GRX2672

GRX2672 is a novel aptamer-drug conjugate (ApDC) designed to target LRRC15-expressing tumors. Developed by Guardian Therapeutics in collaboration with Pinotbio, it consists of a high-affinity LRRC15-targeting aptamer conjugated to a novel topoisomerase I inhibitor payload, PBX-7016, with a drug-to-aptamer ratio (DAR) of 2. The construct also incorporates a proprietary half-life-extending fatty acid moiety at the 3' end to improve pharmacokinetic properties while maintaining a small molecular size for superior tumor penetration compared to traditional antibody-drug conjugates (ADCs). LRRC15 is highly expressed in mesenchymal-derived tumors such as sarcoma, glioblastoma, and melanoma. In preclinical studies, GRX2672 demonstrated selective cytotoxicity and complete tumor growth inhibition in vivo.