比卡鲁胺

目的观察比卡鲁胺（bicalutamide，康士得，casodex）治疗激素抵抗性前列腺癌（HRPC）的疗效。

Objective To evaluate the efficacy of bicalutamide ( casodex ) in the treatment of hormone-refractory prostate cancer .

比卡鲁胺片在健康人体内的药物动力学及生物等效性评价

Assessment of pharmacokinetics and bioequivalence of bicalutamide tablets in healthy volunteers

睾酮和比卡鲁胺对雄激素依赖性前列腺癌细胞株LNcap-FCG生长的影响

Effects of testosterone and androgen blocker bicalutamide on the cell growth of androgen-dependent prostate cancer cell line LNcap-FCG

采用气相色谱法测定比卡鲁胺原料药中有机溶剂残留量。

The residual solvents in bicalutamide substance were determined by GC .

目的：对自制比卡鲁胺的化学结构进行确证。

Objective : To identify the structure of bicalutamide .

比卡鲁胺治疗进展期前列腺癌52例

Bicalutamide in the treatment of advanced prostate cancer : a 52 case report

比卡鲁胺是非甾体雄激素拮抗剂，用于治疗前列腺癌和良性前列腺肥大。

The nonsteroidal antiandrogen bicalutamide was used to treat prostate cancer , benign prostatic hypertrophy or hyperplasia .

前列腺癌是男性生殖泌尿系统中常见的恶性肿瘤，比卡鲁胺是治疗前列腺癌的重要药物之一。

Prostate cancer is common malignant tumor of male reproductive urinary system . Bicalutamide is one kind of important drug for treating prostate cancer .

方法：以3-三氟甲基-4-氰基苯胺和2-甲基丙烯酰氯为起始原料经过酰化、环氧化、取代和氧化四步反应合成比卡鲁胺。

Methods : Bicalutamide was prepared from 4-cyano-3 - ( trifluoromethyl ) aniline and 2-methylacryloyl chloride by four steps : acylation , cyclization , substitution , and oxidization .

在体内比卡鲁胺主要有3种代谢途径，包括：羟基化、酰胺键水解、葡萄糖醛酸结合，这些代谢途径还可能发生交叉，生成次级代谢产物。

The major metabolic pathways of bicalutamide in vivo were hydroxylation 、 hydrolysis at the amide and glucuronide conjugation . Secondary metabolism via these pathways was also evidenced . 3 .

结论：血清游离前列腺特异抗原等可作为判断前列腺癌内分泌治疗效果的标准，比卡鲁胺治疗晚期前列腺癌有较好疗效。

Conclusion Serum prostate specific antigen and free prostate specific antigen evaluation is useful in prostate cancer patients undergoing hormonal therapy . Bicalutamide therapy is effective for advanced prostate cancer patients .

并概述了分别以溴丙酮、2-甲基丙烯酰氯、2-甲基丙烯酸甲酯、2,3-二羟基-2-甲基丙酸以及丙酮酸或丙酮酸酯为起始原料合成比卡鲁胺的方法。

The different methods for synthesizing bicalutamide using bromoacetone , 2-methyl acryloyl chloride , 2-methyl methacrylate , 2,3-dihydroxy-2-methyl propanoic acid , pyruvic acid or pyruvate as raw materials were summarized respectively .

比卡鲁胺是一种新型的非甾体类抗雄激素药物，临床上是与促黄体（生成）激素释放激素类似物合用或配合阉割手术，用于晚期前列腺癌的治疗。

Bicalutamide is a nonsteroidal pure antiandrogen . It is used at a dosage of 50 mg once daily in combination with a luteinizing hormone-releasing hormone analogue or surgical castration for the treatement of advanced prostate cancer .

为此建议严重肝功能损害患者禁用氟他胺和比卡鲁胺，对肝功能不全或有肝病史患者应慎用或权衡利弊，其他患者用药过程中应定期监测肝功能，至少每月1次。

It is suggested that patients with severe liver damage should not take flutamide and bicalutamide and that individuals with poor liver function or hepatitis history take them cautiously while examined for LFT , once a month at least .