The mechanism of action of antibody-drug conjugates (ADCs). (IMAGE)
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Following intravenous administration, ADCs circulate in the bloodstream (①) and specifically bind to their target antigen on the tumor cell surface (②). The antigen–ADC complex undergoes receptor-mediated endocytosis (③), after which the conjugate is trafficked into endolysosomal compartments, where proteolytic cleavage or linker degradation occurs to release the cytotoxic payload (④). The liberated payload exerts diverse effector functions (⑤), including inhibition of microtubule polymerization, induction of DNA damage, disruption of energy metabolism, and in some cases phototoxicity upon irradiation, ultimately leading to tumor cell death.
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