Omarigliptin

Summary

Omarigliptin (CHEMBL2105762) is an approved small molecule targeting DPP4; indicated across 2 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 1 (DPP4)
• Indications: 2 conditions
• Clinical trials: 18
• Chemistry: 398.4 Da · C17H20F2N4O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105762
Name	Omarigliptin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	46209133
Molecular formula	C17H20F2N4O3S
Molecular weight	398.4
InChIKey	MKMPWKUAHLTIBJ-ISTRZQFTSA-N

SMILES: CS(=O)(=O)N1C=C2CN(CC2=N1)[C@@H]3C[C@@H]([C@H](OC3)C4=C(C=CC(=C4)F)F)N

IUPAC name: (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine

Also known as: MK-3102, Omarigliptin, Omarigliptina, Omarigliptine, OMARIGLIPTIN

Parent form; salt/anhydrous children: CHEMBL3234203

Patent coverage: 395 distinct patent families (1,107 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,093 (99%) 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

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	9.1	0%	P27487

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Voltage-gated inwardly rectifying potassium channel KCNH2, Dipeptidyl peptidase 4, Dipeptidyl peptidase 4, Dipeptidyl peptidase 4.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	9.1	Ki	0.8	nM	CHEMBL_ACT_14597078
DPP4	8.8	IC50	1.6	nM	CHEMBL_ACT_14597077
DPP4	8.8	IC50	1.6	nM	CHEMBL_ACT_25636113
DPP4	8.8	IC50	1.6	nM	CHEMBL_ACT_25636156
DPP4	8.7	IC50	2	nM	CHEMBL_ACT_27811436
DPP4	8.65	IC50	2.22	nM	CHEMBL_ACT_16763284
DPP4	8.6	EC50	2.5	nM	CHEMBL_ACT_25636112
DPP4	8.59	IC50	2.6	nM	CHEMBL_ACT_16394165
DPP4	8.56	Kd	2.75	nM	CHEMBL_ACT_16763287
DPP4	8.56	Kd	2.75	nM	CHEMBL_ACT_19483872
DPP4	8.51	IC50	3.1	nM	CHEMBL_ACT_20653421
DPP4	8.38	IC50	4.2	nM	CHEMBL_ACT_27085580
P14740	8.38	IC50	4.2	nM	CHEMBL_ACT_28170389
P28843	7.36	IC50	43.9	nM	CHEMBL_ACT_14597092

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

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
diabetes mellitus	3	MONDO:0005015	EFO:0000400
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 18.

Phase distribution

Phase	Trials
PHASE3	11
PHASE1	3
PHASE4	2
PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06449235	PHASE4	NOT_YET_RECRUITING	Real-World Evaluation of Omarigliptin for Type 2 Diabetes Meliitus in Bangladesh
NCT02906709	PHASE4	COMPLETED	Omarigliptin Add-on to Insulin in Japanese Participants With Type 2 Diabetes Mellitus (T2DM, MK-3102-039)
NCT01682759	PHASE3	COMPLETED	A Study of the Safety and Efficacy of Omarigliptin (MK-3102) Compared With Glimepiride in Participants With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin (MK-3102-016)
NCT01697592	PHASE3	COMPLETED	Omarigliptin (MK-3102) Clinical Trial - Add-on to Oral Antihyperglycemic Agent Study in Japanese Participants With Type 2 Diabetes Mellitus (MK-3102-015)
NCT01698775	PHASE3	COMPLETED	A Study of Omarigliptin (MK-3102) in Participants With Type 2 Diabetes Mellitus With Chronic Kidney Disease or Kidney Failure on Dialysis (MK-3102-019)
NCT01703208	PHASE3	TERMINATED	A Study to Assess Cardiovascular Outcomes Following Treatment With Omarigliptin (MK-3102) in Participants With Type 2 Diabetes Mellitus (MK-3102-018)
NCT01703221	PHASE3	COMPLETED	Omarigliptin (MK-3102) Clinical Trial - Placebo- and Sitagliptin-Controlled Monotherapy Study in Japanese Patients With Type 2 Diabetes Mellitus (MK-3102-020)
NCT01704261	PHASE3	COMPLETED	Addition of Omarigliptin (MK-3102) to Participants With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Combination Therapy With Glimepiride and Metformin (MK-3102-022)
NCT01717313	PHASE3	COMPLETED	A Study to Assess the Safety and Efficacy of Omarigliptin (MK-3102) in Participants With Type 2 Diabetes Mellitus (T2DM) and Inadequate Glycemic Control (MK-3102-011)
NCT01755156	PHASE3	COMPLETED	A Study to Evaluate the Safety, Tolerability, and Efficacy of the Addition of Omarigliptin (MK-3102) to Participants With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Metformin Therapy (MK-3102-024)
NCT01814748	PHASE3	COMPLETED	A Study of the Safety and Efficacy of Omarigliptin (MK-3102) in ≥18 and <45 Year-Old Participants With Type 2 Diabetes Mellitus and Inadequate Glycemic Control (MK-3102-028)
NCT01841697	PHASE3	COMPLETED	Study to Evaluate the Safety and Efficacy of the Addition of Omarigliptin (MK-3102) Compared With the Addition of Sitagliptin in Participants With Type 2 Diabetes Mellitus With Inadequate Glycemic Control on Metformin (MK-3102-026)
NCT01863667	PHASE3	TERMINATED	A Study to Evaluate the Safety and Efficacy of Omarigliptin (MK-3102) Compared With Glimepiride in Participants With Type 2 Diabetes Mellitus for Whom Metformin is Inappropriate (MK-3102-027)
NCT01217073	PHASE2	COMPLETED	A Dose-Range Finding Study in Participants With Type 2 Diabetes (MK-3102-006)
NCT01088711	PHASE1	COMPLETED	Evaluation of Omarigliptin (MK-3102) in Obese Participants and in Participants With Type 2 Diabetes (MK-3102-004)
NCT01407276	PHASE1	COMPLETED	A Study of Omarigliptin (MK-3102) in Participants With Impaired Renal Function (MK-3102-009)
NCT01767688	PHASE1	COMPLETED	A Pharmacokinetic Study of MK-3102 in Participants With Impaired Hepatic Function (MK-3102-031)
NCT03362398	Not specified	COMPLETED	Omarigliptin & Trelagliptin in Twelve Healthy Egyptian Volunteers

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
ANAGLIPTIN	ChEMBL	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
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