[關(guān)鍵詞]
[摘要]
肺高壓是一種進(jìn)行性、致死性疾病,其特征是肺動(dòng)脈壓升高,導(dǎo)致血管重構(gòu)、右心肥大和心衰。研究表明,肺高壓與內(nèi)源性血管擴(kuò)張劑NO的產(chǎn)生受損有關(guān)。Riociguat是首個(gè)新一類(lèi)可溶性鳥(niǎo)苷酸環(huán)化酶(sGC)激動(dòng)劑,它直接刺激sGC,增強(qiáng)其對(duì)低水平NO的敏感度。目前應(yīng)用本品對(duì)肺動(dòng)脈高壓(PAH)患者進(jìn)行III期臨床、對(duì)慢性血栓栓塞性肺高壓(CTEPH)患者進(jìn)行II期臨床研究,表明療效好,易耐受,不良反應(yīng)輕微。
[Key word]
[Abstract]
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.
[中圖分類(lèi)號(hào)]
[基金項(xiàng)目]