tablet2.5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated2.5 mg/1oralAstra Zeneca Pharmaceuticals Lp2014-11-20Not applicableUs
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated5 mg/1oralCardinal Health2014-11-20Not applicableUs
OnglyzaFilm-coated tablet2.5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Onglyzatablet, film coated5 mg/1oralAstra Zeneca Pharmaceuticals Lp2014-11-20Not applicableUs
OnglyzaFilm-coated tablet5 mgOral useAstra Zeneca Ab2009-10-01Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Kombiglyze XRE.R. Squibb & Sons, L.L.C.
KomboglyzeAstrazeneca Canada Inc
Salts
Name/CASStructureProperties
Saxagliptin Hydrochloride
Thumb
  • InChI Key: TUAZNHHHYVBVBR-NHKADLRUSA-N
  • Monoisotopic Mass: 351.171354798
  • Average Mass: 351.871
DBSALT000158
Categories
UNII8I7IO46IVQ
CAS number361442-04-8
WeightAverage: 315.41
Monoisotopic: 315.194677059
Chemical FormulaC18H25N3O2
InChI KeyInChIKey=QGJUIPDUBHWZPV-SGTAVMJGSA-N
InChI
InChI=1S/C18H25N3O2/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17/h10-15,23H,1-7,9,20H2/t10?,11?,12-,13+,14+,15-,17?,18?/m1/s1
IUPAC Name
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
SMILES
N[[email protected]](C(=O)N1[[email protected]]2C[[email protected]]2C[[email protected]]1C#N)C12CC3CC(CC(O)(C3)C1)C2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentAlpha amino acid amides
Alternative Parents
Substituents
  • Alpha-amino acid amide
  • N-acyl-piperidine
  • N-acylpyrrolidine
  • Piperidine
  • Tertiary carboxylic acid amide
  • Tertiary alcohol
  • Pyrrolidine
  • Cyclic alcohol
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Nitrile
  • Carbonitrile
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of type 2 diabetes mellitus to improve glycemic control in combination with other agents or as monotherapy.
PharmacodynamicsPost-administration of saxagliptin, GLP-1 and GIP levels rise up to 2- to 3- fold. Because it is very selective of DPP-4 inhibition, there are fewer systemic side effects. Saxagliptin inhibits DPP-4 enzyme activity for a 24-hour period. It also decreased glucagon concentrations and increased glucose-dependent insulin secretion from pancreatic beta cells. The half maximal inhibitory concentration (IC50) is 0.5 nmol/L. Saxagliptin did not prolong the QTc interval to a clinically significant degree.
Mechanism of actionSaxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor antidiabetic for the treatment of type 2 diabetes. DPP-4 inhibitors are a class of compounds that work by affecting the action of natural hormones in the body called incretins. Incretins decrease blood sugar by increasing consumption of sugar by the body, mainly through increasing insulin production in the pancreas, and by reducing production of sugar by the liver. [Bristol-Myers Squibb Press Release] DPP-4 is a membrane associated peptidase which is found in many tissues, lymphocytes and plasma. DPP-4 has two main mechanisms of action, an enzymatic function and another mechanism where DPP-4 binds adenosine deaminase, which conveys intracellular signals via dimerization when activated. Saxagliptin forms a reversible, histidine-assisted covalent bond between its nitrile group and the S630 hydroxyl oxygen on DPP-4. The inhibition of DPP-4 increases levels active of glucagon like peptide 1 (GLP-1), which inhibits glucagon production from pancreatic alpha cells and increases production of insulin from pancreatic beta cells.
Related Articles
AbsorptionFollowing a 5 mg single oral dose of saxagliptin to healthy subjects, the mean plasma AUC values for saxagliptin and its active metabolite were 78 ng•h/mL and 214 ng•h/mL, respectively. The corresponding plasma Cmax values were 24 ng/mL and 47 ng/mL, respectively. Saxagliptin did not accumulate following repeated doses. The median time to maximum concentration (Tmax) following the 5 mg once daily dose was 2 hours for saxagliptin and 4 hours for its active metabolite. Bioavailability, 2.5 - 50 mg dose = 67%
Volume of distribution

151 L

Protein bindingThe in vitro protein binding of saxagliptin and its active metabolite in human serum is negligible (<10%).
Metabolism

The metabolism of saxagliptin is primarily mediated by cytochrome P450 3A4/5 (CYP3A4/5). 50% of the absorbed dose will undergo hepatic metabolism. The major metabolite of saxagliptin, 5-hydroxy saxagliptin, is also a DPP4 inhibitor, which is one-half as potent as saxagliptin.

SubstrateEnzymesProduct
Saxagliptin
5-hydroxy saxagliptinDetails
Route of eliminationSaxagliptin is eliminated by both renal and hepatic pathways. Following a single 50 mg dose of 14C-saxagliptin, 24%, 36%, and 75% of the dose was excreted in the urine as saxagliptin, its active metabolite, and total radioactivity, respectively. A total of 22% of the administered radioactivity was recovered in feces representing the fraction of the saxagliptin dose excreted in bile and/or unabsorbed drug from the gastrointestinal tract.
Half lifeSaxagliptin = 2.5 hours; 5-hydroxy saxagliptin = 3.1 hours;
Clearance

Renal clearance, single 50 mg dose = 14 L/h

ToxicityAdverse reactions reported in ≥5% of patients treated with saxagliptin and more commonly than in patients treated with placebo are: upper respiratory tract infection, urinary tract infection, and headache.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9894
Blood Brain Barrier+0.8823
Caco-2 permeable-0.5446
P-glycoprotein substrateSubstrate0.5909
P-glycoprotein inhibitor INon-inhibitor0.696
P-glycoprotein inhibitor IINon-inhibitor0.7875
Renal organic cation transporterNon-inhibitor0.7903
CYP450 2C9 substrateNon-substrate0.8618
CYP450 2D6 substrateNon-substrate0.7519
CYP450 3A4 substrateSubstrate0.5944
CYP450 1A2 substrateNon-inhibitor0.8448
CYP450 2C9 inhibitorNon-inhibitor0.8017
CYP450 2D6 inhibitorNon-inhibitor0.8198
CYP450 2C19 inhibitorNon-inhibitor0.81
CYP450 3A4 inhibitorNon-inhibitor0.8641
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9032
Ames testNon AMES toxic0.7569
CarcinogenicityNon-carcinogens0.9122
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7529 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9912
hERG inhibition (predictor II)Non-inhibitor0.832
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseoral
Tabletoral
Film-coated tabletOral use2.5 mg
Film-coated tabletOral use5 mg
Tabletoral2.5 mg
Tabletoral5 mg
Tablet, film coatedoral2.5 mg/1
Tablet, film coatedoral5 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6395767 No2001-02-162021-02-16Us
US7951400 No2008-11-302028-11-30Us
US8628799 No2005-07-132025-07-13Us
USRE44186 No2003-07-312023-07-31Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySparingly solubleFDA label
Predicted Properties
PropertyValueSource
Water Solubility2.26 mg/mLALOGPS
logP0.88ALOGPS
logP-0.08ChemAxon
logS-2.1ALOGPS
pKa (Strongest Acidic)14.74ChemAxon
pKa (Strongest Basic)7.9ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area90.35 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity83.99 m3·mol-1ChemAxon
Polarizability34.22 Å3ChemAxon
Number of Rings5ChemAxon
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

Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage, “CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME.” U.S. Patent US20090054303, issued February 26, 2009.

US20090054303
General References
  1. Rosenstock J, Sankoh S, List JF: Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes. Diabetes Obes Metab. 2008 May;10(5):376-86. doi: 10.1111/j.1463-1326.2008.00876.x. Epub 2008 Mar 18. [PubMed:18355324 ]
  2. Metzler WJ, Yanchunas J, Weigelt C, Kish K, Klei HE, Xie D, Zhang Y, Corbett M, Tamura JK, He B, Hamann LG, Kirby MS, Marcinkeviciene J: Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci. 2008 Feb;17(2):240-50. doi: 10.1110/ps.073253208. [PubMed:18227430 ]
  3. Crepaldi G, Carruba M, Comaschi M, Del Prato S, Frajese G, Paolisso G: Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management. J Endocrinol Invest. 2007 Jul-Aug;30(7):610-4. [PubMed:17848846 ]
  4. Barnett A: DPP-4 inhibitors and their potential role in the management of type 2 diabetes. Int J Clin Pract. 2006 Nov;60(11):1454-70. [PubMed:17073841 ]
  5. Kulasa K, Edelman S: Saxagliptin: the evidence for its place in the treatment of type 2 diabetes mellitus. Core Evid. 2010 Oct 21;5:23-37. [PubMed:21042540 ]
  6. Russell S: Incretin-based therapies for type 2 diabetes mellitus: a review of direct comparisons of efficacy, safety and patient satisfaction. Int J Clin Pharm. 2013 Apr;35(2):159-72. doi: 10.1007/s11096-012-9729-9. Epub 2012 Dec 22. [PubMed:23263796 ]
  7. Ali S, Fonseca V: Saxagliptin overview: special focus on safety and adverse effects. Expert Opin Drug Saf. 2013 Jan;12(1):103-9. doi: 10.1517/14740338.2013.741584. Epub 2012 Nov 9. [PubMed:23137182 ]
  8. Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547 ]
External Links
ATC CodesA10BD10A10BH03A10BD21
AHFS Codes
  • 68:20.05
PDB EntriesNot Available
FDA labelDownload (492 KB)
MSDSDownload (479 KB)
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 Saxagliptin.
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Saxagliptin.
AcetaminophenThe serum concentration of Saxagliptin can be decreased when it is combined with Acetaminophen.
AcetohexamideSaxagliptin may increase the hypoglycemic activities of Acetohexamide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Saxagliptin.
AlclometasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Alclometasone.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Saxagliptin.
AlimemazineThe serum concentration of Saxagliptin can be decreased when it is combined with Alimemazine.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Saxagliptin.
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Saxagliptin.
AminoglutethimideThe serum concentration of Saxagliptin can be decreased when it is combined with Aminoglutethimide.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Saxagliptin.
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Saxagliptin.
AmiodaroneThe serum concentration of Saxagliptin can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Saxagliptin.
AmoxapineAmoxapine may increase the hypoglycemic activities of Saxagliptin.
AprepitantThe serum concentration of Saxagliptin can be increased when it is combined with Aprepitant.
AripiprazoleThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Aripiprazole.
ArmodafinilThe serum concentration of Saxagliptin can be decreased when it is combined with Armodafinil.
Arsenic trioxideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Arsenic trioxide.
ArtemetherThe serum concentration of Saxagliptin can be decreased when it is combined with Artemether.
ArticaineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Atazanavir.
AtomoxetineThe serum concentration of Saxagliptin can be increased when it is combined with Atomoxetine.
AtorvastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Atorvastatin.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Saxagliptin.
AvasimibeThe serum concentration of Saxagliptin can be decreased when it is combined with Avasimibe.
AzatadineThe serum concentration of Saxagliptin can be decreased when it is combined with Azatadine.
BenazeprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Benazepril.
BendroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Bendroflumethiazide.
BenmoxinBenmoxin may increase the hypoglycemic activities of Saxagliptin.
BetamethasoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Betamethasone.
BexaroteneThe serum concentration of Saxagliptin can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Saxagliptin can be decreased when it is combined with Boceprevir.
BortezomibThe serum concentration of Saxagliptin can be increased when it is combined with Bortezomib.
BosentanThe serum concentration of Saxagliptin can be decreased when it is combined with Bosentan.
BrexpiprazoleThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Brexpiprazole.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Saxagliptin.
BumetanideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Bumetanide.
BuserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Buserelin.
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Saxagliptin.
CalcitriolThe serum concentration of Saxagliptin can be decreased when it is combined with Calcitriol.
CandoxatrilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Candoxatril.
CaptoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Captopril.
CarbamazepineThe serum concentration of Saxagliptin can be decreased when it is combined with Carbamazepine.
CaroxazoneCaroxazone may increase the hypoglycemic activities of Saxagliptin.
CefradineThe serum concentration of Saxagliptin can be decreased when it is combined with Cefradine.
CeritinibThe serum concentration of Saxagliptin can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Cerivastatin.
ChlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorothiazide.
ChlorphenesinThe serum concentration of Saxagliptin can be decreased when it is combined with Chlorphenesin.
ChlorpropamideSaxagliptin may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorthalidone.
CilazaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Cilazapril.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Saxagliptin.
CitalopramCitalopram may increase the hypoglycemic activities of Saxagliptin.
ClarithromycinThe serum concentration of Saxagliptin can be decreased when it is combined with Clarithromycin.
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Saxagliptin.
ClemastineThe serum concentration of Saxagliptin can be increased when it is combined with Clemastine.
ClevidipineThe serum concentration of Saxagliptin can be decreased when it is combined with Clevidipine.
ClofibrateThe serum concentration of Saxagliptin can be decreased when it is combined with Clofibrate.
ClomipramineClomipramine may increase the hypoglycemic activities of Saxagliptin.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Saxagliptin.
ClotrimazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Clotrimazole.
ClozapineThe serum concentration of Saxagliptin can be decreased when it is combined with Clozapine.
CobicistatThe serum concentration of Saxagliptin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Saxagliptin can be decreased when it is combined with Colchicine.
ConivaptanThe serum concentration of Saxagliptin can be increased when it is combined with Conivaptan.
CorticotropinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Cortisone acetate.
CrizotinibThe serum concentration of Saxagliptin can be increased when it is combined with Crizotinib.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Saxagliptin.
CyclophosphamideThe serum concentration of Saxagliptin can be decreased when it is combined with Cyclophosphamide.
CyclophosphamideThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Saxagliptin can be increased when it is combined with Cyclosporine.
Cyproterone acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe serum concentration of Saxagliptin can be decreased when it is combined with Dabrafenib.
DanazolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Danazol.
DapoxetineDapoxetine may increase the hypoglycemic activities of Saxagliptin.
DarunavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Darunavir.
DasatinibThe serum concentration of Saxagliptin can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Saxagliptin can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Saxagliptin can be increased when it is combined with Delavirdine.
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Saxagliptin.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Saxagliptin.
DesogestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Desogestrel.
DexamethasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Dexamethasone.
DiazoxideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Diazoxide.
DicloxacillinThe serum concentration of Saxagliptin can be decreased when it is combined with Dicloxacillin.
DienogestThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the hypoglycemic activities of Saxagliptin.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Saxagliptin.
DihydroergotamineThe serum concentration of Saxagliptin can be increased when it is combined with Dihydroergotamine.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Saxagliptin.
DiltiazemThe serum concentration of Saxagliptin can be increased when it is combined with Diltiazem.
DisopyramideSaxagliptin may increase the hypoglycemic activities of Disopyramide.
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Saxagliptin.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Saxagliptin.
DoxycyclineThe serum concentration of Saxagliptin can be increased when it is combined with Doxycycline.
DronedaroneThe serum concentration of Saxagliptin can be increased when it is combined with Dronedarone.
DrospirenoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Drospirenone.
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Saxagliptin.
EfavirenzThe serum concentration of Saxagliptin can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Saxagliptin can be decreased when it is combined with Eletriptan.
EnalaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Enalaprilat.
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Saxagliptin.
EnzalutamideThe serum concentration of Saxagliptin can be decreased when it is combined with Enzalutamide.
EpinephrineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Epinephrine.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Saxagliptin.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Saxagliptin.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Saxagliptin.
ErythromycinThe serum concentration of Saxagliptin can be increased when it is combined with Erythromycin.
EscitalopramEscitalopram may increase the hypoglycemic activities of Saxagliptin.
Eslicarbazepine acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Eslicarbazepine acetate.
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Saxagliptin.
EstradiolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Etacrynic acid.
EthanolThe serum concentration of Saxagliptin can be decreased when it is combined with Ethanol.
Ethinyl EstradiolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Etonogestrel.
EtoperidoneEtoperidone may increase the hypoglycemic activities of Saxagliptin.
EtoposideThe serum concentration of Saxagliptin can be decreased when it is combined with Etoposide.
EtravirineThe serum concentration of Saxagliptin can be decreased when it is combined with Etravirine.
EverolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Everolimus.
FelbamateThe serum concentration of Saxagliptin can be decreased when it is combined with Felbamate.
FenfluramineFenfluramine may increase the hypoglycemic activities of Saxagliptin.
FlucloxacillinThe serum concentration of Saxagliptin can be decreased when it is combined with Flucloxacillin.
FluconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Fludrocortisone.
FluorometholoneThe serum concentration of Saxagliptin can be decreased when it is combined with Fluorometholone.
FluoxetineFluoxetine may increase the hypoglycemic activities of Saxagliptin.
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Saxagliptin.
FluvastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Fluvastatin.
FluvoxamineThe serum concentration of Saxagliptin can be increased when it is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Saxagliptin can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Saxagliptin can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Fosinopril.
FosphenytoinThe serum concentration of Saxagliptin can be decreased when it is combined with Fosphenytoin.
FurazolidoneFurazolidone may increase the hypoglycemic activities of Saxagliptin.
FurosemideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Furosemide.
Fusidic AcidThe serum concentration of Saxagliptin can be increased when it is combined with Fusidic Acid.
GarlicThe serum concentration of Saxagliptin can be decreased when it is combined with Garlic.
GemfibrozilThe serum concentration of Saxagliptin can be decreased when it is combined with Gemfibrozil.
GlibornurideSaxagliptin may increase the hypoglycemic activities of Glibornuride.
GliclazideSaxagliptin may increase the hypoglycemic activities of Gliclazide.
GlimepirideSaxagliptin may increase the hypoglycemic activities of Glimepiride.
GlipizideSaxagliptin may increase the hypoglycemic activities of Glipizide.
GliquidoneSaxagliptin may increase the hypoglycemic activities of Gliquidone.
GlisoxepideSaxagliptin may increase the hypoglycemic activities of Glisoxepide.
GlyburideSaxagliptin may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Goserelin.
GriseofulvinThe serum concentration of Saxagliptin can be decreased when it is combined with Griseofulvin.
GuanethidineThe serum concentration of Saxagliptin can be decreased when it is combined with Guanethidine.
HistrelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Histrelin.
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Saxagliptin.
HydrochlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydrochlorothiazide.
HydrocortamateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortamate.
HydrocortisoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.
IdelalisibThe serum concentration of Saxagliptin can be increased when it is combined with Idelalisib.
IfosfamideThe serum concentration of Saxagliptin can be decreased when it is combined with Ifosfamide.
IloperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Iloperidone.
ImatinibThe serum concentration of Saxagliptin can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Saxagliptin.
IndalpineIndalpine may increase the hypoglycemic activities of Saxagliptin.
IndapamideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Indinavir.
Insulin AspartSaxagliptin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirSaxagliptin may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineSaxagliptin may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineSaxagliptin may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanSaxagliptin may increase the hypoglycemic activities of Insulin Human.
Insulin LisproSaxagliptin may increase the hypoglycemic activities of Insulin Lispro.
Insulin PorkSaxagliptin may increase the hypoglycemic activities of Insulin Pork.
IproclozideIproclozide may increase the hypoglycemic activities of Saxagliptin.
IproniazidIproniazid may increase the hypoglycemic activities of Saxagliptin.
IsavuconazoniumThe serum concentration of Saxagliptin can be increased when it is combined with Isavuconazonium.
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Saxagliptin.
IsradipineThe serum concentration of Saxagliptin can be increased when it is combined with Isradipine.
ItraconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Saxagliptin can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Ketoconazole.
LanreotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lanreotide.
LanreotideSaxagliptin may increase the hypoglycemic activities of Lanreotide.
LansoprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Lansoprazole.
LeuprolideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Saxagliptin.
LevonorgestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Levonorgestrel.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Saxagliptin.
LisinoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Lisinopril.
LopinavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lopinavir.
LoratadineThe serum concentration of Saxagliptin can be decreased when it is combined with Loratadine.
LovastatinThe serum concentration of Saxagliptin can be increased when it is combined with Lovastatin.
Lu AA21004Lu AA21004 may increase the hypoglycemic activities of Saxagliptin.
LuliconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Luliconazole.
LurasidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lurasidone.
MebanazineMebanazine may increase the hypoglycemic activities of Saxagliptin.
MecaserminSaxagliptin may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Medroxyprogesterone acetate.
Megestrol acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Megestrol acetate.
MesalazineMesalazine may increase the hypoglycemic activities of Saxagliptin.
MestranolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Mestranol.
MetamizoleThe serum concentration of Saxagliptin can be decreased when it is combined with Metamizole.
MethadoneThe serum concentration of Saxagliptin can be decreased when it is combined with Methadone.
MethotrimeprazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methyclothiazide.
Methylene blueMethylene blue may increase the hypoglycemic activities of Saxagliptin.
MethylprednisoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methylprednisolone.
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Saxagliptin.
MetolazoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Metolazone.
MetyraponeThe serum concentration of Saxagliptin can be decreased when it is combined with Metyrapone.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Saxagliptin.
MifepristoneThe serum concentration of Saxagliptin can be decreased when it is combined with Mifepristone.
MifepristoneSaxagliptin may increase the hypoglycemic activities of Mifepristone.
MilnacipranMilnacipran may increase the hypoglycemic activities of Saxagliptin.
MinaprineMinaprine may increase the hypoglycemic activities of Saxagliptin.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Saxagliptin.
MitotaneThe serum concentration of Saxagliptin can be decreased when it is combined with Mitotane.
MoclobemideMoclobemide may increase the hypoglycemic activities of Saxagliptin.
ModafinilThe serum concentration of Saxagliptin can be decreased when it is combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Moexipril.
NafcillinThe serum concentration of Saxagliptin can be decreased when it is combined with Nafcillin.
NateglinideSaxagliptin may increase the hypoglycemic activities of Nateglinide.
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Saxagliptin.
NelfinavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Nelfinavir.
NetupitantThe serum concentration of Saxagliptin can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Saxagliptin can be decreased when it is combined with Nevirapine.
NiacinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Niacin.
NialamideNialamide may increase the hypoglycemic activities of Saxagliptin.
NicardipineThe serum concentration of Saxagliptin can be decreased when it is combined with Nicardipine.
NifedipineThe serum concentration of Saxagliptin can be decreased when it is combined with Nifedipine.
NilotinibThe serum concentration of Saxagliptin can be increased when it is combined with Nilotinib.
NorethisteroneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Norgestimate.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Saxagliptin.
OctamoxinOctamoxin may increase the hypoglycemic activities of Saxagliptin.
OctreotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Octreotide.
OctreotideSaxagliptin may increase the hypoglycemic activities of Octreotide.
OlanzapineOlanzapine may increase the hypoglycemic activities of Saxagliptin.
OlaparibThe serum concentration of Saxagliptin can be increased when it is combined with Olaparib.
OmapatrilatThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Omapatrilat.
OmeprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Omeprazole.
OrlistatThe serum concentration of Saxagliptin can be decreased when it is combined with Orlistat.
OsimertinibThe serum concentration of Saxagliptin can be decreased when it is combined with Osimertinib.
OxandroloneOxandrolone may increase the hypoglycemic activities of Saxagliptin.
OxcarbazepineThe serum concentration of Saxagliptin can be decreased when it is combined with Oxcarbazepine.
OxiconazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Oxiconazole.
OxymetholoneOxymetholone may increase the hypoglycemic activities of Saxagliptin.
PaclitaxelThe serum concentration of Saxagliptin can be decreased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Saxagliptin can be increased when it is combined with Palbociclib.
PaliperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Paliperidone.
PantoprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Pantoprazole.
PargylinePargyline may increase the hypoglycemic activities of Saxagliptin.
ParoxetineParoxetine may increase the hypoglycemic activities of Saxagliptin.
PasireotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.
PasireotideSaxagliptin may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Saxagliptin.
PentamidineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pentamidine.
PentamidineSaxagliptin may increase the hypoglycemic activities of Pentamidine.
PentobarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Pentobarbital.
PerampanelThe serum concentration of Saxagliptin can be decreased when it is combined with Perampanel.
PerindoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Perindopril.
PethidineThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Pethidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Saxagliptin.
PheniprazinePheniprazine may increase the hypoglycemic activities of Saxagliptin.
PhenobarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Phenobarbital.
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Saxagliptin.
PhenylbutazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Phenylbutazone.
PhenytoinThe serum concentration of Saxagliptin can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Saxagliptin.
PioglitazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Pioglitazone.
PiperazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pipotiazine.
PirlindolePirlindole may increase the hypoglycemic activities of Saxagliptin.
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Saxagliptin.
PolythiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Polythiazide.
PosaconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Posaconazole.
PrednisoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Prednisolone.
PrednisoneThe serum concentration of Saxagliptin can be decreased when it is combined with Prednisone.
PrimidoneThe serum concentration of Saxagliptin can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Saxagliptin can be decreased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Progesterone.
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Saxagliptin.
PyridostigmineThe serum concentration of Saxagliptin can be decreased when it is combined with Pyridostigmine.
QuetiapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quetiapine.
QuinaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Quinapril.
QuinethazoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quinethazone.
QuinidineThe serum concentration of Saxagliptin can be decreased when it is combined with Quinidine.
QuinineThe serum concentration of Saxagliptin can be decreased when it is combined with Quinine.
QuinineSaxagliptin may increase the hypoglycemic activities of Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Ramipril.
RanolazineThe serum concentration of Saxagliptin can be increased when it is combined with Ranolazine.
RasagilineRasagiline may increase the hypoglycemic activities of Saxagliptin.
RepaglinideSaxagliptin may increase the hypoglycemic activities of Repaglinide.
RescinnamineThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Rescinnamine.
RifabutinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Saxagliptin can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifaximin.
RilpivirineThe serum concentration of Saxagliptin can be decreased when it is combined with Rilpivirine.
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Saxagliptin.
RisperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Ritonavir.
RofecoxibThe serum concentration of Saxagliptin can be decreased when it is combined with Rofecoxib.
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Saxagliptin.
RufinamideThe serum concentration of Saxagliptin can be decreased when it is combined with Rufinamide.
SafrazineSafrazine may increase the hypoglycemic activities of Saxagliptin.
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Saxagliptin.
SaquinavirThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Saquinavir.
SelegilineSelegiline may increase the hypoglycemic activities of Saxagliptin.
SeratrodastThe serum concentration of Saxagliptin can be decreased when it is combined with Seratrodast.
SertralineSertraline may increase the hypoglycemic activities of Saxagliptin.
SildenafilThe serum concentration of Saxagliptin can be increased when it is combined with Sildenafil.
SiltuximabThe serum concentration of Saxagliptin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Saxagliptin can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Simvastatin.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Saxagliptin.
SirolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Sirolimus.
SpiraprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Spirapril.
St. John's WortThe metabolism of Saxagliptin can be increased when combined with St. John&#39;s Wort.
StanozololStanozolol may increase the hypoglycemic activities of Saxagliptin.
StiripentolThe serum concentration of Saxagliptin can be increased when it is combined with Stiripentol.
SulfadiazineSaxagliptin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleSaxagliptin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe serum concentration of Saxagliptin can be increased when it is combined with Sulfisoxazole.
SulfisoxazoleSaxagliptin may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibSaxagliptin may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Saxagliptin.
TacrolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.
TamoxifenThe serum concentration of Saxagliptin can be decreased when it is combined with Tamoxifen.
TelaprevirThe serum concentration of Saxagliptin can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Saxagliptin can be increased when it is combined with Telithromycin.
TemocaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Temocapril.
TemozolomideThe serum concentration of Saxagliptin can be decreased when it is combined with Temozolomide.
TemsirolimusThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Temsirolimus.
TemsirolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Temsirolimus.
TerbinafineThe serum concentration of Saxagliptin can be decreased when it is combined with Terbinafine.
TerfenadineThe serum concentration of Saxagliptin can be decreased when it is combined with Terfenadine.
TesmilifeneThe serum concentration of Saxagliptin can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Testosterone.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Saxagliptin.
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Saxagliptin.
TiclopidineThe serum concentration of Saxagliptin can be increased when it is combined with Ticlopidine.
TipranavirThe serum concentration of Saxagliptin can be decreased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Saxagliptin can be decreased when it is combined with Tocilizumab.
TolazamideSaxagliptin may increase the hypoglycemic activities of Tolazamide.
TolbutamideSaxagliptin may increase the hypoglycemic activities of Tolbutamide.
ToloxatoneToloxatone may increase the hypoglycemic activities of Saxagliptin.
TopiramateThe serum concentration of Saxagliptin can be decreased when it is combined with Topiramate.
TopotecanThe serum concentration of Saxagliptin can be decreased when it is combined with Topotecan.
TorasemideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Torasemide.
TrametinibThe serum concentration of Saxagliptin can be decreased when it is combined with Trametinib.
TrandolaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Trandolapril.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Saxagliptin.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Saxagliptin.
TrazodoneTrazodone may increase the hypoglycemic activities of Saxagliptin.
TriamcinoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Triamcinolone.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Saxagliptin.
TrichlormethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Trichlormethiazide.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Saxagliptin.
TriptorelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Triptorelin.
TroglitazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Troglitazone.
VemurafenibThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.
VenlafaxineThe serum concentration of Saxagliptin can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Saxagliptin can be increased when it is combined with Verapamil.
VilazodoneVilazodone may increase the hypoglycemic activities of Saxagliptin.
VoriconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Voriconazole.
VorinostatThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Vorinostat.
VortioxetineVortioxetine may increase the hypoglycemic activities of Saxagliptin.
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Saxagliptin.
ZimelidineZimelidine may increase the hypoglycemic activities of Saxagliptin.
ZiprasidoneThe serum concentration of Saxagliptin can be increased when it is combined with Ziprasidone.
Food Interactions
  • Administration with a high-fat meal resulted in an increase in Tmax of saxagliptin by approximately 20 minutes as compared to fasted conditions. There was a 27% increase in the AUC of saxagliptin when given with a meal as compared to fasted conditions.

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. Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG: Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem. 2005 Jul 28;48(15):5025-37. [PubMed:16033281 ]

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. Upreti VV, Boulton DW, Li L, Ching A, Su H, Lacreta FP, Patel CG: Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol. 2011 Jul;72(1):92-102. doi: 10.1111/j.1365-2125.2011.03937.x. [PubMed:21651615 ]
  2. Patel CG, Kornhauser D, Vachharajani N, Komoroski B, Brenner E, Handschuh del Corral M, Li L, Boulton DW: Saxagliptin, a potent, selective inhibitor of DPP-4, does not alter the pharmacokinetics of three oral antidiabetic drugs (metformin, glyburide or pioglitazone) in healthy subjects. Diabetes Obes Metab. 2011 Jul;13(7):604-14. doi: 10.1111/j.1463-1326.2011.01381.x. [PubMed:21332626 ]
  3. Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Upreti VV, Boulton DW, Li L, Ching A, Su H, Lacreta FP, Patel CG: Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol. 2011 Jul;72(1):92-102. doi: 10.1111/j.1365-2125.2011.03937.x. [PubMed:21651615 ]
  2. Patel CG, Kornhauser D, Vachharajani N, Komoroski B, Brenner E, Handschuh del Corral M, Li L, Boulton DW: Saxagliptin, a potent, selective inhibitor of DPP-4, does not alter the pharmacokinetics of three oral antidiabetic drugs (metformin, glyburide or pioglitazone) in healthy subjects. Diabetes Obes Metab. 2011 Jul;13(7):604-14. doi: 10.1111/j.1463-1326.2011.01381.x. [PubMed:21332626 ]
  3. Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Scheen AJ: Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions. Clin Pharmacokinet. 2010 Sep;49(9):573-88. doi: 10.2165/11532980-000000000-00000. [PubMed:20690781 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Organic anion transporter, capable of transporting pharmacological substances such as digoxin, ouabain, thyroxine, methotrexate and cAMP. May participate in the regulation of membrane transport of ouabain. Involved in the uptake of the dipeptidyl peptidase-4 inhibitor sitagliptin and hence may play a role in its transport into and out of renal proximal tubule cells. May be involved in the first...
Gene Name:
SLCO4C1
Uniprot ID:
Q6ZQN7
Molecular Weight:
78947.525 Da
References
  1. Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. Golightly LK, Drayna CC, McDermott MT: Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14. doi: 10.2165/11632930-000000000-00000. [PubMed:22686547 ]
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Drug created on March 19, 2008 10:24 / Updated on September 27, 2016 02:27