Anagliptin

Summary

Anagliptin (CHEMBL1929396) is an approved small molecule targeting DPP4; indicated across 1 condition including type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 1 (DPP4)
• Indications: 1 condition
• Clinical trials: 8
• Chemistry: 383.4 Da · C19H25N7O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1929396
Name	Anagliptin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	44513473
Molecular formula	C19H25N7O2
Molecular weight	383.4
InChIKey	LDXYBEHACFJIEL-HNNXBMFYSA-N

SMILES: CC1=NN2C=C(C=NC2=C1)C(=O)NCC(C)(C)NCC(=O)N3CCC[C@H]3C#N

IUPAC name: N-[2-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide

Also known as: Anagliptin, Anagliptina, Anagliptine, CWP-403, Sk-0403, SK-0403, Suiny, ANAGLIPTIN

Parent form; salt/anhydrous children: CHEMBL1929387

Patent coverage: 426 distinct patent families (1,091 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
DPP4	dipeptidyl peptidase 4	Inhibition	8.42	0%	P27487

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

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	8.48	IC50	3.3	nM	CHEMBL_ACT_24872437
FAP	6.42	Ki	380	nM	CHEMBL_ACT_29108081

Target pathways

Aggregated over 1 target gene(s): DPP4.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)	1	DPP4
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)	1	DPP4

Dominant GO biological processes

GO term	Targets
behavioral fear response	1
response to hypoxia	1
proteolysis	1
cell adhesion	1
positive regulation of cell population proliferation	1
negative regulation of extracellular matrix disassembly	1
peptide hormone processing	1
receptor-mediated endocytosis of virus by host cell	1
T cell costimulation	1
regulation of cell-cell adhesion mediated by integrin	1
locomotory exploration behavior	1
psychomotor behavior	1
T cell activation	1
endothelial cell migration	1
symbiont entry into host cell	1

Indications & clinical

Indications

1 indication (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

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
PHASE4	2
PHASE3	2
PHASE2	2
PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07442006	PHASE4	RECRUITING	Glycemic Variability of Combination Therapies in T2DM
NCT02330406	PHASE4	COMPLETED	Randomized Evaluation of Anagliptin Versus Sitagliptin On Low-density lipoproteiN Cholesterol in Diabetes Trial
NCT01529528	PHASE3	COMPLETED	A Study to Efficacy and Safety of CWP-0403 in Type 2 Diabetes Mellitus Patients
NCT01529541	PHASE3	COMPLETED	Efficacy and Safety of CWP-0403 Compared to Sitagliptin in Patients With Type 2 Diabetes Mellitus Insufficiently Controlled With Metformin Alone
NCT00532506	PHASE2	COMPLETED	Phase II Dose-Finding Study of SK-0403 With Type 2 Diabetes Mellitus
NCT01169090	PHASE2	COMPLETED	A Study Comparing the Safety, Tolerance, and Efficacy of Various Doses of SK-0403 Versus Placebo and Sitagliptin 100 mg in Patients Not Well-Controlled on Metformin Therapy
NCT01131091	PHASE1	COMPLETED	A Multicenter, Open Label, Single Dose Study to Evaluate the Effect of Renal Insufficiency on the Pharmacokinetics of SK 0403
NCT04267601	Not specified	UNKNOWN	Korean Observational Study to Evaluate the Efficacy and Safety of Anagliptin Switching From Other DPP4is in type2 DM

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

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

28 molecules share ≥1 primary target. Top 28 by shared-target count:

Molecule	Source	Status	Shared targets
ALOGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4
SAXAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4
EVOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
GEMIFLOXACIN	ChEMBL	Phase 4 (approved)	DPP4
GOSOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
METFORMIN	ChEMBL	Phase 4 (approved)	DPP4
OMARIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
SITAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TENELIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TRELAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
VIDARABINE	ChEMBL	Phase 4 (approved)	DPP4
VILDAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
CAFFEIC ACID	ChEMBL	Phase 3	DPP4
DBPR-108	ChEMBL	Phase 3	DPP4
DUTOGLIPTIN	ChEMBL	Phase 3	DPP4
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	DPP4
QUERCETIN	ChEMBL	Phase 3	DPP4
RESVERATROL	ChEMBL	Phase 3	DPP4
RETAGLIPTIN	ChEMBL	Phase 3	DPP4
TALABOSTAT	ChEMBL	Phase 3	DPP4
CARMEGLIPTIN	ChEMBL	Phase 2	DPP4
COFROGLIPTIN	ChEMBL	Phase 2	DPP4
FLAVONE	ChEMBL	Phase 2	DPP4
GALLIC ACID	ChEMBL	Phase 2	DPP4
GENISTEIN	ChEMBL	Phase 2	DPP4
LUTEOLIN	ChEMBL	Phase 2	DPP4
Carfilzomib	PubChem	Approved	DPP4