HaiChuang Pharma Announces First-in-Human Dosing of HP518, China's First Oral AR-Targeting PROTAC Drug, in Phase I Clinical Trial in Australia
On January 19, 2022 (Melbourne time), HP518, an oral PROTAC drug targeting the androgen receptor (AR) developed by Haichuang Pharmaceutical, achieved first-in-human (FIH) dosing in its Phase I clinical trial in Australia.
HP518 is an orally administered PROTAC drug independently developed by HaiChuang Pharma, which can highly selectively target and degrade the androgen receptor (AR), holding potential for the treatment of resistant prostate cancer.
The Phase I clinical trial of HP518 currently being conducted in Australia is an open-label study designed to evaluate the safety, pharmacokinetics, and antitumor activity of HP518 in patients with metastatic castration-resistant prostate cancer (mCRPC).
Dr. Chen Yuanwei, Founder and Chairman of Haichuang Pharmaceutical, stated, “We have made in-depth investments in PROTAC technology and accumulated extensive R&D experience. The administration of the first dose to a patient marks a significant milestone for our company in this field. We will actively advance our ongoing PROTAC projects to provide cutting-edge, high-quality innovative medicines to patients worldwide!”
HaiChuang Pharma began its exploration in the PROTAC field as early as 2016 and has since established a “PROTAC Targeted Protein Degradation Technology Platform.” This platform enables rapid assessment of compounds’ protein degradation activity, efficient PROTAC molecular design, druggability screening, and optimization. The company also possesses extensive expertise in the CMC (Chemistry, Manufacturing, and Controls) of PROTAC compounds.
Prostate cancer is an epithelial malignant tumor arising in the prostate gland. It is the most common malignancy of the male genitourinary system and predominantly affects individuals aged 65 years and older. Prostate cancer is one of the most common malignancies worldwide. In the United States, it has long ranked first in incidence and second in mortality among male cancers. In China, prostate cancer ranks sixth in incidence and seventh in mortality among male malignancies.
According to Frost & Sullivan, in 2019, prostate cancer ranked fifth globally in terms of new cases, with 1.316 million cases; the global market size for prostate cancer is projected to reach $37.6 billion by 2030.
PROTAC technology represents a revolutionary breakthrough in the field of small-molecule drugs in recent years, enabling the targeting of previously "undruggable" proteins and addressing drug resistance issues. By simultaneously binding to the target protein and an E3 ligase, PROTAC molecules facilitate the ubiquitination of the target protein, leading to its subsequent proteasome-dependent degradation. This technology holds broad application prospects and is one of the most prominent frontiers in small-molecule drug development.
HP518 is an oral PROTAC drug independently developed by Haichuang Pharmaceutical for the treatment of prostate cancer, targeting the degradation of the androgen receptor (AR). It holds potential for treating drug-resistant prostate cancer and is currently undergoing Phase I clinical trials in Australia. Preclinical study results have shown that HP518 exhibits high degradation activity against both wild-type AR and certain enzalutamide-resistant AR mutants, demonstrates high selectivity for AR, displays excellent anti-proliferative activity in AR-dependent prostate cancer cell lines, and shows superior efficacy in animal models of prostate cancer. Additionally, HP518 has demonstrated favorable druggability and safety profiles.
Haichuang Pharmaceutical is a global innovative pharmaceutical company focused on cancer and metabolic diseases. Guided by its mission to “Create Quality Medicines, Benefit the World,” the company is dedicated to providing patients with safe, effective, and affordable drugs, and committed to researching, developing, and manufacturing innovative medicines with global rights that address significant unmet clinical needs.
The company boasts four core technology platforms: the PROTAC Targeted Protein Degradation Platform, the Deuterated Drug Development Platform, the Targeted Drug Discovery and Validation Platform, and the Lead Compound Optimization and Screening Platform. It is currently undertaking two National Major Science and Technology Projects for “Major New Drug Creation” as well as multiple provincial and municipal research projects, with 10 products in its development pipeline. The company’s management team possesses extensive experience in drug research and development, with core members hailing from renowned Fortune 500 pharmaceutical companies.
Within the Company’s current product pipeline, HC-1119 is undergoing two Phase III clinical trials in China and globally for the treatment of castration-resistant prostate cancer; HP501, indicated for hyperuricemia/gout, has completed its Phase II clinical trial; HP558, which shows potential therapeutic effects against gastrointestinal tumors, has completed its Phase I clinical trial in Europe, and its Phase II clinical trial application has been approved by the NMPA; and HP518, an oral PROTAC drug targeting the androgen receptor (AR), is currently conducting a Phase I clinical trial in Australia.