Gosogliptin
drug drugOn this page
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
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL515387 |
| Name | Gosogliptin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 11516136 |
| Molecular formula | C17H24F2N6O |
| Molecular weight | 366.4 |
| InChIKey | QWEWGXUTRTXFRF-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):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| DPP4 | 7.95 | IC50 | 11.3 | nM | CHEMBL_ACT_2516375 |
| DPP4 | 7.89 | IC50 | 12.9 | nM | CHEMBL_ACT_12588815 |
| DPP4 | 7.89 | IC50 | 12.9 | nM | CHEMBL_ACT_2515605 |
| P14740 | 7.89 | IC50 | 12.8 | nM | CHEMBL_ACT_2516376 |
| DPP7 | 5.48 | IC50 | 3300 | nM | CHEMBL_ACT_2515624 |
| DPP9 | 5.22 | IC50 | 5980 | nM | CHEMBL_ACT_2515564 |
| DPP8 | 5.16 | IC50 | 7000 | nM | CHEMBL_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) | Phase | MONDO | EFO |
|---|---|---|---|
| type 2 diabetes mellitus | 3 | MONDO:0005148 | MONDO:0005148 |
| chronic kidney disease | 1 | MONDO:0005300 | EFO:0003884 |
Clinical trials
Total trials: 2.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03088670 | PHASE3 | COMPLETED | Efficacy 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. |
| NCT00596518 | PHASE1 | COMPLETED | A 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.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- In clinical trials for: type 2 diabetes mellitus