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

Stem definition	Drug id	CAS RN
guanylate cyclase activators and stimulators	5439	1350653-20-1

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
10	mg	O

ADMET properties:

None

Approvals:

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

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypotension	66.67	63.64	31	203	221618	34735079

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:76022	soluble guanylyl cyclase activators

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

Disease	Relation	SNOMED_ID	DOID
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	VERQUVO	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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	MERCK SHARP DOHME	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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	VERQUVO	MERCK SHARP DOHME	N214377	Jan. 19, 2021	RX	TABLET	ORAL	Jan. 19, 2026	NEW CHEMICAL ENTITY
2.5MG	VERQUVO	MERCK SHARP DOHME	N214377	Jan. 19, 2021	RX	TABLET	ORAL	Jan. 19, 2026	NEW CHEMICAL ENTITY
5MG	VERQUVO	MERCK SHARP DOHME	N214377	Jan. 19, 2021	RX	TABLET	ORAL	Jan. 19, 2026	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Guanylate cyclase soluble subunit beta-1	Enzyme	Q02153	GCYB1_HUMAN	ACTIVATOR				DRUG LABEL	DRUG LABEL
Guanylate cyclase soluble subunit beta-1	Enzyme		GCYB1_RAT	ACTIVATOR	EC50	6		SCIENTIFIC LITERATURE

External reference:

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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5028	TABLET, FILM COATED	2.50 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5028	TABLET, FILM COATED	2.50 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5028	TABLET, FILM COATED	2.50 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5029	TABLET, FILM COATED	5 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5029	TABLET, FILM COATED	5 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5029	TABLET, FILM COATED	5 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5030	TABLET, FILM COATED	10 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5030	TABLET, FILM COATED	10 mg	ORAL	NDA	33 sections
VERQUVO	HUMAN PRESCRIPTION DRUG LABEL	1	0006-5030	TABLET, FILM COATED	10 mg	ORAL	NDA	33 sections