luxdegalutamide

Luxdegalutamide is an orally bioavailable, small molecule androgen receptor (AR) degrader developed using PROTAC (proteolysis targeting chimera) technology. It is designed to selectively degrade the androgen receptor by recruiting an E3 ubiquitin ligase, leading to ubiquitination and subsequent proteasomal degradation of the AR protein. This mechanism inhibits AR-mediated signaling pathways that drive tumor growth in prostate cancer, including castration-resistant and hormone-sensitive forms. Luxdegalutamide has demonstrated activity against both wild-type and clinically relevant mutant forms of the AR, such as L702H, H875Y, and T878A mutations—mutations often associated with resistance to standard antiandrogen therapies. The drug is being developed primarily for metastatic castration-resistant prostate cancer (mCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC). Clinical trials have shown promising efficacy with a favorable safety profile; most adverse events are mild or moderate in severity[1][4][5][6][7][8].

Other names

2750830-09-0