Identification

Name
Saxagliptin
Accession Number
DB06335
Type
Small Molecule
Groups
Approved
Description

Saxagliptin (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
  • Saxagliptin anhydrous
External IDs
BMS 477118 / BMS-477118
Product Ingredients
IngredientUNIICASInChI Key
Saxagliptin hydrochlorideZ8J84YIX6L709031-78-7TUAZNHHHYVBVBR-NHKADLRUSA-N
Saxagliptin monohydrate9GB927LAJW945667-22-1AFNTWHMDBNQQPX-NHKADLRUSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OnglyzaTablet, film coated2.5 mg/1OralE.R. Squibb & Sons, L.L.C.2009-07-312017-04-30Us00003 4214 21 nlmimage10 1a1b8d0c
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet5 mgOralAstra Zeneca2009-10-29Not applicableCanada
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mg/1OralAstra Zeneca Lp2014-11-20Not applicableUs
OnglyzaTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2011-09-22Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-04-30Us
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralAstra Zeneca Lp2014-12-04Not applicableUs
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-03-31Us
Kombiglyze XRSaxagliptin hydrochloride (5 mg/1) + Metformin Hydrochloride (500 mg/1)Tablet, film coated, extended releaseOralAstra Zeneca Lp2014-12-04Not applicableUs
Kombiglyze XRSaxagliptin hydrochloride (2.5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralE.R. Squibb & Sons, L.L.C.2010-11-052017-05-31Us00003 4222 16 nlmimage10 f215f93f
Kombiglyze XRSaxagliptin hydrochloride (2.5 mg/1) + Metformin Hydrochloride (1000 mg/1)Tablet, film coated, extended releaseOralAstra Zeneca Lp2014-12-04Not applicableUs00310 6125 60 nlmimage10 d049e84f
KomboglyzeSaxagliptin (2.5 mg) + Metformin (850 mg)Tablet, film coatedOralAstra Zeneca Ab2011-11-24Not applicableEu
KomboglyzeSaxagliptin (2.5 mg) + Metformin Hydrochloride (1000 mg)TabletOralAstra Zeneca2013-04-26Not applicableCanada
KomboglyzeSaxagliptin (2.5 mg) + Metformin (850 mg)Tablet, film coatedOralAstra Zeneca Ab2011-11-24Not applicableEu
KomboglyzeSaxagliptin (2.5 mg) + Metformin (1000 mg)Tablet, film coatedOralAstra Zeneca Ab2011-11-24Not applicableEu
Categories
UNII
8I7IO46IVQ
CAS number
361442-04-8
Weight
Average: 315.41
Monoisotopic: 315.194677059
Chemical Formula
C18H25N3O2
InChI Key
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[C@H](C(=O)N1[C@H]2C[C@H]2C[C@H]1C#N)C12CC3CC(CC(O)(C3)C1)C2

Pharmacology

Indication

Treatment of type 2 diabetes mellitus to improve glycemic control in combination with other agents or as monotherapy.

Associated Conditions
Pharmacodynamics

Post-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 action

Saxagliptin 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.

TargetActionsOrganism
ADipeptidyl peptidase 4
inhibitor
Human
Absorption

Following 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 binding

The 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.

Route of elimination

Saxagliptin 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 life

Saxagliptin = 2.5 hours; 5-hydroxy saxagliptin = 3.1 hours;

Clearance

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

Toxicity

Adverse 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 organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.Experimental
AcetohexamideSaxagliptin may increase the hypoglycemic activities of Acetohexamide.Approved, Investigational, Withdrawn
Acetyl sulfisoxazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Acetyl sulfisoxazole.Approved, Vet Approved
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
AlaproclateAlaproclate may increase the hypoglycemic activities of Saxagliptin.Experimental
AloxiprinAloxiprin may increase the hypoglycemic activities of Saxagliptin.Experimental
AmineptineAmineptine may decrease the hypoglycemic activities of Saxagliptin.Illicit, Withdrawn
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Saxagliptin.Approved
AmiodaroneThe serum concentration of Saxagliptin can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may decrease the hypoglycemic activities of Saxagliptin.Approved
AmitriptylinoxideAmitriptylinoxide may decrease the hypoglycemic activities of Saxagliptin.Approved, Investigational
AmoxapineAmoxapine may decrease the hypoglycemic activities of Saxagliptin.Approved
AmprenavirThe serum concentration of Saxagliptin can be increased when it is combined with Amprenavir.Approved, Investigational
ApalutamideThe serum concentration of Saxagliptin can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Saxagliptin can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Aripiprazole.Approved, Investigational
ArmodafinilThe serum concentration of Saxagliptin can be decreased when it is combined with Armodafinil.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Asenapine.Approved
AsunaprevirThe serum concentration of Saxagliptin can be decreased when it is combined with Asunaprevir.Approved, Investigational, Withdrawn
AtazanavirThe serum concentration of Saxagliptin can be increased when it is combined with Atazanavir.Approved, Investigational
AvasimibeThe serum concentration of Saxagliptin can be decreased when it is combined with Avasimibe.Investigational
AzosemideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Azosemide.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
BarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Barbital.Illicit
Beclomethasone dipropionateThe serum concentration of Saxagliptin can be decreased when it is combined with Beclomethasone dipropionate.Approved, Investigational
BenazeprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Benazepril.Approved, Investigational
BenazeprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Benazeprilat.Experimental
BendroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Saxagliptin.Withdrawn
BenzthiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Benzthiazide.Approved
BesifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Besifloxacin.Approved
BetamethasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Betamethasone.Approved, Vet Approved
BexaroteneThe serum concentration of Saxagliptin can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe serum concentration of Saxagliptin can be increased when it is combined with Boceprevir.Approved, Withdrawn
BosentanThe serum concentration of Saxagliptin can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Brexpiprazole.Approved, Investigational
BrigatinibThe serum concentration of Saxagliptin can be decreased when it is combined with Brigatinib.Approved, Investigational
BudesonideThe serum concentration of Saxagliptin can be decreased when it is combined with Budesonide.Approved
BumetanideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Buserelin.Approved, Investigational
ButriptylineButriptyline may decrease the hypoglycemic activities of Saxagliptin.Approved
CaptoprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Captopril.Approved
CarbamazepineThe serum concentration of Saxagliptin can be decreased when it is combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumCarbaspirin calcium may increase the hypoglycemic activities of Saxagliptin.Experimental, Investigational
CarbutamideSaxagliptin may increase the hypoglycemic activities of Carbutamide.Experimental
CaroxazoneCaroxazone may increase the hypoglycemic activities of Saxagliptin.Withdrawn
CelecoxibThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Saxagliptin can be increased when it is combined with Ceritinib.Approved
Chloramine-TThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Chloramine-T.Vet Approved
ChlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideSaxagliptin may increase the hypoglycemic activities of Chlorpropamide.Approved, Investigational
ChlorsulfaquinoxalineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Chlorsulfaquinoxaline.Investigational
ChlorthalidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorthalidone.Approved
CilazaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Cilazapril.Approved
CinoxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Cinoxacin.Approved, Investigational, Withdrawn
CiprofloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Ciprofloxacin.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Saxagliptin.Approved
ClarithromycinThe serum concentration of Saxagliptin can be increased when it is combined with Clarithromycin.Approved
ClobetasolThe serum concentration of Saxagliptin can be decreased when it is combined with Clobetasol.Approved, Investigational
Clobetasol propionateThe serum concentration of Saxagliptin can be decreased when it is combined with Clobetasol propionate.Approved
ClofenamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Clofenamide.Experimental
ClofibrateThe serum concentration of Saxagliptin can be decreased when it is combined with Clofibrate.Approved, Investigational
ClomipramineClomipramine may decrease the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved
ClopamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Clopamide.Experimental
ClorexoloneThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Clorexolone.Experimental
ClorsulonThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Clorsulon.Vet Approved
ClotrimazoleThe serum concentration of Saxagliptin can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Clozapine.Approved
CobicistatThe serum concentration of Saxagliptin can be increased when it is combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Saxagliptin.Approved, Investigational
CorticotropinThe serum concentration of Saxagliptin can be decreased when it is combined with Corticotropin.Approved, Investigational, Vet Approved
Cortisone acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Cortisone acetate.Approved, Investigational
CrizotinibThe serum concentration of Saxagliptin can be increased when it is combined with Crizotinib.Approved
CurcuminThe serum concentration of Saxagliptin can be increased when it is combined with Curcumin.Approved, Investigational
CyclobenzaprineCyclobenzaprine may decrease the hypoglycemic activities of Saxagliptin.Approved
CyclopenthiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Cyclopenthiazide.Experimental
CyclosporineThe serum concentration of Saxagliptin can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Cyclothiazide.Approved
Cyproterone acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Saxagliptin can be decreased when it is combined with Dabrafenib.Approved, Investigational
DanazolThe serum concentration of Saxagliptin can be increased when it is combined with Danazol.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Saxagliptin.Investigational
DarunavirThe serum concentration of Saxagliptin can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Saxagliptin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Saxagliptin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Delapril.Investigational
DelavirdineThe serum concentration of Saxagliptin can be increased when it is combined with Delavirdine.Approved
DersalazineDersalazine may increase the hypoglycemic activities of Saxagliptin.Investigational
DesipramineDesipramine may decrease the hypoglycemic activities of Saxagliptin.Approved, Investigational
DesogestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Desogestrel.Approved
DesonideThe serum concentration of Saxagliptin can be decreased when it is combined with Desonide.Approved, Investigational
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
DexamethasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe serum concentration of Saxagliptin can be decreased when it is combined with Dexamethasone isonicotinate.Vet Approved
DiazoxideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Diazoxide.Approved
DibenzepinDibenzepin may decrease the hypoglycemic activities of Saxagliptin.Experimental
DiclofenamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Diclofenamide.Approved, Investigational
DienogestThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Dienogest.Approved
DifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Difloxacin.Vet Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
DiltiazemThe serum concentration of Saxagliptin can be increased when it is combined with Diltiazem.Approved, Investigational
DimetacrineDimetacrine may decrease the hypoglycemic activities of Saxagliptin.Approved, Withdrawn
DisopyramideSaxagliptin may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinDosulepin may decrease the hypoglycemic activities of Saxagliptin.Approved
DoxepinDoxepin may decrease the hypoglycemic activities of Saxagliptin.Approved, Investigational
DoxycyclineThe serum concentration of Saxagliptin can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Saxagliptin can be increased when it is combined with Dronedarone.Approved
DrospirenoneThe serum concentration of Saxagliptin can be decreased when it is combined with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Saxagliptin.Approved
EfavirenzThe serum concentration of Saxagliptin can be increased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Saxagliptin can be decreased when it is combined with Eletriptan.Approved, Investigational
EnalaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Enalaprilat.Approved
EnoxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Enoxacin.Approved, Investigational
EnzalutamideThe serum concentration of Saxagliptin can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EpitizideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Epitizide.Experimental
ErythromycinThe serum concentration of Saxagliptin can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
EstradiolThe serum concentration of Saxagliptin can be decreased when it is combined with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Etacrynic acid.Approved, Investigational
Ethinyl EstradiolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Ethinyl Estradiol.Approved
EthoxzolamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Ethoxzolamide.Withdrawn
Ethynodiol diacetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Etonogestrel.Approved, Investigational
EtravirineThe serum concentration of Saxagliptin can be decreased when it is combined with Etravirine.Approved
EverolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Everolimus.Approved
FenquizoneThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Fenquizone.Experimental
FleroxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Fleroxacin.Approved
FluconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Fluconazole.Approved, Investigational
FludrocortisoneThe serum concentration of Saxagliptin can be decreased when it is combined with Fludrocortisone.Approved, Investigational
FlumequineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Flumequine.Withdrawn
FlunisolideThe serum concentration of Saxagliptin can be decreased when it is combined with Flunisolide.Approved, Investigational
Fluocinolone AcetonideThe serum concentration of Saxagliptin can be decreased when it is combined with Fluocinolone Acetonide.Approved, Investigational, Vet Approved
FluoxetineFluoxetine may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Saxagliptin.Approved, Illicit
FluvoxamineThe serum concentration of Saxagliptin can be increased when it is combined with Fluvoxamine.Approved, Investigational
FormestaneThe serum concentration of Saxagliptin can be decreased when it is combined with Formestane.Approved, Investigational, Withdrawn
FosamprenavirThe serum concentration of Saxagliptin can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Saxagliptin can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Fosinopril.Approved
FosinoprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Fosinoprilat.Experimental
FosphenytoinThe serum concentration of Saxagliptin can be decreased when it is combined with Fosphenytoin.Approved, Investigational
FurazolidoneFurazolidone may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved
FurosemideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Furosemide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Saxagliptin can be increased when it is combined with Fusidic Acid.Approved, Investigational
GarenoxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Garenoxacin.Investigational
GatifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Gatifloxacin.Approved, Investigational
GemifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Gemifloxacin.Approved, Investigational
GenisteinThe serum concentration of Saxagliptin can be decreased when it is combined with Genistein.Investigational
GlibornurideSaxagliptin may increase the hypoglycemic activities of Glibornuride.Investigational, Withdrawn
GliclazideSaxagliptin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideSaxagliptin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideSaxagliptin may increase the hypoglycemic activities of Glipizide.Approved, Investigational
GliquidoneSaxagliptin may increase the hypoglycemic activities of Gliquidone.Approved, Investigational
GlisoxepideSaxagliptin may increase the hypoglycemic activities of Glisoxepide.Investigational
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Saxagliptin.Investigational
GlyburideSaxagliptin may increase the hypoglycemic activities of Glyburide.Approved
Glycerol PhenylbutyrateThe serum concentration of Saxagliptin can be decreased when it is combined with Glycerol Phenylbutyrate.Approved
GlycodiazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Glycodiazine.Approved, Investigational
GoserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Goserelin.Approved
GrepafloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Grepafloxacin.Approved, Investigational, Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Saxagliptin.Experimental
HarmalineHarmaline may increase the hypoglycemic activities of Saxagliptin.Experimental
HistrelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Saxagliptin.Experimental
HydrochlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone.Approved, Vet Approved
Hydrocortisone aceponateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone aceponate.Experimental, Vet Approved
Hydrocortisone acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone acetate.Approved, Vet Approved
Hydrocortisone butyrateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone butyrate.Approved, Vet Approved
Hydrocortisone probutateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone probutate.Approved, Vet Approved
Hydrocortisone succinateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone succinate.Approved
Hydrocortisone valerateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortisone valerate.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
HydroxyfasudilThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Hydroxyfasudil.Experimental
Hydroxyprogesterone caproateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved, Investigational
IdelalisibThe serum concentration of Saxagliptin can be increased when it is combined with Idelalisib.Approved
IloperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Iloperidone.Approved
ImatinibThe serum concentration of Saxagliptin can be increased when it is combined with Imatinib.Approved
ImidaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Imidapril.Investigational
ImipramineImipramine may decrease the hypoglycemic activities of Saxagliptin.Approved
Imipramine oxideImipramine oxide may decrease the hypoglycemic activities of Saxagliptin.Experimental
IndalpineIndalpine may increase the hypoglycemic activities of Saxagliptin.Investigational, Withdrawn
IndapamideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Indapamide.Approved
IndinavirThe serum concentration of Saxagliptin can be increased when it is combined with Indinavir.Approved
Insulin AspartSaxagliptin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DegludecSaxagliptin may increase the hypoglycemic activities of Insulin Degludec.Approved
Insulin DetemirSaxagliptin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineSaxagliptin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineSaxagliptin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanSaxagliptin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproSaxagliptin may increase the hypoglycemic activities of Insulin Lispro.Approved
Insulin peglisproSaxagliptin may increase the hypoglycemic activities of Insulin peglispro.Investigational
Insulin PorkSaxagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
IprindoleIprindole may decrease the hypoglycemic activities of Saxagliptin.Experimental
IproniazidIproniazid may increase the hypoglycemic activities of Saxagliptin.Withdrawn
IsavuconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of Saxagliptin can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Saxagliptin.Approved
IsoniazidThe serum concentration of Saxagliptin can be increased when it is combined with Isoniazid.Approved, Investigational
ItraconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Saxagliptin can be increased when it is combined with Ivacaftor.Approved
IvosidenibThe serum concentration of Saxagliptin can be decreased when it is combined with Ivosidenib.Approved, Investigational
KetoconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Ketoconazole.Approved, Investigational
LanreotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinezolidLinezolid may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Nutraceutical
LisinoprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Lisinopril.Approved, Investigational
LofepramineLofepramine may decrease the hypoglycemic activities of Saxagliptin.Experimental
LomefloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Lomefloxacin.Approved, Investigational
LopinavirThe serum concentration of Saxagliptin can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Saxagliptin can be decreased when it is combined with Loratadine.Approved, Investigational
LorpiprazoleThe serum concentration of Saxagliptin can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Saxagliptin can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Saxagliptin can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lurasidone.Approved, Investigational
MafenideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Mafenide.Approved, Vet Approved
MebanazineMebanazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
MebutizideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Mebutizide.Experimental
MecaserminSaxagliptin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MedrogestoneThe serum concentration of Saxagliptin can be decreased when it is combined with Medrogestone.Approved
Medroxyprogesterone acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Medroxyprogesterone acetate.Approved, Investigational
MefrusideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Mefruside.Experimental
Megestrol acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Megestrol acetate.Approved, Investigational, Vet Approved
MelitracenMelitracen may decrease the hypoglycemic activities of Saxagliptin.Experimental, Investigational
MesalazineMesalazine may increase the hypoglycemic activities of Saxagliptin.Approved
MesteroloneMesterolone may increase the hypoglycemic activities of Saxagliptin.Experimental
MestranolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Mestranol.Approved
MetahexamideSaxagliptin may increase the hypoglycemic activities of Metahexamide.Experimental
MethotrimeprazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methotrimeprazine.Approved, Investigational
MethyclothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methyclothiazide.Approved
Methyl salicylateMethyl salicylate may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
MethylprednisoloneThe serum concentration of Saxagliptin can be decreased when it is combined with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Saxagliptin.Approved
MeticraneThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Meticrane.Experimental
MetolazoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Metolazone.Approved
MetyraponeThe serum concentration of Saxagliptin can be decreased when it is combined with Metyrapone.Approved, Investigational
MibefradilThe serum concentration of Saxagliptin can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidostaurinThe serum concentration of Saxagliptin can be decreased when it is combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Saxagliptin can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
MinaprineMinaprine may increase the hypoglycemic activities of Saxagliptin.Approved
MitotaneThe serum concentration of Saxagliptin can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
ModafinilThe serum concentration of Saxagliptin can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Moexipril.Approved
MoxifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Moxifloxacin.Approved, Investigational
NafcillinThe serum concentration of Saxagliptin can be decreased when it is combined with Nafcillin.Approved, Investigational
Nalidixic AcidThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Nalidixic Acid.Approved, Investigational
NaloxoneThe serum concentration of Saxagliptin can be increased when it is combined with Naloxone.Approved, Vet Approved
NandroloneNandrolone may increase the hypoglycemic activities of Saxagliptin.Experimental, Investigational
Nandrolone decanoateNandrolone decanoate may increase the hypoglycemic activities of Saxagliptin.Approved, Illicit
NateglinideSaxagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NefazodoneThe serum concentration of Saxagliptin can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Saxagliptin can be increased when it is combined with Nelfinavir.Approved
NemonoxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Nemonoxacin.Investigational
NetupitantThe serum concentration of Saxagliptin can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe serum concentration of Saxagliptin can be decreased when it is combined with Nevirapine.Approved
NiacinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NialamideNialamide may increase the hypoglycemic activities of Saxagliptin.Withdrawn
NicardipineThe serum concentration of Saxagliptin can be increased when it is combined with Nicardipine.Approved, Investigational
NifedipineThe serum concentration of Saxagliptin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Saxagliptin can be increased when it is combined with Nilotinib.Approved, Investigational
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Saxagliptin.Investigational
NN344Saxagliptin may increase the hypoglycemic activities of NN344.Investigational
NorethisteroneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Norethisterone.Approved
NorfloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Norfloxacin.Approved
NorgestimateThe serum concentration of Saxagliptin can be decreased when it is combined with Norgestimate.Approved, Investigational
NortriptylineNortriptyline may decrease the hypoglycemic activities of Saxagliptin.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Saxagliptin.Withdrawn
OctreotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Octreotide.Approved, Investigational
OfloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Ofloxacin.Approved
OlanzapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Saxagliptin can be increased when it is combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Saxagliptin.Approved
OmapatrilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Omapatrilat.Investigational
OpipramolOpipramol may decrease the hypoglycemic activities of Saxagliptin.Investigational
OrbifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Orbifloxacin.Vet Approved
OsimertinibThe serum concentration of Saxagliptin can be increased when it is combined with Osimertinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
OxaprotilineOxaprotiline may decrease the hypoglycemic activities of Saxagliptin.Experimental
OxcarbazepineThe serum concentration of Saxagliptin can be decreased when it is combined with Oxcarbazepine.Approved
Oxolinic acidThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Oxolinic acid.Experimental
OxymetholoneOxymetholone may increase the hypoglycemic activities of Saxagliptin.Approved, Illicit
PaclitaxelThe serum concentration of Saxagliptin can be decreased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Saxagliptin can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Paliperidone.Approved
PantoprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Pantoprazole.Approved
PargylinePargyline may increase the hypoglycemic activities of Saxagliptin.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
PasireotideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pasireotide.Approved
PazufloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Pazufloxacin.Investigational
PefloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Pefloxacin.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Saxagliptin.Approved
PentamidineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pentamidine.Approved, Investigational
PentobarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Pentobarbital.Approved, Investigational, Vet Approved
PerindoprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Perindopril.Approved
PerindoprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Perindoprilat.Experimental
PhenelzinePhenelzine may increase the hypoglycemic activities of Saxagliptin.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
PhenobarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Phenobarbital.Approved, Investigational
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
Phenyl aminosalicylatePhenyl aminosalicylate may increase the hypoglycemic activities of Saxagliptin.Approved
PhenylbutazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Phenylbutazone.Approved, Vet Approved
PhenytoinThe serum concentration of Saxagliptin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PhthalylsulfathiazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Phthalylsulfathiazole.Experimental
PioglitazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Pioglitazone.Approved, Investigational
Pipemidic acidThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Pipemidic acid.Experimental
PiperazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pipotiazine.Approved, Investigational
PiretanideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Piretanide.Approved
PirlindolePirlindole may increase the hypoglycemic activities of Saxagliptin.Approved
Piromidic acidThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Piromidic acid.Experimental
PitolisantThe serum concentration of Saxagliptin can be decreased when it is combined with Pitolisant.Approved, Investigational
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
PolythiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Polythiazide.Approved
PosaconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrednicarbateThe serum concentration of Saxagliptin can be decreased when it is combined with Prednicarbate.Approved, Investigational
PrednisoloneThe serum concentration of Saxagliptin can be decreased when it is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Saxagliptin can be decreased when it is combined with Prednisone.Approved, Vet Approved
PregabalinThe risk or severity of heart failure can be increased when Pregabalin is combined with Saxagliptin.Approved, Illicit, Investigational
PrimidoneThe serum concentration of Saxagliptin can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Probenecid.Approved, Investigational
ProgesteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Progesterone.Approved, Vet Approved
ProtriptylineProtriptyline may decrease the hypoglycemic activities of Saxagliptin.Approved
PrulifloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Prulifloxacin.Investigational
QuetiapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quetiapine.Approved
QuinaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Quinapril.Approved, Investigational
QuinaprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Quinaprilat.Experimental
QuinethazoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quinethazone.Approved
QuinineThe serum concentration of Saxagliptin can be decreased when it is combined with Quinine.Approved
QuinupramineQuinupramine may decrease the hypoglycemic activities of Saxagliptin.Experimental
RamiprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Ramipril.Approved
RamiprilatThe risk or severity of angioedema can be increased when Saxagliptin is combined with Ramiprilat.Experimental
RasagilineRasagiline may increase the hypoglycemic activities of Saxagliptin.Approved
RepaglinideSaxagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of angioedema can be increased when Saxagliptin is combined with Rescinnamine.Approved
RifabutinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifabutin.Approved, Investigational
RifampicinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifampicin.Approved
RifamycinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifamycin.Investigational
RifapentineThe serum concentration of Saxagliptin can be decreased when it is combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifaximin.Approved, Investigational
RimexoloneThe serum concentration of Saxagliptin can be decreased when it is combined with Rimexolone.Approved
RisperidoneThe serum concentration of Saxagliptin can be increased when it is combined with Risperidone.Approved, Investigational
RitanserinRitanserin may increase the hypoglycemic activities of Saxagliptin.Investigational
RitonavirThe serum concentration of Saxagliptin can be increased when it is combined with Ritonavir.Approved, Investigational
RofecoxibThe serum concentration of Saxagliptin can be decreased when it is combined with Rofecoxib.Approved, Investigational, Withdrawn
RosoxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Rosoxacin.Approved, Investigational
RosuvastatinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Rosuvastatin.Approved
RufinamideThe serum concentration of Saxagliptin can be decreased when it is combined with Rufinamide.Approved
RufloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Rufloxacin.Experimental
SafinamideSafinamide may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
SafrazineSafrazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved
SaquinavirThe serum concentration of Saxagliptin can be increased when it is combined with Saquinavir.Approved, Investigational
SarafloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sarafloxacin.Vet Approved, Withdrawn
SarilumabThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Sarilumab.Approved, Investigational
SelegilineSelegiline may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Saxagliptin.Approved
SetrobuvirThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Setrobuvir.Investigational
SildenafilThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Saxagliptin can be decreased when it is combined with Siltuximab.Approved, Investigational
Silver sulfadiazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Silver sulfadiazine.Approved, Vet Approved
SimeprevirThe serum concentration of Saxagliptin can be increased when it is combined with Simeprevir.Approved
SirolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Sirolimus.Approved, Investigational
SitafloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sitafloxacin.Experimental, Investigational
SparfloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sparfloxacin.Approved, Investigational
SpiraprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Spirapril.Approved
St. John's WortThe serum concentration of Saxagliptin can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StanoloneStanolone may increase the hypoglycemic activities of Saxagliptin.Illicit, Investigational
StanozololStanozolol may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
StiripentolThe serum concentration of Saxagliptin can be increased when it is combined with Stiripentol.Approved
SuccinylsulfathiazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Succinylsulfathiazole.Experimental
SulfacetamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfacetamide.Approved
SulfachlorpyridazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfachlorpyridazine.Vet Approved
SulfacytineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfacytine.Approved
SulfadiazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfadiazine.Approved, Investigational, Vet Approved
SulfadicramideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfadicramide.Experimental
SulfadimethoxineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfadimethoxine.Approved, Vet Approved
SulfadoxineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfadoxine.Approved, Investigational
SulfaethoxypyridazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaethoxypyridazine.Vet Approved
SulfaguanidineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaguanidine.Experimental
SulfaisodimidineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaisodimidine.Experimental
SulfamazoneThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamazone.Experimental
SulfamerazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamerazine.Approved, Vet Approved
SulfameterThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfameter.Approved
SulfamethazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamethazine.Approved, Investigational, Vet Approved
SulfamethizoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamethizole.Approved, Investigational, Vet Approved
SulfamethoxazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamethoxazole.Approved
SulfamethoxypyridazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamethoxypyridazine.Experimental
SulfametomidineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfametomidine.Experimental
SulfametopyrazineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfametopyrazine.Approved, Withdrawn
SulfamoxoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfamoxole.Approved
SulfanilamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfanilamide.Approved
SulfanitranThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfanitran.Vet Approved
SulfaperinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaperin.Experimental
SulfaphenazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaphenazole.Approved
SulfapyridineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfapyridine.Approved
SulfaquinoxalineThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfaquinoxaline.Vet Approved
SulfasalazineSulfasalazine may increase the hypoglycemic activities of Saxagliptin.Approved
SulfathiazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfathiazole.Approved, Vet Approved
SulfathioureaThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfathiourea.Experimental
SulfatolamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfatolamide.Experimental
SulfisoxazoleThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Sumatriptan.Approved, Investigational
SunitinibSaxagliptin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.Approved, Investigational
Technetium Tc-99m ciprofloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Technetium Tc-99m ciprofloxacin.Investigational
TelaprevirThe serum concentration of Saxagliptin can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Saxagliptin can be increased when it is combined with Telithromycin.Approved
TemafloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Temafloxacin.Withdrawn
TemocaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Temocapril.Experimental, Investigational
TemsirolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Temsirolimus.Approved
TerbinafineThe serum concentration of Saxagliptin can be decreased when it is combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Saxagliptin can be decreased when it is combined with Terfenadine.Approved, Withdrawn
TestosteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Testosterone.Approved, Investigational
Testosterone cypionateTestosterone cypionate may increase the hypoglycemic activities of Saxagliptin.Approved
Testosterone enanthateTestosterone enanthate may increase the hypoglycemic activities of Saxagliptin.Approved
Testosterone propionateTestosterone propionate may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved, Withdrawn
Testosterone undecanoateTestosterone undecanoate may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
TetracosactideThe serum concentration of Saxagliptin can be decreased when it is combined with Tetracosactide.Approved
TianeptineTianeptine may decrease the hypoglycemic activities of Saxagliptin.Approved, Investigational
TipranavirThe serum concentration of Saxagliptin can be increased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Saxagliptin can be decreased when it is combined with Tocilizumab.Approved
TolazamideSaxagliptin may increase the hypoglycemic activities of Tolazamide.Approved, Investigational
TolbutamideSaxagliptin may increase the hypoglycemic activities of Tolbutamide.Approved, Investigational
ToloxatoneToloxatone may increase the hypoglycemic activities of Saxagliptin.Approved
TopiramateThe serum concentration of Saxagliptin can be decreased when it is combined with Topiramate.Approved
TorasemideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Torasemide.Approved
TrandolaprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Trandolapril.Approved
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
TrazodoneTrazodone may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
TriamcinoloneThe serum concentration of Saxagliptin can be decreased when it is combined with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimipramineTrimipramine may decrease the hypoglycemic activities of Saxagliptin.Approved
TriptorelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Triptorelin.Approved, Vet Approved
TroglitazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Troglitazone.Investigational, Withdrawn
Trolamine salicylateTrolamine salicylate may increase the hypoglycemic activities of Saxagliptin.Approved
TroleandomycinThe serum concentration of Saxagliptin can be increased when it is combined with Troleandomycin.Approved
TrovafloxacinThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Trovafloxacin.Approved, Investigational, Withdrawn
UbidecarenoneThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Ubidecarenone.Approved, Investigational, Nutraceutical
VemurafenibThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Saxagliptin.Approved
VerapamilThe serum concentration of Saxagliptin can be increased when it is combined with Verapamil.Approved
VoriconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Vorinostat.Approved, Investigational
XipamideThe therapeutic efficacy of Saxagliptin can be increased when used in combination with Xipamide.Experimental
ZimelidineZimelidine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
ZiprasidoneThe serum concentration of Saxagliptin can be increased when it is combined with Ziprasidone.Approved
ZofenoprilThe risk or severity of angioedema can be increased when Saxagliptin is combined with Zofenopril.Experimental
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.

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
Human Metabolome Database
HMDB0015634
KEGG Drug
D08996
PubChem Compound
11243969
PubChem Substance
99443245
ChemSpider
9419005
BindingDB
11542
ChEBI
71272
ChEMBL
CHEMBL385517
PharmGKB
PA165958362
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Saxagliptin
ATC Codes
A10BH03 — SaxagliptinA10BD10 — Metformin and saxagliptinA10BD21 — Saxagliptin and dapagliflozin
AHFS Codes
  • 68:20.05 — Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
FDA label
Download (492 KB)
MSDS
Download (479 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
1CompletedNot AvailableDiabetes Mellitus (DM)3
1CompletedNot AvailableType 2 Diabetes Mellitus8
1CompletedBasic ScienceBioequivalence, Log-transformed AUCss and Cmax,ss Values for Saxagliptin and Metformin1
1CompletedBasic ScienceType 2 Diabetes Mellitus3
1CompletedTreatmentType 2 Diabetes Mellitus2
1TerminatedNot AvailableType 2 Diabetes Mellitus1
1WithdrawnNot AvailableType 2 Diabetes Mellitus1
2Active Not RecruitingTreatmentInsulin Resistance / Type 2 Diabetes Mellitus1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 11
2CompletedTreatmentImpaired Glucose Tolerance (IGT)1
2CompletedTreatmentType 2 Diabetes Mellitus2
2, 3CompletedTreatmentType 2 Diabetes Mellitus, CKD and Albuminuria / Type 2 Diabetes Mellitus, CKD3 and Albuminuria1
3Active Not RecruitingTreatmentDiabetes Mellitus (DM)1
3CompletedOtherDiabetes Mellitus (DM)1
3CompletedPreventionDiabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
3CompletedTreatmentDiabetes Mellitus (DM)3
3CompletedTreatmentDisorder of Glucose Regulation / Polycystic Ovaries Syndrome1
3CompletedTreatmentInadequate Glycaemic Control / Type 2 Diabetes Mellitus / Type2 Diabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus28
3Not Yet RecruitingTreatmentType 2 Diabetes Mellitus2
3RecruitingTreatmentType 2 Diabetes Mellitus1
4Active Not RecruitingNot AvailableType 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
4CompletedBasic ScienceType 2 Diabetes Mellitus1
4CompletedTreatmentBMI >30 kg/m2 / Pre-Diabetic1
4CompletedTreatmentCoronary Artery Disease / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetes Mellitus, Non-Insulin-Dependent1
4CompletedTreatmentInadequate Glycaemic Control / Type 2 Diabetes Mellitus / Type2 Diabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus8
4CompletedTreatmentType2 Diabetes Mellitus1
4Enrolling by InvitationTreatmentMicroalbuminuria / Microalbuminuria /Creatinine Ratios ACR1
4Not Yet RecruitingTreatmentBMI >30 kg/m2 / Type 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
4RecruitingBasic ScienceHypertriglyceridemias / Type 2 Diabetes Mellitus1
4RecruitingTreatmentDiabetes Mellitus (DM)1
4RecruitingTreatmentDiabetes Mellitus, Non-Insulin-Dependent / Heart Failure, Unspecified1
4RecruitingTreatmentDiabetes, Diabetes Mellitus Type 12
4RecruitingTreatmentDiabetic Foot Ulcers (DFU)1
4RecruitingTreatmentHeart Failure, Unspecified / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus2
4TerminatedNot AvailableCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
4TerminatedTreatmentImpaired Glucose Tolerance (IGT)1
4Unknown StatusNot AvailableType 2 Diabetes Mellitus1
4Unknown StatusTreatmentPre-Diabetic1
4Unknown StatusTreatmentSevere Hyperglycemia - Blood Glucose Level >300mg/dl / Type 2 Diabetes Mellitus1
4Unknown StatusTreatmentType 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableType 2 Diabetes Mellitus5
Not AvailableRecruitingPreventionIncretinomimetics / Pancreas / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentImpaired Fasting Glucose (IFG) / Impaired Glucose Tolerance (IGT) / Type 2 Diabetes Mellitus1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus2
Not AvailableUnknown StatusSupportive CareCystic Fibrosis (CF)2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coated, extended releaseOral
TabletOral
Tablet, film coatedOral
TabletOral2.5 mg
TabletOral5 mg
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral2.5 mg
Tablet, film coatedOral5 mg/1
Tablet, film coatedOral5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6395767No2001-02-162021-02-16Us
USRE44186No2003-07-312023-07-31Us
US7951400No2008-11-302028-11-30Us
US8628799No2005-07-132025-07-13Us
US8501698No2007-06-202027-06-20Us
US6414126No2000-10-042020-10-04Us
US6515117No2000-10-042020-10-04Us
US6936590No2000-10-042020-10-04Us
US9198925No2000-10-042020-10-04Us
US7919598No2009-12-162029-12-16Us
US8361972No2008-03-212028-03-21Us
US8716251No2008-03-212028-03-21Us
US8221786No2008-03-212028-03-21Us
US9339472No2005-07-132025-07-13Us

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as alpha amino acid amides. These are amide derivatives of alpha amino acids.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Alpha amino acid amides
Alternative Parents
N-acylpiperidines / N-acylpyrrolidines / Tertiary carboxylic acid amides / Tertiary alcohols / Cyclic alcohols and derivatives / Nitriles / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Monoalkylamines
show 2 more
Substituents
Alpha-amino acid amide / N-acyl-piperidine / N-acylpyrrolidine / Piperidine / Cyclic alcohol / Pyrrolidine / Tertiary carboxylic acid amide / Tertiary alcohol / Carboxamide group / Carbonitrile
show 16 more
Molecular Framework
Aliphatic heteropolycyclic compounds
External Descriptors
tertiary alcohol, azabicycloalkane, monocarboxylic acid amide, adamantanes, nitrile (CHEBI:71272)

Targets

Details
1. Dipeptidyl peptidase 4
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 bindi...
Gene Name
DPP4
Uniprot ID
P27487
Uniprot Name
Dipeptidyl peptidase 4
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
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 ...
Gene Name
SLCO4C1
Uniprot ID
Q6ZQN7
Uniprot Name
Solute carrier organic anion transporter family member 4C1
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, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
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]

Drug created on March 19, 2008 10:24 / Updated on August 14, 2018 04:32