Table 1.
Chemotherapeutic agents: classification and mechanisms of action.
Mechanism of Action | Site of Action | Examples | |
---|---|---|---|
Antimetabolites | Interfere with DNA/RNA synthesis by inhibiting purine ring synthesis, ribonucleotide reductase or DNA monomers synthesis normally causing cell death during the S phase of cell growth. | Purines and pyrimidines synthesis | Thioguanine Mercaptopurine Methotrexenate |
Ribonucleotides | Hydroxycarbamide | ||
DNA monomers | Methotrexate 5-Fluorouracil |
||
DNA synthesis | Cytarabine Bleomycin |
||
Intercalating agents | Interfere with DNA/RNA synthesis, preventing cell duplication | Topoisomerase inhibitors (Etoposide Topotecan, Irinotecan) Antibiotics (anthracyclines, Chromomycin, Doxorubicin) |
|
Cross-linking agents | Cross-link two DNA bases together preventing DNA from being separated during DNA synthesis or transcription. Nucleotide mispairing, leading to mutations. | Alkylating agents Nitrosoureas Platinum-based coordination complexes |
|
Enzyme | Protein synthesis inhibition, leading to cell death by apoptosis | Protein synthesis | L-Asparaginase |
Microtubule damaging agents | Anti-mitotic agents that inhibit cell proliferation by disrupting the normal function of the mitotic spindle. | Microtubules | Taxanes Vinca alkaloids Taxol Colchicine |
Enzyme inhibitors | Interfere with normal cell metabolism, leading to cell death | Enzyme activity | Methotrexate Kinase inhibitors |
Angiogenesis inhibitors | Inhibit endothelial cells’ proliferation and tumor growth | Angiogenesis | Endostatin |