别名 细胞色素P450家族51、CP51、CYP51 + [15] |
简介 Sterol 14alpha-demethylase that plays a critical role in the cholesterol biosynthesis pathway, being cholesterol the major sterol component in mammalian membranes as well as a precursor for bile acid and steroid hormone synthesis (PubMed:8619637, PubMed:9559662, PubMed:20149798). Cytochrome P450 monooxygenase that catalyzes the three-step oxidative removal of the 14alpha-methyl group (C-32) of sterols such as lanosterol (lanosta-8,24-dien-3beta-ol) and 24,25-dihydrolanosterol (DHL) in the form of formate, and converts the sterols to 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol and 4,4-dimethyl-8,14-cholestadien-3beta-ol, respectively, which are intermediates of cholesterol biosynthesis (PubMed:8619637, PubMed:9559662, PubMed:20149798). Can also demethylate susbtrates not intrinsic to mammals, such as eburicol (24-methylene-24,25-dihydrolanosterol), but at a lower rate than DHL (PubMed:9559662). |
靶点 |
作用机制 CYP51A1抑制剂 |
原研机构 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批国家/地区 日本 |
首次获批日期2018-01-19 |
作用机制 CYP51A1抑制剂 [+1] |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批国家/地区 巴西 |
首次获批日期2016-08-22 |
作用机制 30S subunit抑制剂 [+2] |
在研适应症 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批国家/地区 中国 |
首次获批日期2010-09-23 |
开始日期2024-10-04 |
申办/合作机构 |
开始日期2024-08-26 |
申办/合作机构 |
开始日期2024-07-03 |
申办/合作机构 |