LIT0922

LIT0922 is a potent and selective small molecule inhibitor of Ubiquitin-specific-processing protease 1 (USP1), developed by Lidi (Hangzhou) Pharmaceutical Technology. USP1 is a deubiquitinating enzyme that plays a critical role in the DNA damage response (DDR) pathway, specifically by regulating the Fanconi anemia (FA) pathway and translesion synthesis (TLS) through the deubiquitination of FANCD2 and PCNA. By inhibiting USP1, LIT0922 promotes the accumulation of ubiquitinated substrates, leading to impaired DNA repair, genomic instability, and apoptosis in cancer cells. This mechanism is particularly effective in tumors with homologous recombination deficiencies (HRD) or in combination with other DDR-targeting agents such as PARP inhibitors. LIT0922 is currently being evaluated in Phase 1 clinical trials for the treatment of advanced solid tumors.