Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer[1][2].
[1] Snyder L, et al. In vitro evaluation of PROTAC degrader ARV-766 for cytochrome P450-and transporter-mediated drug-drug interaction[J]. Drug Metabolism and Pharmacokinetics, 2024, 55: 100881.
[2] Snyder L, et al. Abstract ND03: Discovery of ARV-766, an androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer[J]. Cancer Research, 2023, 83(7_Supplement): ND03-ND03.
