Riociguat

肺高压是一种进行性、致死性疾病,其特征是肺动脉压升高,导致血管重构、右心肥大和心衰。研究表明,肺高压与内源性血管扩张剂NO的产生受损有关。Riociguat是首个新一类可溶性鸟苷酸环化酶(sGC)激动剂,它直接刺激sGC,增强其对低水平NO的敏感度。目前应用本品对肺动脉高压(PAH)患者进行III期临床、对慢性血栓栓塞性肺高压(CTEPH)患者进行II期临床研究,表明疗效好,易耐受,不良反应轻微。

Pulmonary hypertension is a debilitating and fatal disease, which is characterized by elevated pulmonary arterial pressure causing vascular remodeling, right heart hypertrophy and heart failure, and is associated with impaired production of the endogenous vasodilator nitric oxide （NO）. Riociguat is the first-in-class drug of soluble guanylate cyclase （sGC） stimulators which, stimulates directly the sGC and increases its sensitivity to low NO levels. Recently, a phase III trial in pulmonary arterial hypertension （PAH） cases and phase II trials in chronic thromboembolic pulmonary hypertension （CTEPH） are underway. The drug shows good efficacy and is well tolerated with slight adverse reactions.