PR00012

PR00012 is a potent and selective small molecule inhibitor of Ubiquitin-Specific Peptidase 7 (USP7), developed by Beijing Zheyuan Technology Co., Ltd. using its proprietary AI-driven computational medicine platform. USP7 is a deubiquitinating enzyme that plays a critical role in regulating the stability of several key proteins involved in oncogenesis, most notably the MDM2-p53 axis. By inhibiting USP7, PR00012 prevents the deubiquitination of MDM2, leading to its degradation and the subsequent stabilization and reactivation of the p53 tumor suppressor protein. This mechanism induces cell cycle arrest and apoptosis in p53-wildtype cancer cells. Additionally, USP7 inhibition has been shown to modulate the tumor immune microenvironment by impairing the suppressive function of regulatory T cells (Tregs). PR00012 is currently being evaluated in Phase 1 clinical trials for the treatment of various advanced solid tumors, including pancreatic cancer, colorectal cancer, triple-negative breast cancer (TNBC), small cell lung cancer (SCLC), and head and neck squamous cell carcinoma.