Development of a facile antibody–drug conjugate platform for increased stability and homogeneity

摘要: Despite the advances in design of antibody–drug conjugates (ADCs), search is still ongoing for novel approaches that lead to increased stability and homogeneity ADCs. We report, first time, an ADC platform technology using a platinum(II)-based linker can re-bridge inter-chain cysteines antibody, post-reduction. The strong platinum–sulfur interaction improves when compared with standard maleimide-linked thereby reducing linker–drug exchange albumin significantly. Moreover, due precise conserved locations cysteines, both site-specificity are simultaneously achieved. Additionally, we demonstrate our ADCs exhibit anticancer efficacy vitro vivo. Pt-based emerge as simple exciting proposition address limitations current technologies.