Luxdegalutamide, also known as ARV-766, is an investigational oral androgen receptor (AR) degrader being developed by Arvinas for the treatment of metastatic castration-resistant prostate cancer (mCRPC).

[1][2] It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system.

[3] Luxdegalutamide is a second-generation PROTAC AR degrader that has demonstrated a broader efficacy profile and better tolerability compared to its predecessor, ARV-110, in clinical settings.

[3] It has shown promise in overcoming resistance associated with certain AR mutations, including the L702H mutation, which is prevalent in up to 24% of treated mCRPC patients.

[3] As of 2024, luxdegalutamide is being evaluated in phase I/II clinical trials for prostate cancer.