阿比特龙,发育代号CB-7598,也称为17-(3-吡啶基)雄甾-5,16-二烯-3β-醇,是合成的甾体CYP17A1抑制剂。 它是醋酸阿比特龙的活性代谢产物,阿比特龙的酯和前药。
临床资料
已发现阿比特龙的代谢产物可作为雄激素受体的激动剂,并可能拮抗醋酸阿比特龙的临床疗效。[1]
醋酸阿比特龙
主要文章:醋酸阿比特龙
醋酸阿比特龙(商品名Zytiga,Abiratas,Abretone,Abirapro)用于治疗前列腺癌。[2] [3]通过循环雄激素激素刺激前列腺癌细胞生长和扩散。该药物的预期作用是阻断生理和肿瘤相关的雄激素(例如睾酮)产生,以减缓或阻止癌细胞的扩散。[4]由于该药物通过肾上腺阻断了类固醇的正常生理性生成,因此通常使用低剂量类固醇来预防肾上腺功能不全。
除作为CYP17A1(17α-羟化酶/ 17,20-裂解酶)的不可逆抑制剂外,阿比特龙还抑制3β-羟基类固醇脱氢酶(3β-HSD),类固醇11β-羟化酶(CYP11B1),5α-还原酶(通过代谢产物) [5]和某些肝细胞色素P450酶(如CYP1A2,CYP2C9和CYP3A4)。[6]该药物是雄激素受体的部分拮抗剂,也是雌激素受体的激动剂。[6] [7]
参考:
Δ4-Abiraterone
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