DGIdb - SITAGLIPTIN Drug Record

SITAGLIPTIN chembl:CHEMBL1422 Approved

Alternate Names:

MK-0431
JANUVIA
LEZ763
SITAGLIPTIN
LEZ-763
SITAGLIPTINUM
SITAGLIPTINA
SITAGLIPTAN
SITAGLIPTINE
SITAGLIPTIN PHOSPHATE
JANUVIA®
(2R)-4-OXO-4-[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE
drugbank:01261
rxcui:593411
chemidplus:486460-32-6
pubchem.compound:4369359
chembl:CHEMBL1422

Drug Info:

Drug Class	hypoglycemic agents
Year of Approval	2006
FDA Approval	not approved
Drug Class	Small Molecule
Drug Indications	antidiabetic
Drug Categories	pyrazines
Drug Categories	agents causing angioedema
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	hypoglycemia-associated agents
Drug Categories	oat3/slc22a8 substrates
Drug Categories	p-glycoprotein substrates

(4 More Sources)

Publications:

Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab
Bergman et al., 2006, Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers., Clin Ther
Gallwitz, 2007, Sitagliptin: Profile of a novel DPP-4 inhibitor for the treatment of type 2 diabetes., Drugs Today
Pratley et al., 2007, Inhibition of DPP-4: a new therapeutic approach for the treatment of type 2 diabetes., Curr Med Res Opin
Lyseng-Williamson, 2007, Sitagliptin., Drugs
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Richter et al., 2008, Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes., Vasc Health Risk Manag
Herman et al., 2005, Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses., Clin. Pharmacol. Ther.
Karasik et al., 2008, Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials., Curr Med Res Opin
Miller et al., Sitagliptin: a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes., Ann Pharmacother
Herman et al., 2006, Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects., J Clin Pharmacol
Gallwitz, 2006, Therapies for the treatment of type 2 diabetes mellitus based on incretin action., Minerva Endocrinol.
Hermansen et al., 2007, Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin., Diabetes Obes Metab

SITAGLIPTIN DPP4

Interaction Score: 5.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Sitagliptin

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
16490580 17315049 17407649 17352516 11752352 19065993 16338283 18182122 16868220 16855072 16682937 17593236

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
SITAGLIPTIN GPR119

Interaction Score: 2.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SITAGLIPTIN GLP1R

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27160388

Sources:
PharmGKB

DrugBank: DB01261

Version: 5.1.7

Alternate Names:

SITAGLIPTIN DrugBank Drug Name

486460-32-6 CAS Number

Janumet Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Richter et al., 2008, Emerging role of dipeptidyl peptidase-4 inhibitors in the management of type 2 diabetes., Vasc Health Risk Manag

Herman et al., 2005, Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses., Clin. Pharmacol. Ther.

Gallwitz, 2006, Therapies for the treatment of type 2 diabetes mellitus based on incretin action., Minerva Endocrinol.

TEND: SITAGLIPTIN
- Version: 01-August-2011
Alternate Names:

SITAGLIPTIN Primary Drug Name

Drug Info:

Year of Approval 2006

Drug Class hypoglycemic agents

Publications:
TdgClinicalTrial: SITAGLIPTIN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval not approved

Publications:
PharmGKB: sitagliptin
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab
TTD: LEZ763
- Version: 2020.06.01
Alternate Names:

D05RTM TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178102906
- Version: 29-September-2020
Alternate Names:

SITAGLIPTIN GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Sitagliptin
- Version: 2020.06.01
Alternate Names:

D0U2JP TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1422
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	Sitagliptin
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

SITAGLIPTIN	DrugBank Drug Name
486460-32-6	CAS Number
Janumet	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

SITAGLIPTIN Drug Record

SITAGLIPTIN chembl:CHEMBL1422 Approved

Alternate Names:

Drug Info:

Publications:

SITAGLIPTIN DPP4

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Sitagliptin Novel drug target Established target Specific Action of the Ligand Inhibition

PMIDs: 16490580 17315049 17407649 17352516 11752352 19065993 16338283 18182122 16868220 16855072 16682937 17593236

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

SITAGLIPTIN GPR119

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

SITAGLIPTIN GLP1R

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27160388

Sources: PharmGKB

DrugBank: DB01261

Alternate Names: SITAGLIPTIN DrugBank Drug Name 486460-32-6 CAS Number Janumet Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: SITAGLIPTIN

Alternate Names: SITAGLIPTIN Primary Drug Name

Drug Info: Year of Approval 2006 Drug Class hypoglycemic agents

Publications:

TdgClinicalTrial: SITAGLIPTIN

Alternate Names:

Drug Info: Drug Indications antidiabetic Drug Class Small Molecule FDA Approval not approved

Publications:

PharmGKB: sitagliptin

Alternate Names:

Drug Info:

Publications: Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab

TTD: LEZ763

Alternate Names: D05RTM TTD Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178102906

Alternate Names: SITAGLIPTIN GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Sitagliptin

Alternate Names: D0U2JP TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1422

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Sitagliptin

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
16490580 17315049 17407649 17352516 11752352 19065993 16338283 18182122 16868220 16855072 16682937 17593236

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
27160388

Sources:
PharmGKB

Alternate Names:

SITAGLIPTIN DrugBank Drug Name

486460-32-6 CAS Number

Janumet Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

SITAGLIPTIN Primary Drug Name

Drug Info:

Year of Approval 2006

Drug Class hypoglycemic agents

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval not approved

Publications:

Javorský M et al., 2016, A missense variant in GLP1R gene is associated with the glycaemic response to treatment with gliptins., Diabetes Obes Metab

Alternate Names:

D05RTM TTD Drug ID

Alternate Names:

SITAGLIPTIN GuideToPharmacology Ligand Name

Alternate Names:

D0U2JP TTD Drug ID