On October 28, 2022 Hinova Pharmaceuticals Inc. (STAR: 688302), a clinical-stage biopharmaceutical company focused on developing novel therapeutics for cancers and metabolic diseases through targeted protein degradation technologies, reported their preclinical results of HP518, an orally bioavailable chimeric degrader targeting androgen receptor (AR) for prostate cancer treatment, at the 5th Annual TPD Summit (Press release, Hinova Pharmaceuticals, OCT 28, 2022, View Source [SID1234622587]).
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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).
"Existing data makes us more confident that HP518 has the potential to be an innovative clinical option to patients with mCRPC," said Xinghai Li, MD/Ph.D., Chief Science Officer of Hinova, "Considering prostate cancer is a progressive disease, we have established a strong pipeline targeting the androgen receptor pathway for prostate cancer treatment. Based on our targeted protein degradation drug discovery platform, we are committed to develop best-in-class and first-in-class medicines to address unmet medical needs."
Hinova has established a targeted protein degradation drug discovery platform, which allows Hinova to integrate TPD biology and medicinal chemistry and to identify and optimize chimeric degraders with high efficiency. Furthermore, Hinova has accumulated much experience in development of Chimeric degrader.