Drug name Target Mode of Action Example
Auristatinsα-TubulinPrevent tubulin polymerization
Maytansinoidsα-TubulinPrevent tubulin polymerization
CalicheamicinsSequence-specific minor groove of DNACauses double-strand DNA breaks
Duocarmycin analoguesBind to specific minor groove of DNABreak down adenine-specific molecules in the DNA structure
Doxorubicin and Doxorubicin derivativesTopoisomerase II
DNA complexes
Inhibit DNA religation, leading to DNA double-strand breaks
  • BR96-DOX
CC-1065Sequence-specific minor groove of DNAInduces adenine alkylation
AnthracyclinesDNA, RNA complexesInhibit DNA and RNA synthesis by intercalating between base pairs, preventing replications
PyrrolobenzodiazepineSequence-selective. Bind to the minor groove of DNA and covalently attach to guanine residues

Interfere with the action of endonuclease enzymes on DNA and block transcription by inhibiting DNA polymerase in a sequence specific manner


Other cytotoxic agents used in the development of antibody-drug conjugates include:

  • Streptonigtin (anti CD30 and anti CD70)
  • Geldanamycin (HSP90 inhibitor)
  • Centanamycin (ML-970; indolecarboxamide);
  • SN38 is the active metabolite of irinotecan (an analog of Camptothecin, a topoisomerase I inhibitor)

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