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SIM0501 Tablets, a USP1 Small-Molecule Inhibitor, Obtained Clinical Trial Approval in China

Release time:2024-01-16

On January 13, 2024, Simcere Zaiming Pharmaceutical Co. Ltd. (“Simcere Zaiming”), an innovative oncology company and a subsidiary of Simcere Pharmaceutical Group Ltd. (HKEX: 2096, “Simcere”), announced that SIM0501 tablet, a small-molecule inhibitor of Ubiquitin Specific Peptidase 1 (“USP1”) and an anti-tumor drug candidate independently developed by Simcere, has obtained the Clinical Trial Approval issued by the National Medical Products Administration (NMPA) in China. Clinical trials for SIM0501 tablet as a monotherapy will be initiated for patients with advanced malignant solid tumors.


SIM0501 is an oral, non-covalent, and highly selective inhibitor of USP1. USP1 is found to be overexpressed in various tumors and plays a key role in DNA damage response and repair. The inhibition of USP1 can promote apoptosis in tumors, especially in tumors with homologous recombination deficiency (“HRD”). Following the success of the PARP inhibitor (“PARPi”), the USP1 inhibitor is expected to provide innovative solutions for more patients with solid tumors in the field of “synthetic lethality”. In preclinical in vitro and in vivo pharmacology studies, SIM0501 has shown significant anti-proliferation activity against HRD tumors as a monotherapy or in combination with PARPi, which demonstrates high potential for clinical development. On December 2, 2023, the Investigational New Drug (IND) application of SIM0501 to initiate clinical trials for advanced solid tumors was approved by the U.S. Food and Drug Administration (FDA).