摘要
肺动脉高压是一种进行性疾病,病因复杂,患者的生存率较低。目前,能使临床获益的药物比较有限。利奥西呱(Riociguat商品名:Adempas)是拜耳公司开发上市的首个新一类可溶性鸟苷酸环化酶(s GC)激动剂,具有双重作用机制,它可以增强s GC对内源性NO的敏感性,且不依赖于NO,通过其他的结合位点直接激活s GC。2013年10月,美国FDA批准Riociguat用于治疗持续性/复发性或慢性不能手术治疗的栓塞性肺动脉高压(CTEPH)和成人肺动脉高压(PAH)。本文对其作用机制、药效学、药动学、临床评价以及安全性等做一综述。
Pulmonary arterial hypertension （PAH） is a severe, progressive and often fatal disease for which only a limited number of drugs have proven to be of clinical benefit. Bayer has developed and launched rio- ciguat （Adempas） , which is the first stimulator of soluble guanylate cyclase （sGC）. Riociguat has a dual mode of action. It sensitizes sGC to endogenous NO by stabilizing the NO-sGC binding. Riociguat also directly stimulates sGC via a different binding site independently of NO. In October 2013, riociguat has been approved in the US for the treatment of chronic thromboembolic pulmonary hypertension （CTEPH） and for pulmonary arterial hypertension （PAH）. The mechanism, pharmacokinetics, pharmacodynamics, clinical evaluations and safety were reviewed in this paper.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2015年第1期1-4,共4页
Chinese Journal of New Drugs
