2E7-MMAE

2E7-MMAE is an antibody-drug conjugate (ADC) consisting of the monoclonal antibody 2E7, which specifically targets the integrin α3β1 (ITGA3B1) heterodimer, conjugated to the cytotoxic payload monomethyl auristatin E (MMAE). Identified through a target-unbiased phenotypic discovery platform, the 2E7 antibody exhibits rapid internalization upon binding to ITGA3B1, a protein found to be overexpressed in various solid tumors, particularly aggressive subtypes of bladder cancer. Once internalized, the MMAE payload is released, where it acts as a potent tubulin inhibitor, disrupting microtubule polymerization and leading to cell cycle arrest and apoptosis. In preclinical xenograft models of bladder cancer, 2E7-MMAE has demonstrated dose-dependent antitumor activity, including tumor regression and improved survival.