luxdegalutamide + abiraterone

This drug is a **combination of luxdegalutamide (JSB462, ARV-766)** and **abiraterone**. Luxdegalutamide is an oral proteolysis targeting chimera (PROTAC) that causes targeted degradation of the androgen receptor (AR), including wild-type and certain clinically relevant AR mutants (such as T878, H875, and L702H). Its mechanism involves recruiting the cellular ubiquitin-proteasome system to degrade the AR protein, going beyond standard AR antagonists by removing the receptor protein from the cell. Abiraterone is an inhibitor of CYP17A1, an enzyme required for androgen biosynthesis, thereby strongly suppressing androgen production. The combination is under evaluation for metastatic hormone-sensitive prostate cancer (mHSPC), with the hypothesis that AR protein degradation by luxdegalutamide will synergize with androgen production suppression by abiraterone, especially in patients prone to resistance to standard AR-directed therapies. The combination is being studied in Phase II trials, primarily to determine safety, tolerability, and efficacy, along with the optimal combination dose for future development[1][2][3][5][7][9].

Brand names

Zytiga

Other names

JSB462 + abirateroneARV-766 + abiraterone