Hinova Pharmaceuticals Inc. recently announced that the U.S. Food and Drug Administration (FDA) has cleared the company's investigational new drug application (IND) for its innovative drug HP518, an oral chimeric degrader targeting androgen receptor (AR) for the treatment of metastatic castration-resistant prostate cancer (mCRPC). HP518 is currently in Phase I clinical trials in Australia. The open-label study approved by FDA will assess the safety, pharmacokinetics, and anti-tumor activity of HP518.

HP518 has been discovered and developed through Hinova's targeted protein degradation drug discovery platform. It has the potential to overcome the drug resistance of prostate cancer that is due to some specific AR mutations. AR is a validated therapeutic target to treat prostate cancer.

During the treatment of prostate cancer, drug resistance becomes inevitable due to multiple mechanisms, including AR amplification or mutations, etc. In preclinical studies, HP518 showed excellent selectivity and degradation activity against wild type AR and some specific AR mutants that are resistant to enzalutamide. HP518 also demonstrated excellent antitumor efficacy in xenograft mouse models.