Mechanism of Action of Antibody-Drug Conjugates

ADC's are composed of three parts:

• Antibody – monoclonal antibodies are commonly used to target a tumor-specific antigen or receptor on the surface of the cell
• Linker – a chemical linker that attaches the antibody to the payload
• Payload – biologically active drug or cytotoxic compound

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• The ADC binds to the antigen or receptor on the target cell's surface.
• The bound drug and antibody conjugates are internalized by the cell through endocytosis.
• Once internalized and within the lysosome, the antibody is digested, and the linker is degraded, releasing the "deactivated" cytotoxic compound payload.
• The cytotoxic payload regains full activity and is released into the cytoplasm of the cell.
• The released cytotoxic compound exerts microtubule or DNA disruption.
• Damage to the DNA and microtubules induces apoptosis, resulting in cell death.