Vibegron

Summary

Vibegron (CHEMBL2107826) is an approved small-molecule β-adrenergic agonist (ATC G04BD15) targeting ADRB3; indicated across 6 conditions including overactive bladder and irritable bowel syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G04BD15
• Targets: 1 (ADRB3)
• Indications: 6 conditions
• Clinical trials: 14
• Chemistry: 444.5 Da · C26H28N4O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2107826
Name	Vibegron
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	44472635
ChEBI	CHEBI:142418
ATC	G04BD15
Molecular formula	C26H28N4O3
Molecular weight	444.5
InChIKey	DJXRIQMCROIRCZ-XOEOCAAJSA-N

SMILES: C1C[C@@H](N[C@@H]1CC2=CC=C(C=C2)NC(=O)[C@@H]3CCC4=NC=CC(=O)N34)[C@@H](C5=CC=CC=C5)O

IUPAC name: (6S)-N-[4-[[(2S,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl]methyl]phenyl]-4-oxo-7,8-dihydro-6H-pyrrolo[1,2-a]pyrimidine-6-carboxamide

ChEBI definition: A pyrrolopyrimidine obtained by formal condensation of the carboxy group of (6S)-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxylic acid with the amino group of (R)-(2R,5S)-5-(4-aminobenzyl)pyrrolidin-2-ylmethanol. It is a β3-adrenergic receptor agonist currently in clinical development for the treatment of patients with overactive bladder.

Pharmacological roles (ChEBI): β-adrenergic agonist.

Also known as: Gemtesa, KRP-114V, Mk4618, Obgemsa, Vibegron, VIBEGRON

Patent coverage: 97 distinct patent families (210 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
ADRB3	β3-adrenoceptor	Agonist	7.96	0.1%	P13945

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Beta-3 adrenergic receptor, Beta-3 adrenergic receptor, Beta-3 adrenergic receptor, Beta-3 adrenergic receptor.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q28524	9.24	EC50	0.57	nM	CHEMBL_ACT_16465454
ADRB3	8.96	EC50	1.1	nM	CHEMBL_ACT_16464511
ADRB3	8.8	EC50	1.6	nM	CHEMBL_ACT_16465470
Q28524	8.15	EC50	7.1	nM	CHEMBL_ACT_16465466
O02662	7.96	EC50	11	nM	CHEMBL_ACT_16465539
P26255	7.07	EC50	86	nM	CHEMBL_ACT_16465446
P26255	6.91	EC50	122	nM	CHEMBL_ACT_16465462

Target pathways

Aggregated over 1 target gene(s): ADRB3.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	ADRB3
Signaling by GPCR	1	ADRB3
Class A/1 (Rhodopsin-like receptors)	1	ADRB3
Amine ligand-binding receptors	1	ADRB3
GPCR downstream signalling	1	ADRB3
Adrenoceptors	1	ADRB3
G alpha (s) signalling events	1	ADRB3
GPCR ligand binding	1	ADRB3

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	1
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	1
carbohydrate metabolic process	1
generation of precursor metabolites and energy	1
energy reserve metabolic process	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
response to cold	1
heat generation	1
negative regulation of multicellular organism growth	1
eating behavior	1
positive regulation of MAPK cascade	1
negative regulation of smooth muscle contraction	1
brown fat cell differentiation	1

Indications & clinical

Indications

6 indications (4 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
overactive bladder	4	MONDO:0006624	EFO:1000781
irritable bowel syndrome	2	MONDO:0005052	EFO:0000555
hypertensive disorder	1	MONDO:0005044	EFO:0000537

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 14.

Phase distribution

Phase	Trials
PHASE3	5
PHASE1	3
PHASE2	2
Not specified	2
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05491525	PHASE2/PHASE3	RECRUITING	A Study of Vibegron in Pediatric Participants 2 Years to Less Than (<) 18 Years of Age With NDO and on CIC
NCT06987383	PHASE3	NOT_YET_RECRUITING	Vibegron for ENergy Thinking and Resilience in Aging
NCT03492281	PHASE3	COMPLETED	A Study to Examine the Safety and Efficacy of a New Drug in Patients With Symptoms of Overactive Bladder (OAB)
NCT03583372	PHASE3	COMPLETED	An Extension Study to Examine the Safety and Tolerability of a New Drug in Patients With Symptoms of Overactive Bladder (OAB).
NCT03902080	PHASE3	COMPLETED	Study to Evaluate the Efficacy, Safety and Tolerability of Vibegron in Men With Overactive Bladder (OAB) Symptoms on Pharmacological Therapy for Benign Prostatic Hyperplasia (BPH)
NCT04103450	PHASE3	COMPLETED	Extension Study of Vibegron in Men With Overactive Bladder (OAB) Symptoms on Pharmacological Therapy for Benign Prostatic Hyperplasia
NCT01314872	PHASE2	COMPLETED	A Study of the Efficacy and Safety of Vibegron (MK-4618) in Participants With Overactive Bladder (OAB) (MK-4618-008)
NCT03806127	PHASE2	COMPLETED	Study to Evaluate the Efficacy and Safety of Vibegron Administered Orally for 12 Weeks to Women With Irritable Bowel Syndrome
NCT01500382	PHASE1	TERMINATED	A Study of the Pharmacokinetics and Pharmacodynamics of Vibegron (MK-4618) in Women With Overactive Bladder (MK-4618-004)
NCT01628042	PHASE1	COMPLETED	A Single Dose Study of the Pharmacokinetics of Vibegron (MK-4618) in Participants With Renal Insufficiency (MK-4618-014)
NCT01737684	PHASE1	COMPLETED	A Single-Dose Study of the Pharmacokinetics of Vibegron (MK-4618) in Adults With Hepatic Insufficiency (MK-4618-013)
NCT06417177	EARLY_PHASE1	RECRUITING	Impact of Early Aging and Menopause on the Vascular Responses to Hypoxia
NCT05067478	Not specified	COMPLETED	Composur: Study to Understand the Performance of Vibegron in Participants with Overactive Bladder (OAB)
NCT06438861	Not specified	WITHDRAWN	Role of Combination Therapy in Women With Refractory Overactive Bladder

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.

106 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	ADRB3
AMIODARONE	ChEMBL	Phase 4 (approved)	ADRB3
AMLODIPINE	ChEMBL	Phase 4 (approved)	ADRB3
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	ADRB3
BEPRIDIL	ChEMBL	Phase 4 (approved)	ADRB3
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB3
BOSUTINIB	ChEMBL	Phase 4 (approved)	ADRB3
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB3
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB3
CELECOXIB	ChEMBL	Phase 4 (approved)	ADRB3
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	ADRB3
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
DANAZOL	ChEMBL	Phase 4 (approved)	ADRB3
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	ADRB3
DISOPYRAMIDE	ChEMBL	Phase 4 (approved)	ADRB3
DOXAZOSIN	ChEMBL	Phase 4 (approved)	ADRB3
EBASTINE	ChEMBL	Phase 4 (approved)	ADRB3
ECONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
ETHINYL ESTRADIOL	ChEMBL	Phase 4 (approved)	ADRB3
FELODIPINE	ChEMBL	Phase 4 (approved)	ADRB3
FENOFIBRATE	ChEMBL	Phase 4 (approved)	ADRB3
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB3
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	ADRB3
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB3
HALOPERIDOL	ChEMBL	Phase 4 (approved)	ADRB3
IBUPROFEN	ChEMBL	Phase 4 (approved)	ADRB3
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB3
IVACAFTOR	ChEMBL	Phase 4 (approved)	ADRB3
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB3
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB3
LORATADINE	ChEMBL	Phase 4 (approved)	ADRB3
LOVASTATIN	ChEMBL	Phase 4 (approved)	ADRB3
MEMANTINE	ChEMBL	Phase 4 (approved)	ADRB3
MICONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
MIRABEGRON	ChEMBL	Phase 4 (approved)	ADRB3
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB3
NEFAZODONE	ChEMBL	Phase 4 (approved)	ADRB3
NELFINAVIR	ChEMBL	Phase 4 (approved)	ADRB3
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
OXICONAZOLE	ChEMBL	Phase 4 (approved)	ADRB3
PAMIDRONIC ACID	ChEMBL	Phase 4 (approved)	ADRB3
PERGOLIDE	ChEMBL	Phase 4 (approved)	ADRB3
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB3
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB3
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB3
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB3
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	ADRB3
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB3
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB3
RALOXIFENE	ChEMBL	Phase 4 (approved)	ADRB3
RITONAVIR	ChEMBL	Phase 4 (approved)	ADRB3
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB3
SIMVASTATIN	ChEMBL	Phase 4 (approved)	ADRB3
SIROLIMUS	ChEMBL	Phase 4 (approved)	ADRB3
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB3