HSK-46575 / Haisco - LARVOL DELTA

Phase 1, multicenter, open-label study of HSK46575 in patients with metastatic castration-resistant prostate cancer progressing after next-generation hormonal agents and chemotherapy. (ASCO 2026) - P1 | "HSK46575 shows a manageable safety profile and preliminary antitumor activity, especially in the population with AR - LBD mutations. These findings support further exploration in the mCRPC population. Clinical trial information: NCT07007910"

Clinical • Metastases • P1 data • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

HSK46575, a potent CYP11A1 inhibitor, demonstrates promising monotherapy and synergistic efficacy with SOCs for the treatment of castration-resistant prostate cancer (CRPC) (AACR 2026) - "A CYP11A1 inhibitor, ODM-208, showed a decrease in prostate-specific antigen levels of 50% (PSA50) in about 50% patients with AR LBD mutation (AR-mut), but lower response in CRPC patients with wild type AR (AR-wt) in phase1/2 studies...Model mice were treated with HSK46575 and/or other mechanic drugs, including PARP inhibitor (Olaparib), docetaxel or EZH2 inhibitor... Preliminary clinical data confirm the manageable safety profile and promising antitumor activity of HSK46575, particularly in patients harboring AR-LBD mutations. Furthermore. HSK46575 exhibits strong synergistic efficacy when combined with docetaxel or targeted agents (PARPi or EZH2i) in CRPC xenograft models."

Clinical • Late-breaking abstract • Monotherapy • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

HSK46575: A best-in-class, long lasting, small molecular CYP11A1 inhibitor for the treatment of castration-resistant prostate cancer (CRPC) (AACR 2025) - "Approximately half of the castration-resistant prostate cancer (CRPC) patients will benefit from abiraterone or enzalutamide treatment initially...Notably, 2.5 mg/kg/day dosage of HSK46575 exhibited superior efficacy compared to Abiraterone (200 mg/kg/day) and ODM-208 (60 mg/kg/day)... HSK46575 potently blocks the CYP11A1 enzymatic activity and the biosynthesis of Preg and TE at low nM concentrations in vitro. In normal male rats, the inhibition of both Preg and TE by HSK46575 was dose-dependent and long-lasting. In the LNCap (with AR-T877A) castrated xenograft model, HSK46575 significantly inhibited tumor growth and serum PSA level at a low dosage of 1 mg/kg/day."

Late-breaking abstract • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Phase I Study of HSK46575 in Patients With Metastatic Castration-Resistant Prostate Cancer (clinicaltrials.gov) - P1 | N=90 | Recruiting | Sponsor: Haisco Pharmaceutical Group Co., Ltd.

New P1 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Phase I clinical study to evaluate the safety, pharmacokinetics and efficacy of HSK46575 tablets in patients with metastatic castration-resistant prostate cancer (mCRPC) (ChiCTR) - P1 | N=90 | Sponsor: West China Hospital of Sichuan University; Xizang Heske Pharmaceutical Co., LTD

New P1 trial • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Hiseco: Received IND Application Acceptance Notice for Innovative Drug HSK46575 Tablets [Google translation] (Shanghai Securities News) - "Shanghai Securities News China Securities Network....Haisike announced that its subsidiary Tibet Haisike Pharmaceutical Co., Ltd. received the 'Acceptance Notice' issued by the State Food and Drug Administration on September 23, 2024. The drug name is HSK46575 tablets. HSK46575 tablets are an oral, potent and highly selective small molecule inhibitor independently developed by the company, intended for the treatment of prostate cancer."

New trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor