The document discusses antibody-drug conjugates (ADCs), which connect cytotoxic drugs to monoclonal antibodies. ADCs selectively deliver drugs to cancer cells by binding to antigens on tumors. The ADC-antigen complex is internalized and the linker connecting the drug is cleaved in the lysosome, releasing the cytotoxic drug to induce apoptosis. Common linkers are cleaved at low pH in lysosomes or are self-immolative. Future research aims to develop more selective and potent ADCs targeting specific tumor antigens.

1. Antibody-Drug Conjugates

2. Connection
to antibody
Drug
Selectivity Cytotoxicity
Linker
Self-
immolative
spacer
Polarity TriggerLinker

3. Antibody-Drug Conjugate
Apoptosis
(a) The ADC binds to the antigen on the target cell.
(b) The antigen-ADC complex is internalized
through receptor-mediated endocytosis and, in
most cases, is transported from early endosomes
to lysosomes.
(c) In the lysosome, internal conditions may
destabilize the linker or mAb backbone, causing
the cytotoxic component to dissociate and
circulate freely in the cytoplasm. Most cytotoxic
components of current ADCs either bind to the
minor groove of DNA and induce strand breakage
(d ) or bind to tubulin, resulting in microtubule
disruption
(e). ( f ) Both processes lead to apoptosis.

4. Linker
Connection
to antibody

5. Polarity
Linker

6. Linker
Trigger

7. Linker
Self-
immolative
spacer
Para-aminobenzyl “PAB”

8. Drug
MMAF

9. Examples
1
2
3

10. Future Directions
With the approval of Adcetris and the more than 20 ADCs currently
undergoing human clinical trials, ADCs are becoming a viable method
for selectively delivering a highly cytotoxic agent to tumor cells while
sparing the normal tissue. Future research in this area will continue to
produce highly selective and potent ADCs that will target specific
tumor antigens.

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