HSK39775 / Haisco - LARVOL DELTA

USP1 inhibition: A journey from target discovery to clinical translation. (PubMed, Pharmacol Ther) - "RO7623066 (KSQ-4279) reported an acceptable safety profile during a phase I dose escalation study, with anemia being the most common side effect, and demonstrated robust pharmacokinetic, pharmacodynamic, and clinical activity. Other USP1 inhibitors, including SIM0501, XL309-101, and HSK39775, are currently in early clinical development. In this review, we provide an overview of the molecular function of USP1 and its importance as a therapeutic target in oncology, before focusing on the current state of preclinical and clinical development of USP1 inhibitors."

Journal • Review • Hematological Disorders • Oncology • Targeted Protein Degradation • BRCA1 • FANCD2 • FANCI • PCNA • USP1

HSK39775: A USP1 inhibitor for the treatment of cancers with homologous recombination deficiencies (AACR 2024) - "Meanwhile, combination with PARP inhibitors significantly enhanced the therapeutic efficacy of HSK39775 in xenograft model and led to tumor regressions and durable tumor control even at low dose (TGI:89% (HSK39775, 5 mg/kg + Olaparib, 50 mg/kg)). Interestingly, HSK39775 inhibited the tumor growth of a HRP and BRCA wild-type lung cancer xenograft as a single agent with TGI of 94% at 30 mg/kg QD, suggesting the therapeutic effect of USP1 inhibitors beyond canonical BRCA mutant or HRD tumors. In summary, these results indicate HSK39775 as a potent and selective USP1 inhibitor and support further development."

Breast Cancer • Lung Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • BRCA • BRCA1 • BRCA2 • HRD • PCNA • USP1

A Study for HSK39775 in Participants With Solid Tumors (clinicaltrials.gov) - P1/2 | N=243 | Recruiting | Sponsor: Xizang Haisco Pharmaceutical Co., Ltd

Metastases • Monotherapy • New P1/2 trial • Oncology • Solid Tumor