Haicrane Pharmaceuticals (688302.SH): Oral PROTAC drug HP518 tablets approved for clinical trials in combination with anticancer drugs for the treatment of advanced prostate cancer.

Hicin Pharmaceuticals (688302.SH) announced that the company has recently received the "Drug Clinical Trial Approval Notice" issued by the China National Medical Products Administration Drug Evaluation Center, approving the initiation of Phase Ib/II clinical trials of HP518 tablets, a combination antitumor drug, for the treatment of advanced prostate cancer. As of now, HP518 tablets have been approved for clinical trials in advanced prostate cancer in China, Australia, and the United States. There are currently no similar products approved for marketing domestically or internationally. HP518 is composed of a target protein ligand, an E3 ligase ligand, and a linker, which induces ubiquitination of AR and relies on proteasomal degradation of AR protein, thus achieving deep inhibition of the AR signaling pathway for antitumor purposes. It has typical advantages of PROTAC drugs, including catalytic activity, high selectivity, and good safety. As a new type of oral PROTAC drug, preclinical research results have shown that HP518 tablets have high degradation activity against resistant AR mutants and wild-type AR proteins, and exhibit excellent antitumor activity against AR-dependent prostate cancer cells. It is expected to overcome the issue of drug resistance caused by mutations in prostate cancer treatment and provide new treatment options for this group of patients.