BIK-E715E

BIK-E715E is an integrin-targeting ligand-drug conjugate (LDC) developed by BIK Therapeutics for the treatment of glioblastoma. It utilizes the proprietary ELiTE-DDS (Enhancing Ligand Targeting and Endocytosis) platform, which is designed to improve target-selective intracellular delivery and blood-brain barrier (BBB) penetration. The conjugate consists of a high-affinity cyclic peptide ligand, D-[c(RGDfK)]2, which targets integrins αvβ3 and αvβ5, and the topoisomerase I inhibitor exatecan as the cytotoxic payload. Upon binding to integrins highly expressed on glioblastoma cells and the tumor vasculature, BIK-E715E is internalized via an Arf6-dependent endocytic pathway. Once inside the cell, the exatecan payload induces DNA damage and apoptosis. Preclinical studies have demonstrated its ability to cross the BBB via receptor-mediated transcytosis and show significant antitumor efficacy in orthotopic xenograft models.