| Drug name | Target | Mode of Action | Example |
| Auristatins | α-Tubulin | Prevent tubulin polymerization | |
| Maytansinoids | α-Tubulin | Prevent tubulin polymerization | |
| Calicheamicins | Sequence-specific minor groove of DNA | Causes double-strand DNA breaks | |
| Duocarmycin analogues | Bind to specific minor groove of DNA | Break down adenine-specific molecules in the DNA structure | |
| Doxorubicin and Doxorubicin derivatives | Topoisomerase II DNA complexes | Inhibit DNA religation, leading to DNA double-strand breaks |
|
| CC-1065 | Sequence-specific minor groove of DNA | Induces adenine alkylation | |
| Anthracyclines | DNA, RNA complexes | Inhibit DNA and RNA synthesis by intercalating between base pairs, preventing replications | |
| Pyrrolobenzodiazepine | Sequence-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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