Val-Cit-MMAE

A widely used antibody-drug conjugate (ADC) payload system combining a protease-cleavable valine-citrulline (Val-Cit) dipeptide linker with monomethyl auristatin E (MMAE), a potent microtubule-disrupting agent. The linker-toxin structure enables high plasma stability and efficient intracellular release of MMAE via cathepsin B-mediated cleavage in target cells, leading to cytotoxic arrest of cell division. This construct is the foundational component of several clinically approved ADCs, including brentuximab vedotin (Adcetris®), for the treatment of Hodgkin lymphoma and other CD30-positive malignancies.

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