Gosogliptin

drug
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Also known as GosogliptinaGosogliptinePF-00734200PF-734,200PF-734200

Summary

Gosogliptin (CHEMBL515387) is an approved small molecule; indicated across 2 conditions including type 2 diabetes mellitus and chronic kidney disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • Indications: 2 conditions
  • Clinical trials: 2
  • Chemistry: 366.4 Da · C17H24F2N6O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL515387
NameGosogliptin
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID11516136
Molecular formulaC17H24F2N6O
Molecular weight366.4
InChIKeyQWEWGXUTRTXFRF-KBPBESRZSA-N

SMILES: C1CN(CC1(F)F)C(=O)[C@@H]2C[C@@H](CN2)N3CCN(CC3)C4=NC=CC=N4

IUPAC name: (3,3-difluoropyrrolidin-1-yl)-[(2S,4S)-4-(4-pyrimidin-2-ylpiperazin-1-yl)pyrrolidin-2-yl]methanone

Also known as: Gosogliptin, Gosogliptina, Gosogliptine, PF-00734200, PF-734,200, PF-734200, GOSOGLIPTIN

Parent form; salt/anhydrous children: CHEMBL3526419

Patent coverage: 254 distinct patent families (785 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Dipeptidyl peptidase 4, Dipeptidyl peptidase 2, Dipeptidyl peptidase 4, Dipeptidyl peptidase 8, Prolyl endopeptidase FAP, Dipeptidyl peptidase 9.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 8 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
DPP47.95IC5011.3nMCHEMBL_ACT_2516375
DPP47.89IC5012.9nMCHEMBL_ACT_12588815
DPP47.89IC5012.9nMCHEMBL_ACT_2515605
P147407.89IC5012.8nMCHEMBL_ACT_2516376
DPP75.48IC503300nMCHEMBL_ACT_2515624
DPP95.22IC505980nMCHEMBL_ACT_2515564
DPP85.16IC507000nMCHEMBL_ACT_2515643

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
chronic kidney disease1MONDO:0005300EFO:0003884

Clinical trials

Total trials: 2.

Phase distribution

PhaseTrials
PHASE31
PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03088670PHASE3COMPLETEDEfficacy and Safety of Gosogliptin as Monotherapy and in Combination With Metformin vs. Vildagliptin as Monotherapy and in Combination With Metformin in Drug-naive Type 2 Diabetic Patients.
NCT00596518PHASE1COMPLETEDA Study to Evaluate the Blood Levels, Safety, and Tolerability of PF-00734200 in Subjects With Impaired Kidney Function and Normal Kidney Function

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).