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Concept: Riociguat

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The nitric oxide (NO)-soluble guanylate cyclase (sGC)-cyclic guanosine monophosphate (cGMP) signal-transduction pathway is impaired in many cardiovascular diseases, including pulmonary arterial hypertension (PAH). Riociguat (BAY 63-2521) is a stimulator of sGC that works both in synergy with and independently of NO to increase levels of cGMP. The aims of this study were to investigate the role of NO-sGC-cGMP signaling in a model of severe PAH and to evaluate the effects of sGC stimulation by riociguat and PDE5 inhibition by sildenafil on pulmonary hemodynamics and vascular remodeling in severe experimental PAH.

Concepts: Pulmonology, Myocardial infarction, Pulmonary artery, Nitric oxide, Pulmonary hypertension, Guanylate cyclase, Sildenafil, Riociguat

137

A proportion of patients with pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH) do not achieve treatment goals or experience side effects on their current therapy. In such cases, switching patients to a new drug while discontinuing the first may be a viable and appropriate treatment option. CAPTURE was designed to investigate how physicians manage the switching of patients to riociguat in real-world clinical practice. Observations from the study were used to assess whether recommendations in the riociguat prescribing information are reflected in clinical practice.

Concepts: Medicine, Pulmonology, Cardiology, Blood pressure, Pulmonary artery, Pharmaceutical industry, Pulmonary hypertension, Riociguat

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Riociguat, a member of a new class of compounds (soluble guanylate cyclase stimulators), has been shown in previous clinical studies to be beneficial in the treatment of chronic thromboembolic pulmonary hypertension.

Concepts: Clinical trial, Pulmonary artery, Nitric oxide, Pulmonary hypertension, Member of Parliament, Guanylate cyclase, Riociguat

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Following positive results from the Phase III CHEST-1 study in patients with inoperable or persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH), the Phase IIIb CTEPH early access study (EAS) was designed to assess the safety and tolerability of riociguat in real-world clinical practice, as well as to provide patients with early access to riociguat before launch. Riociguat is approved for the treatment of inoperable and persistent/recurrent CTEPH.

Concepts: Clinical trial, Pulmonology, Pulmonary artery, Pulmonary hypertension, Riociguat

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Riociguat was well tolerated and improved exercise and functional capacity in patients with pulmonary arterial hypertension (PAH) and inoperable chronic thromboembolic pulmonary hypertension (CTEPH) in a 12-week Phase II trial. We present final data from the long-term extension phase of this study.

Concepts: Clinical trial, Pulmonology, Cardiology, Blood pressure, Pulmonary artery, Pulmonary hypertension, Iloprost, Riociguat

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Riociguat, the first approved drug for patients with chronic thromboembolic pulmonary hypertension (CTEPH), is a soluble guanylate cyclase (sGC) Stimulator. It directly stimulates sGC independently of nitric oxide (NO) and increases sGC sensitivity for NO. The safety and efficacy of transitioning from a phosphodiesterase 5 inhibitor (PDE5i) to riociguat is unknown.

Concepts: Pulmonology, Pulmonary artery, Nitric oxide, Pulmonary hypertension, Nitric acid, Guanylate cyclase, Sildenafil, Riociguat

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We compared the haemodynamic effects of riociguat in patients with inoperable chronic thromboembolic pulmonary hypertension (CTEPH) or persistent/recurrent CTEPH after pulmonary endarterectomy in the Chronic Thromboembolic Pulmonary Hypertension Soluble Guanylate Cyclase-Stimulator Trial 1 study.

Concepts: Pulmonology, The Chronic, Pulmonary artery, Pulmonary hypertension, Endarterectomy, Riociguat

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Riociguat is a soluble guanylate cyclase stimulator approved for pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH). The objective of this study was to evaluate the change of right heart size and function assessed by echocardiography during long-term treatment with riociguat.

Concepts: Pulmonology, Cardiology, Heart, Pulmonary artery, Nitric oxide, Pulmonary hypertension, Guanylate cyclase, Riociguat

0

Background: Riociguat (BAY 63-2521) is an oral NO-independent as well as NO-synergistic stimulator of soluble guanylate cyclase (sGC) for the treatment of pulmonary hypertension. BAY 60-4552 (M-1) is its pharmacologically active major metabolite. An isotope dilution LC-ESI-MS/MS method has been developed and validated for the simultaneous determination of riociguat and M-1 in lithium heparinized human plasma. Results: The validated concentration range covers 0.500 μg/l (LLOQ) to 100 μg/l (ULOQ) for both analytes. Interassay accuracy and precision (%CV) for both analytes ranged from 92.7 to 111% and from 2.61 to 9.89%, respectively. Conclusion: The method proved to be selective, specific, sufficiently sensitive, highly reproducible and robust for the analysis of large numbers of samples.

Concepts: Pharmacology, Pulmonary hypertension, Accuracy and precision, Guanylate cyclase, Riociguat

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