5-isothiocyanato-3-(trifluoromethyl)picolinonitrile is one of key intermediates of apalutamide (N-1).

Function of Apalutamide

As a second-generation nonsteroidal androgen receptor inhibitory drug, apalutamide can prevent the fusion of androgen and receptors, and block the transfer of AR to the nucleus of cancer cells. In addition, apalutamide can also control androgen and promote the growth of cancer cells.

The safety and efficacy of apalutamide are based on a randomized clinical trial of 1,207 patients with non-metastatic, castration-resistant prostate cancer. Patients in the trial received apalutamide or placebo. All patients also received hormone therapy, either with a gonadotropin-releasing hormone (GnRH) analog, or with surgery to lower the amount of testosterone in the body (surgical castration). Median metastasis-free survival was 40.5 months for patients taking apalutamide, compared with 16.2 months for patients taking placebo. From the above experiments, we can see that the effect of apalutamide in the treatment of prostate cancer is very significant.