Riociguat

目录号: HY-14779

GPCR/G Protein-

Riociguat 是一种可口服的可溶性鸟苷酸环化酶(sGC) 刺激剂,常用于治疗肺动脉高压症。

Guanylate Cyclase

相关产品

Lificiguat-Linaclotide-Cinaciguat-BAY 41-2272-Vericiguat-

生物活性

Description

Riociguat is an oral stimulator of soluble guanylate cyclase (sGC), and used in the treatment of pulmonary hypertension.

In Vitro

Riocigua stimulates the recombinant sGC concentration dependently from 0.1 to 100?μM with a two-fold to 73-fold effect by an NO-independent but haem-dependent mechanism[1].?Riociguat inhibits platelet function in washed platelets but not in whole blood, and exerts no direct effects on contractility and relaxation of cardiac myocytes[2].

In Vivo

Riociguat (10 mg/kg/d, p.o.) partially reverses the pulmonary arterial hypertension, the right heart hypertrophy and the structural remodelling of the lung vasculature in chronic treatment of hypoxic mice and MCT-injected rats[1].

Clinical Trial

NCT02915835

Dinesh Khanna, MD, MS-Bayer-University of Michigan

Scleroderma-Digital Ulcers

September 2016

Phase 2

NCT02117791

Bayer

Hypertension, Pulmonary

July 16, 2014

NCT02024386

Richard Moon-Duke University

Hypertension, Pulmonary-Altitude Sickness

January 2014

Phase 4

NCT02633397

Gregory J. Kato, MD-University of Pittsburgh

Sickle Cell Disease

April 11, 2017

Phase 2

NCT02428985

Bayer

Hypertension, Pulmonary

June 29, 2015

NCT02744339

Medical University of Vienna

Hypertension, Pulmonary-Heart Failure With Normal Ejection Fraction

March 2016

Phase 2

NCT02007629

Bayer

Hypertension, Pulmonary

February 2014

Phase 3

NCT02634203

Assistance Publique - Hôpitaux de Paris-Bayer

Chronic Thromboembolic Pulmonary Hypertension

January 2016

NCT00855660

Bayer

Pharmacology, Clinical

March 2009

Phase 1

NCT02625558

University of Cincinnati

Sarcoidosis

April 2015

Phase 4

NCT02562235

Bayer-Merck Sharp & Dohme Corp.

Hypertension, Pulmonary

October 29, 2015

Phase 3

NCT01179334

Bayer

Pulmonary Hypertension

August 2010

Phase 2

NCT01165931

Bayer

Coronary Artery Disease

May 2012

Phase 2

NCT02283762

Bayer

Scleroderma, Systemic

January 15, 2015

Phase 2

NCT02138825

Bayer

Idiopathic Interstitial Pneumonias / Hypertension,Pulmonary

June 4, 2014

Phase 2

NCT02159326

Bayer

Drug Interactions

June 2014

Phase 1

NCT01065051

Bayer

Hypertension, Pulmonary-Ventricular Dysfunction, Left

November 2010

Phase 2

NCT02759419

Bayer

Hypertension, Pulmonary

June 16, 2016

Phase 4

NCT01784562

Bayer

Hypertension, Pulmonary

NCT02092818

Bayer

Hypertension, Pulmonary

May 31, 2014

NCT02891850

Bayer

Pulmonary Arterial Hypertension

January 12, 2017

Phase 4

NCT01065454

Bayer

Hypertension, Pulmonary-Ventricular Dysfunction, Left

April 14, 2010

Phase 2

NCT00640315

Bayer

Hypertension, Pulmonary-Pulmonary Disease, Chronic Obstructive

August 2008

Phase 1

NCT00855465

Bayer

Pulmonary Hypertension

February 2009

Phase 3

NCT02159313

Bayer

Healthy Volunteers

June 2014

Phase 1

NCT02545465

Bayer

Hypertension, Pulmonary

September 15, 2015

NCT01172756

Bayer

Hypertension, Pulmonary-Ventricular Dysfunction, Left

July 2010

Phase 2

NCT00810693

Bayer

Pulmonary Hypertension

December 2008

Phase 3

NCT02170025

Bayer-Merck Sharp & Dohme Corp.

Cystic Fibrosis

September 30, 2014

Phase 2

NCT00910429

Bayer

Pulmonary Hypertension

July 1, 2009

Phase 3

NCT00863681

Bayer

Hypertension, Pulmonary

March 12, 2009

Phase 3

NCT00694850

Bayer

Hypertension, Pulmonary

August 2, 2008

Phase 2

NCT01926847

Bayer

Raynaud Disease

October 2013

Phase 2

NCT00454558

Bayer

Hypertension, Pulmonary

January 2007

Phase 2

NCT00680654

Bayer

Hypertension, Pulmonary

October 2008

Phase 1

NCT02191137

Bayer

Hypertension, Pulmonary

September 2014

Phase 4

NCT02556268

Bayer

HIV-DDI

February 2016

Phase 1

NCT01489488

Bayer

Pharmacology, Clinical

January 2012

Phase 1

NCT03074539

Medical University of Vienna

Chronic Thromboembolic Pulmonary Hypertension-Sleep Disordered Breathing

February 1, 2017

View MoreCollapse

References

[1].Schermuly RT, et al. Expression and function of soluble guanylate cyclase in pulmonary arterial hypertension. Eur Respir J. 2008 Oct;32(4):881-91.

[2].Schermuly RT, et al. Riociguat for the treatment of pulmonary hypertension. Expert Opin Investig Drugs. 2011 Apr;20(4):567-76.

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