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Simcere Zaiming announces global FIH dosing of USP1 inhibitor in clinical trial

Release time:2024-03-22


On March 19, 2024, Simcere Zaiming, an innovative oncology company and a subsidiary of Simcere Pharmaceutical Group Ltd., announced that a Phase 1 clinical study of SIM0501, Zaiming’s USP1 inhibitor, enrolled the first patient with advanced solid tumors in a First-in-Human (FIH) trial in China.

This international multi-center, open-label phase 1 study, led by Prof. Yu Jinming at the Shandong Cancer Hospital and Institute, plans to enroll approximately 140 adult patients with advanced solid tumors to evaluate the efficacy, safety as well as pharmacokinetics of SIM0501 monotherapy and combination therapy in advanced solid tumors. This study has obtained approval to be carried out both in China and the United States.

SIM0501 is an oral, non-covalent, and highly selective inhibitor of USP1 independently developed by Simcere Zaiming. It is also the first USP1 inhibitor to enter the clinical research stage in China. USP1 is overexpressed in various tumors and plays a key role in DNA damage response and repair. Inhibition of USP1 can promote apoptosis in cancer cells, especially in tumors harboring homologous recombination deficiency (“HRD”). Following the success of the PARP inhibitors (“PARPi”), the USP1 inhibitor is expected to provide innovative solutions for more patients by utilizing a precision medicine strategy called “synthetic lethality”. In preclinical in vitro and in vivo pharmacology studies, SIM0501 has shown significant anti-proliferative activity against HRD tumors as a monotherapy or in combination with PARPi, which demonstrates high potential for clinical development. The latest preclinical data will be presented at the 2024 AACR annual meeting as late-breaking research(#LB271).

By precisely targeting tumor cells with homologous recombination defects, SIM0501 treatment may cause less harm to normal cells and can offer a favorable efficacy and safety profile. SIM0501 also has the potential to be combined with PARP inhibitors to solve the problem of clinical drug resistance. Simcere Zaiming is actively working with clinical experts toward clinical validation and development of this therapeutic pipeline program for the benefit of a broad population of cancer patients globally.