DC10190

DC10190 is an orally bioavailable small molecule inhibitor of Ubiquitin-Specific Protease 1 (USP1), currently under clinical development by Beijing Double-Crane Run-Chuang Technology, a subsidiary of China Resources Double-Crane Pharmaceutical. USP1 is a deubiquitinating enzyme that plays a critical role in the DNA damage response (DDR) by regulating the monoubiquitination of PCNA and FANCD2, which are essential for translesion synthesis and the Fanconi anemia pathway, respectively. By inhibiting USP1, DC10190 disrupts these DNA repair mechanisms, leading to increased genomic instability and apoptosis in cancer cells. This mechanism is particularly effective in tumors with existing defects in homologous recombination repair (HRR), such as those with BRCA mutations, and may overcome resistance to PARP inhibitors. DC10190 is being evaluated in Phase I clinical trials for the treatment of advanced or metastatic solid tumors.