vibegron 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
beta3-adrenoreceptor agonists 5311 1190389-15-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vibegron
  • beova
  • MK-4618
  • RVT-901
  • KRP-114V
Vibegron is selectively binds to the beta 3 adrenergic receptor (beta3 AR) in bladder smooth muscle, resulting in relaxation of the detrusor muscle.
  • Molecular weight: 444.54
  • Formula: C26H28N4O3
  • CLOGP: 1.87
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 94.03
  • ALOGS: -4.12
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.16 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 4 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 2020 FDA UROVANT SCIENCES GMBH
Sept. 21, 2018 PMDA Kyorin Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pleurothotonus 46.42 43.44 7 95 1198 34955631
Urinary retention 45.59 43.44 12 90 36276 34920553

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Pleurothotonus 42.77 36.41 7 178 2509 79741694

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000185007 Adrenergic beta3-Agonists
FDA EPC N0000185008 beta3-Adrenergic Agonist
CHEBI has role CHEBI:35522 beta-adrenergic agonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Bladder muscle dysfunction - overactive indication 236633002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.78 acidic
pKa2 8.94 Basic
pKa3 2.54 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
75MG GEMTESA UROVANT N213006 Dec. 23, 2020 RX TABLET ORAL 8247415 Dec. 1, 2030 TREATMENT OF OVERACTIVE BLADDER (OAB) WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND URINARY FREQUENCY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
75MG GEMTESA UROVANT N213006 Dec. 23, 2020 RX TABLET ORAL Dec. 23, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Beta-3 adrenergic receptor GPCR AGONIST EC50 8.96 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Beta-3 adrenergic receptor GPCR EC50 7.07 CHEMBL
Beta-3 adrenergic receptor GPCR EC50 7.96 CHEMBL
Beta-3 adrenergic receptor GPCR EC50 9.24 CHEMBL

External reference:

IDSource
M5TSE03W5U UNII
C4279743 UMLSCUI
CHEBI:142418 CHEBI
CHEMBL2107826 ChEMBL_ID
44472635 PUBCHEM_CID
DB14895 DRUGBANK_ID
D10433 KEGG_DRUG
9676 INN_ID
10100 IUPHAR_LIGAND_ID
018600 NDDF
1149377005 SNOMEDCT_US
1149380006 SNOMEDCT_US
4039964 VANDF
2472254 RXNORM
39113 MMSL
d09697 MMSL
C000608232 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
GEMTESA HUMAN PRESCRIPTION DRUG LABEL 1 73336-075 TABLET, FILM COATED 75 mg ORAL NDA 31 sections