Hinova Pharmaceuticals Inc., a clinical-stage biopharmaceutical company focused on developing novel therapeutics for cancers and metabolic diseases through targeted protein degradation technologies, announced that the first patient with metastatic castration-resistant prostate cancer (mCRPC) has been successfully dosed in a Phase I clinical trial of HP518, a highly selective and orally bioavailable chimeric degrader targeting androgen receptor (AR). The ongoing open-label Phase I study in Australia will evaluate the safety, pharmacokinetics, and anti-tumor activity of HP518 in patients with mCRPC.
HP518 has been discovered and developed by Hinova’s targeted protein degradation drug discovery platform. It has the potential to overcome the drug resistance of prostate cancer due to some specific AR mutations.
Chimeric degraders are bifunctional small molecules that promote degradation of target proteins with high potency and high selectivity. This technology has the potential to target non-druggable targets and to overcome the drug resistance issue of traditional small molecule drugs.
“This is a significant milestone in the progress of our efforts from drug discovery to the clinical study,” said Yuanwei Chen, Ph.D., President and CEO of Hinova. “We are excited about it and dedicated to bringing new treatment options to patients worldwide!”
Through the targeted protein degradation drug discovery platform, Hinova can screen protein degradation activity rapidly and accomplish efficient design and optimization of chimeric degraders. Furthermore, Hinova has profound experience in chemical manufacturing control of Chimeric degrader compounds.
In 2019, the number of new cases of prostate cancer worldwide reached 1.3 million. AR is a validated therapeutic target to treat prostate cancer. HP518, is an orally bioavailable chimeric degrader targeting AR, with the potential to overcome the drug resistance of prostate cancer due to some specific AR mutations. In discovery and preclinical studies, HP518 showed high degradation activity against wild type AR and some specific AR mutants that are resistant to enzalutamide, and excellent antitumor activity in xenograft mouse models. HP518 is highly selective for AR.
Hinova is an international and clinical-stage biopharmaceutical company focused on developing novel therapeutics for cancers and metabolic diseases. Hinova has committed to the discovery and development of innovative medicines for patients globally through deuteration and targeted protein degradation technologies.
Source: Hinova Pharmaceuticals Inc.