Enzalutamide CAS NO.915087-33-1

Xtandi and enzalutamide are oral androgen like receptor antagonists. Currently, they have been approved by clinical research and FDA (food and Drug Administration) for the treatment of metastatic castration tolerant prostate cancer after chemotherapy (i.e. patients with prostate cancer whose tumor or cancer cells are still growing after chemotherapy), which can prolong the survival of patients. The incidence rate of incidence of prostate cancer in the United States is very high. Nearly 240 thousand patients (the highest in all cancers) are newly added each year, and nearly 30 thousand deaths occur each year (second only to lung, breast and colorectal cancer). China has a low incidence rate. Enzalutamide is an androgen receptor inhibitor. Its target is different from cabataxel approved in 2010 and abiraterone approved in 2011. It can competitively inhibit the binding of androgen and receptor, and inhibit the nuclear transport of androgen chemobook receptor and the interaction between androgen receptor and DNA. In vitro experiments show that enzalutamide can inhibit prostate cancer cells The main metabolite of enzalutamide is n-demethylenzalutamide, which has similar inhibitory activity in vitro as enzalutamide. The recommended adult dose of enzalutamide is 160 mg per day, which can be absorbed rapidly after administration, and the plasma concentration reaches the highest level within 0.5-3 H, The average terminal half-life was 5.8 days, and the main metabolic enzymes were cyp2c8 and CYP3A4. The drug should not be used in combination with strong cyp2c8 inhibitors (such as gemfibrozil, gemfibrozil). If co administration is needed, the dose of enzalutamide should be reduced to 80 mg, once a day.

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