Retagliptin

Summary

Retagliptin (CHEMBL4297435) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including type 2 diabetes mellitus and kidney failure.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 16
• Chemistry: 464.4 Da · C19H18F6N4O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297435
Name	Retagliptin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	44193830
Molecular formula	C19H18F6N4O3
Molecular weight	464.4
InChIKey	WIIAMRXFUJLYEF-SNVBAGLBSA-N

SMILES: COC(=O)C1=C2CN(CCN2C(=N1)C(F)(F)F)C(=O)C[C@@H](CC3=CC(=C(C=C3F)F)F)N

IUPAC name: methyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-6,8-dihydro-5H-imidazo[1,5-a]pyrazine-1-carboxylate

Also known as: Retagliptin, SP-2086, Sp2086, SP2086, RETAGLIPTIN

Patent coverage: 58 distinct patent families (125 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 121 (97%) of the total. 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: 1 (assay-derived). Sample: Dipeptidyl peptidase 4.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	7.92	IC50	12	nM	CHEMBL_ACT_25636106

Target pathways

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

Indications & clinical

Indications

2 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
kidney failure	1	MONDO:0001106	HP:0000083

Clinical trials

Total trials: 16.

Phase distribution

Phase	Trials
PHASE1	13
PHASE3	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04667143	PHASE3	UNKNOWN	Dual Add-on Therapy in Type 2 Diabetes Poorly Controlled With Metformin Monotherapy
NCT05054842	PHASE3	UNKNOWN	Clinical Study of Retagliptin Phosphate Combined With Metformin in the Treatment of Type 2 Diabetes
NCT01969357	PHASE2	COMPLETED	A Study of the Effectiveness and Safety of SP2086 to Treat Type 2 Diabetes
NCT02500485	PHASE1	UNKNOWN	The Drug-drug Interaction of SHR3824 and SP2086
NCT02813863	PHASE1	COMPLETED	The Drug-drug Interaction of SP2086 and Metformin
NCT02815657	PHASE1	COMPLETED	The Drug-drug Interaction of SP2086 and Valsartan
NCT02815722	PHASE1	COMPLETED	The Drug-drug Interaction of SP2086 and Simvastatin
NCT02815748	PHASE1	COMPLETED	The Metabolite Identification and Material Balance Study of SP2086
NCT02815774	PHASE1	COMPLETED	SP2086 Pharmacokinetic Study in Renal Insufficiency Patients
NCT02815787	PHASE1	COMPLETED	The Drug -Drug Interaction of SP2086 and Glyburide
NCT02817217	PHASE1	UNKNOWN	The DDI Study of SP2086 and Valsartan
NCT02817243	PHASE1	UNKNOWN	The DDI Study of SP2086 and Simvastatin
NCT02821871	PHASE1	UNKNOWN	the Food Effect Pharmacokinetic, Material Balance and Metabolite Identification of SP2086 in Healthy Volunteers
NCT02822534	PHASE1	UNKNOWN	The Pharmacokinetics and Pharmacodynamics Study of Single and Multiple Dose of SP2086 in Type 2 Diabetes Patients
NCT02826044	PHASE1	UNKNOWN	The Pharmacokinetics Study of Single and Multiple Dose of SP2086 in Healthy Volunteers
NCT06035406	PHASE1	UNKNOWN	A Trial of SP2086 With Hepatic Insufficiency

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).