TQB3217

TQB3217 is an orally bioavailable small molecule inhibitor of ubiquitin-specific peptidase 1 (USP1), currently under development by Chia Tai Tianqing Pharmaceutical Group for the treatment of advanced solid tumors. 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, TQB3217 promotes the accumulation of ubiquitinated substrates, leading to impaired DNA repair and increased genomic instability, particularly in tumors with existing defects in homologous recombination repair. It is currently being evaluated in Phase 1 clinical trials to assess its safety, pharmacokinetics, and preliminary anti-tumor activity in patients with advanced malignancies who have progressed on standard therapies.