Rezvilutamide (Ariane)

Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable androgen receptor (AR) antagonist with potential antineoplastic activity. Upon administration, rezvilutamide competitively binds to AR in target tissues, which both prevents androgen-induced receptor activation and facilitates the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of cell growth of AR-expressing tumor cells.

Diseases for which it is used

• Prostate cancer

History of changes in NMPA indication

• 2022-06-29: Approved for the treatment of patients with metastatic hormone-sensitive prostate cancer (mHSPC) with high tumour burden. (Based on CHART)

Also known as

• Code name: SHR-3680
• Brand name: Ariane