proxalutamide

Proxalutamide is a nonsteroidal antiandrogen (NSAA) and a selective high-affinity silent antagonist of the androgen receptor (AR). It acts by binding to the AR in target tissues, inhibiting androgen-induced receptor activation, and promoting the formation of inactive complexes that cannot translocate to the nucleus. This prevents transcription of AR-responsive genes involved in cell proliferation, particularly in prostate cancer. Proxalutamide also induces downregulation of AR expression, further suppressing AR-mediated signaling. The drug is orally bioavailable and has been investigated for its antineoplastic activity against metastatic castration-resistant prostate cancer (mCRPC), as well as for potential use in COVID-19 and breast cancer. It was developed by Suzhou Kintor Pharmaceuticals, a subsidiary of Kintor Pharmaceutical Limited. Proxalutamide was approved for COVID-19 treatment in Paraguay but remains investigational elsewhere[1][2][3][4].

Other names

pruxelutamide1398046-21-3