ICT12035

ICT12035 is a potent, small-molecule antagonist of the formyl peptide receptor-1 (FPR1), a member of the 7-transmembrane G protein-coupled receptor (GPCR) family. Developed by researchers at the University of Bradford, ICT12035 is a pyrazole-based compound designed to block the activation of FPR1 by ligands such as Annexin-A1 and short-chain N-formylated peptides (e.g., fMLF) that are typically released from the hypoxic or necrotic cores of tumors. FPR1 is frequently overexpressed in malignant cancers, particularly glioblastoma, where it drives proliferation, invasion, and angiogenesis. Preclinical studies have demonstrated that ICT12035 can arrest tumor growth in vivo and significantly enhance the efficacy of cytotoxic agents like temozolomide (TMZ) and carmustine (BCNU), as well as radiotherapy, by overcoming FPR1-mediated resistance mechanisms.