摘要
吡非尼酮是正在开发中的新型抗纤维化药物,具有广谱的抗肺、肝、肾、心和腹膜纤维化作用,其作用机制包括:抑制脂质过氧化,减少转化生长因子β(TGF-β)、血小板源性的生长因子(PDGF)和肿瘤坏死因子α(TNF-α)的生成,从而减轻炎症反应。和目前常用的抗纤维药物相比,本品不良反应较低。现对其药动学、药理作用、临床试验、作用机制和不良反应进行综述。
Pirfenidone is an orally active pyridine derivative that is under Phase Ⅲ clinical studies as orphan drug designation by US FDA for the treatment of idiopathic pulmonary fibrosis （IPF）. In vitro evidence has shown that pirfenidone may inhibit collagen synthesis, block fibroblast proliferation and stimulation in response to cytokines, and down-regulate production of multiple cytokines, including inhibition of transforming growth factor-beta （TGF-beta）, tumor necrosis factor-alpha （TNF-alpha） and platelet derived growth factor （PDGF）. Pirfenidone has demonstrated activity in multiple fibrotic conditions, including those of the lung, liver, kidney, heart and peritoneum. In the clinical experiences, pirfenidone has generally well tolerated with the most frequent side effects reported being photosensitivity rash and gastrointestinal symptoms. This review presents the pharmacokinetics, pharmacological mechanism, clinical efficacy and safety profiles.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2005年第8期1070-1073,共4页
Chinese Journal of New Drugs
