Hinova Pharmaceuticals Inc. presented their preclinical results of HP518, an orally bioavailable chimeric degrader targeting androgen receptor (AR) for prostate cancer treatment, at the 5th Annual TPD Summit. Discovered and developed by Hinova, HP518 showed high degradation activity against fl-AR and most enzalutamide resistant AR point mutants, and demonstrated excellent antiproliferation activities against prostate cancer cell lines. Meanwhile, HP518 exhibited good metabolic stability and is stable in human plasma.

HP518 showed excellent antitumor efficacy in xenograft model by oral dosing. HP518 was also well tolerated in preclinical tox studies. HP518 is currently in Phase-I clinical trials in Australia.

The ongoing open-label clinical study will evaluate the safety, pharmacokinetics, and anti-tumor activity of HP518 in patients with metastatic castration-resistant prostate cancer (mCRPC).