抗前列腺癌药恩杂鲁胺的研究进展

Research progress of anti-prostate cancer drug enzalutamide

前列腺癌是中老年男性常见的癌症之一,近年来抗前列腺癌药物成为药物研发的新热点.恩杂鲁胺是一种雄激素受体抑制剂,用于治疗去势难治性前列腺癌(Castration-resistant Prostate cancer,CRPC)患者且效果良好,逐渐成为治疗CRPC患者的新方案.它可以阻止二氢睾酮(Dihydrotestosterone,DHT)与雄激素受体结合,抑制前列腺癌细胞核和DNA结合.相比于第一代抗前列腺癌药物,恩杂鲁胺具有疗效更好、安全性更高、副作用更小等优点.因此,对恩杂鲁胺的药学研究具有重要意义.以"恩杂鲁胺""雄激素受体抑制剂""Enzalutamide""MDV3100"等为关键词,综合检索清华数据库、维普数据库、Pub Med、Sci Finder Scholar中有关恩杂鲁胺的研究文献,就其临床研究、合成研究、原料药的含量测定方法、药物多晶型及其剂型研究等方面进行了综述,并展望了今后的发展方向.

Prostate cancer is one of common cancers to the middle-aged and old male. The anti-prostate cancer drugs become the new hot spot for drug development in recent years. Enzalutamide is a kind of androgen receptor inhibitor in the use of treatment of patients with castration-resistant prostate cancer（CRPC）,and it has gradually become a new treatment for patients with CRPC because of its good effect. It can prevent the combination of dihydrotestosterone and androgen receptor,and inhibit the binding of prostate cancer cell nucleus and DNA. Compared with the first generation of anti-prostate cancer drugs,enzalutamide has many advantages such as better curative effect,higher safety and fewer side effect,etc. So it is essential to do some pharmaceutical research on enzalutamide. Using androgen receptor inhibitor,enzalutamide,MDV310 as keywords,we studied the relevant research literature of enzalutamide in databases of China National Knowledge Infrastructure,VIP,Pub Med,Sci Finder Scholar,and reviewed its researching status from clinical research,synthesis research,method for determination of APIs,drugs and dosage form polymorph research. Research prospects in this field were discussed.