rezvilutamide + androgen deprivation therapy

Rezvilutamide is a second-generation, orally bioavailable androgen receptor (AR) antagonist developed by Jiangsu Hengrui Pharmaceuticals. It is specifically designed with low blood-brain barrier penetration to minimize central nervous system toxicities, such as seizures, which are sometimes associated with other AR inhibitors. In combination with androgen deprivation therapy (ADT), rezvilutamide provides a dual blockade of the androgen signaling axis by reducing circulating testosterone levels and competitively inhibiting the binding of remaining androgens to the AR. This combination was approved in China in June 2022 for the treatment of high-volume metastatic hormone-sensitive prostate cancer (mHSPC) based on the results of the Phase III CHART trial. Fudan University is currently leading a multicenter Phase II trial (MA-PCa-II-023) to evaluate the efficacy of this combination when integrated with radical prostatectomy and metastasis-directed radiotherapy for patients with newly diagnosed oligometastatic hormone-sensitive prostate cancer (OMPC).

Brand names

Airuika

Other names

rezvilutamide + ADT