Luhan Pharmachem Co., Ltd.

Luhan Pharmachem Co., Ltd. supplies Riociguat bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Riociguat is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Riociguat?

Riociguat (BAY 63-2521, diagnosis trade name Adempas) is a novel drug (by Bayer) that is a stimulator of soluble guanylate cyclase (sGC). Clinical trials have looked at riociguat as a new approach to treat two forms of pulmonary hypertension(PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.

Mechanisms of Action

In healthy individuals nitric oxide (NO) acts as a signalling molecule on vascular smooth muscle cells to induce vasodilation. NO binds to soluble guanylate cyclase (sGC) and mediates the synthesis of the secondary messenger cyclic guanosine monophosphate (cGMP). sGC forms heterodimers consisting of a larger alpha-subunit and a smaller haem-binding beta-subunit. The synthesised cGMP acts as a secondary messenger and activates cGMP-dependent protein kinase (protein kinase G) to regulate cytosolic calcium ion concentration. This changes the actin–myosin contractility, which results in vasodilation. In patients with pulmonary arterial hypertension endothelial NO synthase, the enzyme that is responsible for the production of NO, is expressed to reduced levels. This results in overall lower levels of endothelial cell-derived NO and reduced vasodilation of smooth muscle cells. NO also reduces pulmonary smooth muscle cell growth and antagonises platelet inhibition, factors which play a key role in the pathogenesis of PAH. In contrast to NO- and haem-independent sGC activators like cinaciguat, the sGC stimulator riociguat directly stimulates sGC activity independent of NO and also acts in synergy with NO to produce anti-aggregatory, anti-proliferative, and vasodilatory effects.

Side Effects

Serious adverse effects in clinical trials included bleeding. Hypotension (low blood pressure), headache, and gastrointestinal disorders also occurred

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.