B细胞淋巴瘤因子-2(BCL-2)抑制剂——Venetoclax

An inhibitor of B-cell lymphoma 2(BCL-2) —Venetoclax

Venclexta(venetoclax)是由艾伯维(Abb Vie)与罗氏(Roche)合作开发的第一个选择性B细胞淋巴瘤-2(BCL-2)抑制剂,FDA批准其用于治疗携带17p删除突变(del 17p)以及之前已接受至少一种疗法的慢性淋巴细胞白血病(CLL),其为del 17p患者群体提供了一个新的治疗方式。业界对其市场前景预期很高,其上市后已立即被纳入美国NCCN治疗指南。笔者就Venclexta的研发历程、基本性质、作用机制、药动学、药效学、临床试验及应用等研发动态作一概述,以期能为医院临床用药起到指导作用。

Venclexta （venetoclax） is a first-in-class BCL-2-selective inhibitor developed by AbbVie and Roche. FDA approved it for the treatment of patients with chronic lymphocytic leukemia （CLL） who have a chromosomal abnormality called 17p deletion and who have been treated with at least one prior therapy, which offers a new treatment modality for the del 17p patients. High expectations has been placed on Venclexta and it has also been incorporated into the US NCCN treatment guidelines immediately after coming to the market. The development, process, properties, mechanism, pharmacokinetics, pharmaco- dynamics, clinical trials and applictions of Venclexta were reviewed in this article.