FG-3246 + enzalutamide

FG-3246 + enzalutamide is an investigational combination therapy being evaluated for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The combination pairs FG-3246 (also known as FOR46), a first-in-class antibody-drug conjugate (ADC) targeting CD46, with enzalutamide, an oral second-generation androgen receptor pathway inhibitor. FG-3246 comprises a fully human anti-CD46 monoclonal antibody (YS-5) conjugated to the microtubule-disrupting payload monomethyl auristatin E (MMAE) via a cleavable valine-citrulline linker. Enzalutamide works by inhibiting androgen binding to the androgen receptor, nuclear translocation, and DNA binding. In preclinical models, androgen receptor blockade with enzalutamide upregulates CD46 expression, thereby enhancing the anti-tumor activity of FG-3246. The combination is being evaluated in a Phase 1b/2 investigator-sponsored trial led by the University of California, San Francisco (UCSF) in patients with mCRPC who have progressed on prior androgen receptor pathway inhibitors.

Other names

FG-3246 plus enzalutamideFG3246 plus enzalutamideFG 3246 plus enzalutamideFOR46 + enzalutamideFOR46 plus enzalutamideFOR-46 plus enzalutamideFOR 46 plus enzalutamide