VERICIGUAT

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H16F2N8O2
Molecular Weight	426.3795
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC(=O)NC1=C(N)N=C(N=C1N)C2=NN(CC3=CC=CC=C3F)C4=NC=C(F)C=C24

InChI

InChIKey=QZFHIXARHDBPBY-UHFFFAOYSA-N

InChI=1S/C19H16F2N8O2/c1-31-19(30)25-14-15(22)26-17(27-16(14)23)13-11-6-10(20)7-24-18(11)29(28-13)8-9-4-2-3-5-12(9)21/h2-7H,8H2,1H3,(H,25,30)(H4,22,23,26,27)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28557445 | http://www.chemdiv.com/pivotal-phase-iii-study-started-vericiguat-patients-chronic-heart-failure/ | http://www.prnewswire.com/news-releases/data-on-vericiguat-investigational-heart-failure-medicine-to-be-presented-as-late-breaking-clinical-trial-at-the-2015-american-heart-association-aha-scientific-sessions-300174024.html

Vericiguat, discovered at Bayer, is the first soluble guanylate cyclase (sGC) stimulator. Vericiguat is currently being studied in a Phase III clinical program for the treatment of heart failure with reduced ejection fraction (HFrEF).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Soluble guanylate cyclase 34 Target ID: CHEMBL2111348 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28557445	Activator 1430		1005.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Heart Failure 7 Sources: https://clinicaltrials.gov/ct2/show/NCT02861534	Primary		Phase III 656	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.	2017 Jun 22	28557445

Patents

Sample Use Guides

In Vivo Use Guide

Starting dose of 2.5 mg taken orally once daily with food, on a background of standard of care. Dose will be uptitrated to 5 mg and to 10 mg.

Route of Administration: Oral

In Vitro Use Guide

Studies on the in vitro effects of Vericiguat on highly purified sGC (soluble guanylate cyclase) revealed that Vericiguat (0.01 uM to 100 uM) stimulates recombinant sGC concentration dependently, by 1.7-fold to 57.6-fold.

Name

Type

Language

VERICIGUAT

Official Name

English

METHYL N-(4,6-DIAMINO-2-(5-FLUORO-1-(2-FLUOROBENZYL)-1H-PYRAZOLO(3,4-B)PYRIDIN-3-YL)PYRIMIDIN-5-YL)CARBAMATE

Systematic Name

English

vericiguat [INN]

Common Name

English

METHYL (4,6-DIAMINO-2-(5-FLUORO-1-((2-FLUOROPHENYL)METHYL)-1H-PYRAZOLO(3,4-B)PYRIDIN-3-YL(PYRIMIDIN-5-YL)CARBAMATE

Systematic Name

English

METHYL (4,6-DIAMINO-2-(5-FLUORO-1-(2-FLUOROBENZYL)-1H-PYRAZOLO(3,4-B)PYRIDIN-3-YL)PYRIMIDIN-5-YL)CARBAMATE

Systematic Name

English

BAY-1021189

Code

English

VERICIGUAT [JAN]

Common Name

English

VERICIGUAT [ORANGE BOOK]

Common Name

English

VERQUVO

Brand Name

English

Vericiguat [WHO-DD]

Common Name

English

MK-1242

Code

English

VERICIGUAT [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29707