阿比特龙,生长发育编号CB-7598,也称之为17-(3-吡啶基)雄甾-5,16-二烯-3β-醇,是生成的甾类CYP17A1缓聚剂。 它是冰醋酸阿比特龙的活力新陈代谢产物,阿比特龙的酯和前药。已发觉阿比特龙的新陈代谢产物可做为雄激素蛋白激酶的抑制剂,并很有可能拮抗作用冰醋酸阿比特龙的临床医学功效。[1]。
冰醋酸阿比特龙(商品名Zytiga,Abiratas,Abretone,Abirapro)用以医治前列腺肿瘤。[2] [3]根据循环系统雄激素生长激素刺激前列腺肿瘤细胞生长发育和蔓延。该药品的预估功效是阻隔生理学和恶性肿瘤有关的雄激素(比如睾酮素)造成,以缓解或阻拦肿瘤细胞的蔓延。[4]因为该药品根据肾脏阻隔了类固醇的一切正常生理转化成,因而一般应用小剂量类固醇来防止肾脏作用不全。
除做为CYP17A1(17α-羟化酶/ 17,20-裂化酶)的不可逆缓聚剂外,阿比特龙还抑止3β-甲基类固醇脱氨酶(3β-HSD),类固醇11β-羟化酶(CYP11B1),5α-还原酶(根据新陈代谢产物) [5]和一些肝脏细胞黑色素P450酶(如CYP1A2,CYP2C9和CYP3A4)。[6]该药品是雄激素蛋白激酶的一部分抗剂,也是雌激素受体的抑制剂。[6] [7]
参照:
Δ4-
Abiraterone
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Capper CP, Larios JM, Sikora MJ, Johnson MD, Rae JM (May 2016). “The CYP17A1 inhibitor abiraterone exhibits estrogen receptor agonist activity in breast cancer”. Breast Cancer Research and Treatment. 157 (1): 23�C30. doi:10.1007/s10549-016-3774-3. PMID 27083183.