vericiguat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
guanylate cyclase activators and stimulators 5439 1350653-20-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vericiguat
  • verquvo
  • BAY 1021189
  • MK-1242
Vericiguat is a stimulator of soluble guanylate cyclase (sGC), an important enzyme in the nitric oxide (NO) signaling pathway. When NO binds to sGC, the enzyme catalyzes the synthesis of intracellular cyclic guanosine monophosphate (cGMP), a second messenger that plays a role in the regulation of vascular tone, cardiac contractility, and cardiac remodeling. Heart failure is associated with impaired synthesis of NO and decreased activity of sGC, which may contribute to myocardial and vascular dysfunction. By directly stimulating sGC, independently of and synergistically with NO, vericiguat augments levels of intracellular cGMP, leading to smooth muscle relaxation and vasodilation.
  • Molecular weight: 426.39
  • Formula: C19H16F2N8O2
  • CLOGP: 3.20
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 3
  • TPSA: 146.86
  • ALOGS: -4.14
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PIK3CG,PRKDC 8
kinase-selectivity-class ACVR2B,AXL 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 19, 2021 FDA MERCK SHARP DOHME
July 16, 2021 EMA BAYER AG
June 23, 2021 PMDA BAYER YAKUHIN, Ltd.

FDA Adverse Event Reporting System (Female)

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
Hypotension 43.81 36.78 22 313 325375 90302737

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
Hypotension 105.09 43.07 59 615 257572 42363089
Death 64.13 43.07 55 619 471130 42149531
Cardiac failure 52.82 43.07 28 646 106828 42513833
Ejection fraction abnormal 52.00 43.07 10 664 1285 42619376

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
Hypotension 71.50 37.40 39 495 523810 110064955
Cardiac failure 62.78 37.40 26 508 187600 110401165

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01DX22 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
VASODILATORS USED IN CARDIAC DISEASES
Other vasodilators used in cardiac diseases
FDA MoA N0000190484 Guanylate Cyclase Stimulators
FDA EPC N0000190485 Soluble Guanylate Cyclase Stimulator
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:76022 soluble guanylate cyclase activator

Related Drugs by ATC class:

C01DX Other vasodilators used in cardiac diseases 18 drugs
benziodaronecarbocromencinepazetcloridaroldilazepefloxateetafenoneheptaminolhexobendineimolamineitramin tosilatelinsidomine show all 18 →

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

DiseaseRelationSNOMED_IDDOID
Chronic heart failure indication 48447003
Heart failure indication 84114007 DOID:6000
Pregnancy, function contraindication 289908002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 11439642 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 8921377 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9993476 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 11439642 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 8921377 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9993476 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 11439642 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 8921377 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9993476 May 19, 2031 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9604948 Nov. 26, 2032 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9604948 Nov. 26, 2032 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL 9604948 Nov. 26, 2032 REDUCING THE RISK OF CARDIOVASCULAR DEATH AND HEART FAILURE (HF) HOSPITALIZATION FOLLOWING A HOSPITALIZATION FOR HF OR NEED FOR OUTPATIENT IV DIURETICS, IN ADULTS WITH SYMPTOMATIC CHRONIC HF AND EJECTION FRACTION LESS THAN 45%

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 19, 2026 NEW CHEMICAL ENTITY
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 19, 2026 NEW CHEMICAL ENTITY
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 19, 2026 NEW CHEMICAL ENTITY
10MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 21, 2029 REVISION TO THE RECOMMENDED STARTING DOSAGE
2.5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 21, 2029 REVISION TO THE RECOMMENDED STARTING DOSAGE
5MG VERQUVO MSD N214377 Jan. 19, 2021 RX TABLET ORAL Jan. 21, 2029 REVISION TO THE RECOMMENDED STARTING DOSAGE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Guanylate cyclase soluble subunit beta-1 Enzyme ACTIVATOR DRUG LABEL DRUG LABEL
Guanylate cyclase soluble subunit beta-1 Enzyme ACTIVATOR EC50 6 SCIENTIFIC LITERATURE

External reference:

IDSource
D11051 KEGG_DRUG
LV66ADM269 UNII
C4078709 UMLSCUI
CHEBI:142432 CHEBI
CHEMBL4066936 ChEMBL_ID
54674461 PUBCHEM_CID
DB15456 DRUGBANK_ID
9805 INN_ID
C000603960 MESH_SUPPLEMENTAL_RECORD_UI
10010 IUPHAR_LIGAND_ID
1145150000 SNOMEDCT_US
1145164000 SNOMEDCT_US
4040006 VANDF
342963 MMSL
39282 MMSL
d09705 MMSL
018619 NDDF
2475830 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5028 TABLET, FILM COATED 2.50 mg ORAL NDA 34 sections
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5028 TABLET, FILM COATED 2.50 mg ORAL NDA 34 sections
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5029 TABLET, FILM COATED 5 mg ORAL NDA 34 sections
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5029 TABLET, FILM COATED 5 mg ORAL NDA 34 sections
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5030 TABLET, FILM COATED 10 mg ORAL NDA 34 sections
VERQUVO HUMAN PRESCRIPTION DRUG LABEL 1 0006-5030 TABLET, FILM COATED 10 mg ORAL NDA 34 sections