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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
OnglyzaTablet, film coated2.5 mg/1OralAstra Zeneca Pharmaceuticals Lp2014-11-20Not applicableUs
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated2.5 mg/1OralE.R. Squibb & Sons, L.L.C.2009-07-31Not applicableUs
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
OnglyzaTablet, film coated5 mg/1OralCardinal Health2014-11-20Not applicableUs
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mg/1OralAstra Zeneca Pharmaceuticals Lp2014-11-20Not applicableUs
OnglyzaTablet, film coated5 mg/1OralE.R. Squibb & Sons, L.L.C.2009-07-31Not applicableUs
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 mgOralAstrazeneca Canada Inc2009-10-29Not applicableCanada
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mg/1OralPhysicians Total Care, Inc.2011-09-22Not applicableUs
OnglyzaTablet, film coated2.5 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
OnglyzaTablet2.5 mgOralAstrazeneca Canada Inc2011-12-23Not applicableCanada
OnglyzaTablet, film coated5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mg/1OralCardinal Health2009-07-31Not applicableUs
OnglyzaTablet, film coated2.5 mgOralAstra Zeneca Ab2009-10-01Not applicableEu
OnglyzaTablet, film coated5 mgOralAstra 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
QternAstrazeneca 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 KeyQGJUIPDUBHWZPV-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
Pharmacology
IndicationTreatment of type 2 diabetes mellitus to improve glycemic control in combination with other agents or as monotherapy.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Dipeptidyl peptidase 4Proteinyes
inhibitor
HumanP27487 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Saxagliptin.Experimental
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Saxagliptin.Approved, Investigational
AcetaminophenThe serum concentration of Saxagliptin can be decreased when it is combined with Acetaminophen.Approved
AcetohexamideSaxagliptin may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
AlclometasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Alclometasone.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Saxagliptin.Approved, Investigational
AlimemazineThe serum concentration of Saxagliptin can be decreased when it is combined with Alimemazine.Approved, Vet Approved
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Saxagliptin.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Saxagliptin.Experimental
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Saxagliptin.Illicit, Withdrawn
AminoglutethimideThe serum concentration of Saxagliptin can be decreased when it is combined with Aminoglutethimide.Approved
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Saxagliptin.Approved
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
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Saxagliptin.Approved
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
ArtemetherThe serum concentration of Saxagliptin can be decreased when it is combined with Artemether.Approved
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
AtazanavirThe serum concentration of Saxagliptin can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Saxagliptin can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Saxagliptin.Approved
AvasimibeThe serum concentration of Saxagliptin can be decreased when it is combined with Avasimibe.Investigational
AzatadineThe serum concentration of Saxagliptin can be decreased when it is combined with Azatadine.Approved
BalsalazideBalsalazide may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
BenazeprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Benazepril.Approved, Investigational
BendroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Saxagliptin.Withdrawn
BetamethasoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination 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 decreased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Saxagliptin can be increased when it is combined with Bortezomib.Approved, Investigational
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
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Saxagliptin.Approved, Investigational
BumetanideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Bumetanide.Approved
BuserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Buserelin.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Saxagliptin.Approved
CalcitriolThe serum concentration of Saxagliptin can be decreased when it is combined with Calcitriol.Approved, Nutraceutical
CandoxatrilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Candoxatril.Experimental
CaptoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Captopril.Approved
CarbamazepineThe metabolism of Saxagliptin can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypoglycemic activities of Saxagliptin.Withdrawn
CefradineThe serum concentration of Saxagliptin can be decreased when it is combined with Cefradine.Approved
CeritinibThe serum concentration of Saxagliptin can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Cerivastatin.Withdrawn
ChlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Saxagliptin.Withdrawn
ChlorphenesinThe serum concentration of Saxagliptin can be decreased when it is combined with Chlorphenesin.Approved, Vet Approved, Withdrawn
ChlorpropamideSaxagliptin may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorthalidone.Approved
CilazaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Cilazapril.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Saxagliptin.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the hypoglycemic activities of Saxagliptin.Approved
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Saxagliptin.Approved
ClemastineThe serum concentration of Saxagliptin can be increased when it is combined with Clemastine.Approved
ClevidipineThe serum concentration of Saxagliptin can be decreased when it is combined with Clevidipine.Approved
ClofibrateThe serum concentration of Saxagliptin can be decreased when it is combined with Clofibrate.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Saxagliptin.Approved, Vet Approved
ClotrimazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Saxagliptin can be decreased when it is combined with Clozapine.Approved
CobicistatThe serum concentration of Saxagliptin can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Saxagliptin can be decreased when it is combined with Colchicine.Approved
ConivaptanThe serum concentration of Saxagliptin can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Saxagliptin.Approved
CorticotropinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Cortisone acetate.Approved
CrizotinibThe serum concentration of Saxagliptin can be increased when it is combined with Crizotinib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Saxagliptin.Approved
CyclophosphamideThe serum concentration of Saxagliptin can be decreased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Saxagliptin.Approved, Investigational, Vet 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
DanazolThe therapeutic efficacy of Saxagliptin can be decreased when used in combination 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
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Saxagliptin.Approved
dersalazinedersalazine may increase the hypoglycemic activities of Saxagliptin.Investigational
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Saxagliptin.Approved
DesogestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Desogestrel.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Saxagliptin.Approved
DexamethasoneThe serum concentration of Saxagliptin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Diazoxide.Approved
DicloxacillinThe serum concentration of Saxagliptin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Saxagliptin.Approved
DienogestThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Dienogest.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Saxagliptin.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Saxagliptin.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Saxagliptin.Approved
DihydroergotamineThe serum concentration of Saxagliptin can be increased when it is combined with Dihydroergotamine.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Saxagliptin.Illicit
DiltiazemThe serum concentration of Saxagliptin can be increased when it is combined with Diltiazem.Approved
DisopyramideSaxagliptin may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Saxagliptin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Saxagliptin.Approved
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 therapeutic efficacy of Saxagliptin can be decreased when used in combination with Drospirenone.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Saxagliptin.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Saxagliptin.Approved
EfavirenzThe serum concentration of Saxagliptin can be decreased 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 adverse effects can be increased when Saxagliptin is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Saxagliptin.Approved, Investigational
EnoxacinEnoxacin may increase the hypoglycemic activities of Saxagliptin.Approved
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
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Saxagliptin.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Saxagliptin.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Saxagliptin.Approved
ErythromycinThe serum concentration of Saxagliptin can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Saxagliptin.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Saxagliptin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Saxagliptin.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Saxagliptin.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Saxagliptin.Approved
Etacrynic acidThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Etacrynic acid.Approved
EthanolThe serum concentration of Saxagliptin can be decreased when it is combined with Ethanol.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Saxagliptin.Approved
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
EtoperidoneEtoperidone may increase the hypoglycemic activities of Saxagliptin.Approved
EtoposideThe serum concentration of Saxagliptin can be decreased when it is combined with Etoposide.Approved
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
FelbamateThe serum concentration of Saxagliptin can be decreased when it is combined with Felbamate.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Saxagliptin.Approved
FlucloxacillinThe serum concentration of Saxagliptin can be decreased when it is combined with Flucloxacillin.Approved
FluconazoleThe serum concentration of Saxagliptin can be increased when it is combined with Fluconazole.Approved
FludrocortisoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Fludrocortisone.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
FluorometholoneThe serum concentration of Saxagliptin can be decreased when it is combined with Fluorometholone.Approved
FluoxetineFluoxetine may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Saxagliptin.Approved, Illicit
FluvastatinThe serum concentration of Saxagliptin can be decreased when it is combined with Fluvastatin.Approved
FluvoxamineThe serum concentration of Saxagliptin can be increased when it is combined with Fluvoxamine.Approved, Investigational
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 adverse effects can be increased when Saxagliptin is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Saxagliptin can be decreased when it is combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
FurosemideThe therapeutic efficacy of Saxagliptin can be decreased 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
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Saxagliptin.Investigational
GarlicThe serum concentration of Saxagliptin can be decreased when it is combined with Garlic.Approved
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
GemfibrozilThe serum concentration of Saxagliptin can be decreased when it is combined with Gemfibrozil.Approved
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
GlibornurideSaxagliptin may increase the hypoglycemic activities of Glibornuride.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
GliquidoneSaxagliptin may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideSaxagliptin may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideSaxagliptin may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Goserelin.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Saxagliptin.Withdrawn
GriseofulvinThe serum concentration of Saxagliptin can be decreased when it is combined with Griseofulvin.Approved, Vet Approved
GuanethidineThe serum concentration of Saxagliptin can be decreased when it is combined with Guanethidine.Approved
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Saxagliptin.Withdrawn
HistrelinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Histrelin.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Saxagliptin.Approved
HydrochlorothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortamateThe serum concentration of Saxagliptin can be decreased when it is combined with Hydrocortamate.Approved
HydrocortisoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroflumethiazide.Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IdelalisibThe serum concentration of Saxagliptin can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of Saxagliptin can be decreased when it is combined with Ifosfamide.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 adverse effects can be increased when Saxagliptin is combined with Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Saxagliptin.Approved
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 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 PorkSaxagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Saxagliptin.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Saxagliptin.Withdrawn
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
IsradipineThe serum concentration of Saxagliptin can be increased when it is combined with Isradipine.Approved
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
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
LansoprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Lansoprazole.Approved, Investigational
LeuprolideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Leuprolide.Approved, Investigational
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Saxagliptin.Approved
LevonorgestrelThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Levonorgestrel.Approved, Investigational
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Saxagliptin.Approved, Nutraceutical
LisinoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Lisinopril.Approved, Investigational
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
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
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Saxagliptin.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
MebanazineMebanazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
MecaserminSaxagliptin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe serum concentration of Saxagliptin can be decreased when it is combined with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MesalazineMesalazine may increase the hypoglycemic activities of Saxagliptin.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Saxagliptin.Approved
MetamizoleThe serum concentration of Saxagliptin can be decreased when it is combined with Metamizole.Withdrawn
MethadoneThe serum concentration of Saxagliptin can be decreased when it is combined with Methadone.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Saxagliptin.Experimental
MethotrimeprazineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methyclothiazide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Saxagliptin.Investigational
MethylprednisoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Saxagliptin.Approved
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
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Saxagliptin.Approved, Illicit
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
MinaprineMinaprine may increase the hypoglycemic activities of Saxagliptin.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with 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
ModafinilThe serum concentration of Saxagliptin can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Moexipril.Approved
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational
NafcillinThe serum concentration of Saxagliptin can be decreased when it is combined with Nafcillin.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Saxagliptin.Approved
NateglinideSaxagliptin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Saxagliptin.Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Saxagliptin.Approved, Withdrawn
NelfinavirThe serum concentration of Saxagliptin can be increased when it is combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Saxagliptin.Investigational
NetupitantThe serum concentration of Saxagliptin can be increased when it is combined with Netupitant.Approved
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 decreased when it is combined with Nicardipine.Approved
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
NorethisteroneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
NorgestimateThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Norgestimate.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with 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
OfloxacinOfloxacin may increase the hypoglycemic activities of Saxagliptin.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 adverse effects can be increased when Saxagliptin is combined with Omapatrilat.Investigational
OmeprazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Saxagliptin.Investigational
OrlistatThe serum concentration of Saxagliptin can be decreased when it is combined with Orlistat.Approved, Investigational
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
OxcarbazepineThe serum concentration of Saxagliptin can be decreased when it is combined with Oxcarbazepine.Approved
OxiconazoleThe serum concentration of Saxagliptin can be decreased when it is combined with Oxiconazole.Approved
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
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
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Saxagliptin.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
PegvisomantThe serum concentration of Saxagliptin can be decreased when it is combined with Pegvisomant.Approved
PentamidineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Pentamidine.Approved
PentobarbitalThe serum concentration of Saxagliptin can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerampanelThe serum concentration of Saxagliptin can be decreased when it is combined with Perampanel.Approved
PerindoprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Pethidine.Approved
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
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
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
PimozideThe serum concentration of Pimozide can be increased when it is combined with Saxagliptin.Approved
PioglitazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Pioglitazone.Approved, Investigational
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
PirlindolePirlindole may increase the hypoglycemic activities of Saxagliptin.Approved
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
PrednisoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Saxagliptin can be decreased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Saxagliptin can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Saxagliptin can be decreased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Progesterone.Approved, Vet Approved
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Saxagliptin.Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Saxagliptin.Investigational
PyridostigmineThe serum concentration of Saxagliptin can be decreased when it is combined with Pyridostigmine.Approved
QuetiapineThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quetiapine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Quinapril.Approved, Investigational
QuinethazoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Quinethazone.Approved
QuinidineThe serum concentration of Saxagliptin can be decreased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Saxagliptin can be decreased when it is combined with Quinine.Approved
RamiprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Ramipril.Approved
RanolazineThe serum concentration of Saxagliptin can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Saxagliptin.Approved
RepaglinideSaxagliptin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RescinnamineThe risk or severity of adverse effects 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
RifampicinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Saxagliptin can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Saxagliptin can be decreased when it is combined with Rifaximin.Approved, Investigational
RilpivirineThe serum concentration of Saxagliptin can be decreased when it is combined with Rilpivirine.Approved
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Saxagliptin.Approved
RisperidoneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Risperidone.Approved, 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.Investigational, Withdrawn
RosoxacinRosoxacin may increase the hypoglycemic activities of Saxagliptin.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Saxagliptin.Approved
RufinamideThe serum concentration of Saxagliptin can be decreased when it is combined with Rufinamide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Saxagliptin.Approved, Vet Approved
SaquinavirThe serum concentration of Saxagliptin can be increased when it is combined with Saquinavir.Approved, Investigational
SelegilineSelegiline may increase the hypoglycemic activities of Saxagliptin.Approved, Investigational, Vet Approved
SeratrodastThe serum concentration of Saxagliptin can be decreased when it is combined with Seratrodast.Approved, Investigational
SertralineSertraline may increase the hypoglycemic activities of Saxagliptin.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Saxagliptin.Approved, Investigational
SiltuximabThe serum concentration of Saxagliptin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Saxagliptin.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Saxagliptin.Approved
SirolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Sirolimus.Approved, Investigational
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
SpiraprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Spirapril.Approved
St. John's WortThe metabolism of Saxagliptin can be increased when combined with St. John&#39;s Wort.Nutraceutical
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
SulfadiazineSaxagliptin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleSaxagliptin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Saxagliptin can be decreased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe serum concentration of Saxagliptin can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SunitinibSaxagliptin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Saxagliptin.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Saxagliptin.Approved, Investigational
TacrolimusThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Saxagliptin can be decreased when it is combined with Tamoxifen.Approved
TelaprevirThe serum concentration of Saxagliptin can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Saxagliptin can be increased when it is combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Saxagliptin.Withdrawn
TemocaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Temocapril.Experimental, Investigational
TemozolomideThe serum concentration of Saxagliptin can be decreased when it is combined with Temozolomide.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Saxagliptin is combined 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.Withdrawn
TesmilifeneThe serum concentration of Saxagliptin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Saxagliptin can be decreased when it is combined with Testosterone.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Saxagliptin.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Saxagliptin.Approved
TiclopidineThe serum concentration of Saxagliptin can be increased when it is combined with Ticlopidine.Approved
TipranavirThe serum concentration of Saxagliptin can be decreased 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
TolbutamideSaxagliptin may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Saxagliptin.Approved
TopiramateThe serum concentration of Saxagliptin can be decreased when it is combined with Topiramate.Approved
TopotecanThe serum concentration of Saxagliptin can be decreased when it is combined with Topotecan.Approved, Investigational
TorasemideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Torasemide.Approved
TrametinibThe serum concentration of Saxagliptin can be decreased when it is combined with Trametinib.Approved
TrandolaprilThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Saxagliptin.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Saxagliptin.Approved
TriamcinoloneThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Saxagliptin.Approved
TrichlormethiazideThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with 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.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Saxagliptin.Approved, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Saxagliptin.Approved, Investigational
VemurafenibThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Saxagliptin can be increased when it is combined with Venlafaxine.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
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Saxagliptin.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Saxagliptin.Withdrawn
ZiprasidoneThe serum concentration of Saxagliptin can be increased when it is combined with Ziprasidone.Approved
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
ATC CodesA10BH03A10BD10A10BD21
AHFS Codes
  • 68:20.05
PDB EntriesNot Available
FDA labelDownload (492 KB)
MSDSDownload (479 KB)
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
Tablet, film coatedOral
TabletOral2.5 mg
TabletOral5 mg
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral2.5 mg
Tablet, film coatedOral5 mg
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
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

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 December 05, 2016 02:43