Boissier Emilie, Loriot Yohann, Vignot Stéphane, Massard Christophe
Institut Gustave-Roussy, DITEP, Département d'innovations thérapeutiques et essais précoces, 114, rue Édouard-Vaillant, 94805 Villejuif cedex, France.
Institut Gustave-Roussy, Département de médecine oncologique, 114, rue Édouard-Vaillant, 94805 Villejuif cedex, France.
Bull Cancer. 2014 Apr;101(4):388-93. doi: 10.1684/bdc.2014.1932.
Abiraterone acetate (AA) is a selective inhibitor of cytochrom p450 (CYP)17 which is required for androgen biosynthesis, and can block the androgens synthesis by testicles, surrenals and intratumoral secretion. In phase I and II studies in patients with prostate cancer, therapy with AA 250-2000 mg once daily demonstrated reductions in prostate specific antigen (PSA), and/or circulating tumor cells (CTCs). In two large phase III trials in patients with metastatic castration resistant prostate cancer (CRPC) in post-docetaxel and pre-docetaxel setting, AA plus prednisone compared with placebo plus prednisone demonstrated a significant superior overall survival in post-docetaxel setting, and a superior radiological PFS in pre-docetaxel setting. Based of these results, AA is approved in metastatic CRPC patients in post-docetaxel setting or pre-docetaxel setting in 2013.
醋酸阿比特龙（AA）是细胞色素P450（CYP）17的选择性抑制剂，雄激素生物合成需要该酶，它能够阻断睾丸、肾上腺和肿瘤内分泌产生的雄激素合成。在前列腺癌患者的I期和II期研究中，每日一次服用250 - 2000毫克AA进行治疗可使前列腺特异性抗原（PSA）和/或循环肿瘤细胞（CTC）减少。在两项针对转移性去势抵抗性前列腺癌（CRPC）患者的大型III期试验中，一项是在多西他赛治疗后进行，另一项是在多西他赛治疗前进行，结果显示，与安慰剂加泼尼松相比，AA加泼尼松在多西他赛治疗后组显著提高了总生存期，在多西他赛治疗前组显著提高了影像学无进展生存期（PFS）。基于这些结果，2013年AA被批准用于多西他赛治疗后或治疗前的转移性CRPC患者。
