Blackledge G R, Cockshott I D, Furr B J
Medical Affairs, Zeneca Pharmaceuticals, Cheshire, UK.
Eur Urol. 1997;31 Suppl 2:30-9. doi: 10.1159/000474547.
Casodex (bicalutamide, Zeneca Ltd), has been developed for prostate cancer therapy. Its preclinical, pharmacokinetic, pharmacodynamic, clinical efficacy and tolerability data are described. Casodex is a potent and specific non-steroidal antiandrogen. Clinical studies indicated that Casodex is orally bioavailable and well absorbed, with a plasma half-life of around 1 week. A Casodex dose of 50 mg daily decreased prostatic acid phosphatase comparable with castration. This dose was, therefore, evaluated initially as monotherapy and later as a component of maximal androgen blockade. Using prostate specific antigen as an end point, Casodex 150 mg daily was well-tolerated with demonstrable evidence of activity. Casodex 150 mg monotherapy was less effective than castration in terms of efficacy in patients with metastatic disease at entry. However, in patients non-metastatic at entry, Casodex 150 mg monotherapy appeared to be equivalent to castration in terms of time to death (data immature). Casodex was well-tolerated. In combination treatment, Casodex at 50 mg daily was at least as effective as 750 mg flutamide (Eulexin, Schering-Plough International) with respect to time to treatment failure, equivalent in terms of survival, and better tolerated with respect to diarrhoea. In conclusion, Casodex is a good option for the antiandrogen component of maximal androgen blockade.
康士得（比卡鲁胺，阿斯利康有限公司）已被开发用于前列腺癌治疗。本文描述了其临床前、药代动力学、药效学、临床疗效和耐受性数据。康士得是一种强效且特异性的非甾体抗雄激素药物。临床研究表明，康士得口服生物利用度良好且吸收良好，血浆半衰期约为1周。每日50毫克的康士得剂量可使前列腺酸性磷酸酶降低程度与去势相当。因此，该剂量最初作为单一疗法进行评估，后来作为最大雄激素阻断疗法的一个组成部分进行评估。以前列腺特异性抗原为终点指标，每日150毫克的康士得耐受性良好，且有明显的活性证据。在入组时患有转移性疾病的患者中，就疗效而言，每日150毫克的康士得单一疗法不如去势有效。然而，在入组时无转移的患者中，就至死亡时间而言（数据未成熟），每日150毫克的康士得单一疗法似乎与去势相当。康士得耐受性良好。在联合治疗中，就至治疗失败时间而言，每日50毫克的康士得至少与750毫克氟他胺（福至尔，先灵葆雅国际公司）一样有效，在生存方面相当，且在腹泻方面耐受性更好。总之，康士得是最大雄激素阻断疗法中抗雄激素成分的一个良好选择。
