ridaforolimus + bicalutamide

Ridaforolimus + bicalutamide is an investigational oral combination therapy targeting prostate cancer by inhibiting two critical oncogenic pathways: the mammalian target of rapamycin (mTOR) pathway, via ridaforolimus (a non-prodrug analog of rapamycin), and the androgen receptor (AR) signaling pathway, via bicalutamide (a non-steroidal antiandrogen). The combination aims to overcome tumor resistance that emerges with monotherapy by synergistically arresting cell cycle progression in the G1 phase and suppressing tumor proliferation, particularly in models with PTEN deficiency and elevated AKT/mTOR activity. Preclinical studies and limited early-phase clinical settings have demonstrated synergistic antiproliferative and antitumor effects with notable reductions in PSA levels, but also revealed significant dose-limiting toxicities (e.g., stomatitis, hyperglycemia) that have challenged tolerability in clinical contexts for metastatic castration-resistant prostate cancer[1][2][3][4].

Other names

ridaforolimus and bicalutamide combination