Hinova Pharmaceuticals has dosed the first subject in a Phase I clinical trial of its oral therapy HP518 to treat metastatic castration-resistant prostate cancer (mCRPC).
The open-label study, which is underway in Australia, will evaluate the orally bioavailable chimeric degrader targeting androgen receptor (AR) HP518’s pharmacokinetics, safety and anti-tumour activity in mCRPC patients.
Hinova’s targeted protein degradation drug discovery platform discovered and developed the therapy.
HP518 showed high degradation activity against wild type AR and certain AR mutants in discovery and preclinical studies.
It also demonstrated antitumour activity in xenograft mouse models.
Furthermore, HP518 is intended to overcome the drug resistance of prostate cancer due to specific AR mutations.
Hinova Pharmaceuticals president and CEO Yuanwei Chen said: “The dosing of the first patient is a significant milestone in the progress of our efforts from drug discovery to the clinical study.
“We are excited about it and dedicated to bringing new treatment options to patients worldwide, and will continue to tirelessly advance our ongoing targeted protein degradation projects.”
HP518 is highly selective for AR, a therapeutic target validated for prostate cancer treatment.
The bifunctional small molecules, chimeric degraders, can promote target proteins degradation with high potency and selectivity.
Hinova focuses on the development of new treatments for cancers and metabolic diseases through targeted protein degradation technologies.
A targeted protein degradation drug discovery platform, established by Hinova, allows rapid screening of protein degradation activity and accomplish design and optimisation of Chimeric degraders.
The company also has experience in chemical manufacturing control of chimeric degrader compounds.