代谢
阿巴美替派的生物转化是广泛的,主要由CYP1A2介导。它首先被代谢成阿巴美替派羟基,然后再进一步代谢成阿巴美替派羧基 - 后者从血浆中清除较慢,导致比母药更高的系统浓度。体外研究表明,阿巴美替派羧基可能作为CYP3A4、CYP2B6和CYP1A2的抑制剂,特别是在阿巴美替派局部给药后观察到的相对较高和持续的浓度下。
The biotransformation of abametapir is extensive and primarily mediated by CYP1A2. It is metabolized first to abametapir hydroxyl and then further to abametapir carboxyl - the latter is cleared slowly from the plasma, resulting in higher systemic concentrations than that of the parent drug. _In vitro_ studies suggest that abametapir carboxyl may act as an inhibitor of CYP3A4, CYP2B6, and CYP1A2, particularly at the relatively high and prolonged concentrations observed following topical administration of abametapir.
来源:DrugBank