riociguat (adempas) Report issue

Small molecule Orphan Drug FDA Approved FDA First in Class
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
Riociguat is a potent, oral stimulator of soluble guanylate cyclase (sGC). It is the first member of a novel class of compounds, being developed by Bayer as an investigational, oral treatment to target a key molecular mechanism underlying pulmonary hypertension (PH). Riociguat demonstrated robust clinical efficacy in two separate PH indications: chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension(PAH). Riociguat works in two ways: it sensitizes sGC to endogenous NO by stabilizing the NO-sGC binding and directly stimulates sGC via a different binding site, independently of NO. Riociguat stimulates the NO-sGC-cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation. Through this unique way of working, riociguat decreases blood pressure within the pulmonary arteries that take blood from the heart to the lungs, reducing pressure on the heart leading to improved patient outcomes.   NCATS

Chemistry

  • SMILES: COC(=O)N(C)C1=C(N)N=C(N=C1N)C2=NN(CC3=CC=CC=C3F)C4=C2C=CC=N4
  • InChIKey: WXXSNCNJFUAIDG-UHFFFAOYSA-N
  • Mol. Mass: 422.4157
  • ALogP: 2.44
  • ChEMBL Molecule:
    riociguat  
More Chemistry

Pharmacology

Drug Pricing (per unit)

Australia

$31.7081

United States

$84.1722 - $119.9211
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

adempas | bay 63-2521 | bay-63-2521 | methyl n-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1h-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-n-methyl-carbaminate | riociguat | riociguatum

Organizations (24)

Research & Development (22)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (3)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (21)

Approved Indications (2)


 

Familial Primary Pulmonary Hypertension

Hypertension, Pulmonary

Experimental Indications - Clinical Trial Phases 1-4 (20)


 

Altitude Sickness (Phase 4)

Anemia, Sickle Cell (Phase 2)

Coronary Artery Disease (Phase 2)

Cystic Fibrosis (Phase 2)

Drug Interactions (Phase 1)

General Surgery (Phase 2)

Healthy Volunteers (Phase 1)

Heart Failure, Diastolic (Phase 2)

HIV Infections (Phase 1)

Hypertension, Pulmonary ()

Pharmacology, Clinical (Phase 1)

Pneumonia (Phase 2)

Pulmonary Arterial Hypertension (Phase 4)

Pulmonary Disease, Chronic Obstructive (Phase 1)

Raynaud Disease (Phase 2)

Sarcoidosis (Phase 4)

Scleroderma, Systemic (Phase 2)

Thromboembolism (Phase 2)

Ulcer (Phase 2)

Ventricular Dysfunction, Left (Phase 2)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 50
  • # of Trial Organizations: 22

Trials by Phase

Trial Phase Start Date Organizations Indications

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