Enzalutamide.

White or off-white non-hygroscopic crystalline solid with a melting point of 195-196 °C, soluble in DMSO and acetonitrile, slightly soluble in absolute ethanol, insoluble in water. Pharmacological effectsEnzalutamide (XTANDI, enzalutamide) is an oral androgen receptor antagonist, which is currently approved by clinical studies and the US FDA (Food and Drug Administration) for the treatment of metastatic castration-tolerant prostate cancer that has progressed after chemotherapy (i.e., prostate cancer patients whose tumors or cancer cells are still growing after chemotherapy), and can prolong the survival of patients. The incidence of prostate cancer in the United States is very high, with nearly 240,000 new patients per year (the highest among all cancers) and nearly 30,000 deaths per year (second only to lung cancer, breast cancer, and colorectal cancer), and the incidence rate in China is low. Enzalutamide is an androgen receptor inhibitor, the target of action is different from the cabazitaxel approved in 2010 and abiraterone approved in 2011, which can competitively inhibit the binding of androgens to the receptor, and can inhibit the nuclear transport of the androgen receptor and the interaction between the receptor and DNA. In the model experiment of mouse prostate cancer xenograft, enzalutamide can reduce the tumor volume, the main metabolite of enzalutamide is N-desmethylenzalutamide, which shows similar inhibitory activity to enzalutamide in vitro, the recommended adult dose of the drug is 160mg per day, rapid absorption after taking the drug, the plasma concentration reaches the highest level within 0.5~3h, the average terminal half-life is 5.8d, the main metabolic enzymes are CYP2C8 and CYP3A4, the drug should be avoided with strong CYP2C8 inhibitors ( eg, gemfibrozil) should be reduced to 80 mg once a day if co-administration is required.il