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Chemotherapy Categories

Cell Cycle Nonspecific

  • Exert a cytotoxic effect throughout the cell cycle.
  • Effective against cells in resting phase.
  • Commonly see a dose-response relationship.
  • Concentration dependent – more effective when given in larger intermittent doses.

Alkylating Agents (and similar)

Work by DNA cross linking.

  • Mustard gas derivatives: Mechlorethamine, Cyclophosphamide, Chlorambucil, Melphalan, and Ifosfamide.
  • Ethylenimines: Thiotepa and Hexamethylmelamine.
  • Alkylsulfonates: Busulfan.
  • Hydrazines and Triazines: Altretamine, Procarbazine, Dacarbazine and Temozolomide.
  • Nitrosureas: Nitrosureas are unique because, unlike most types of chemo treatments, they can cross the blood-brain barrier. They can be useful in treating brain tumors.
  • Metal salts: Carboplatin, Cisplatin, and Oxaliplatin.

Anthracycline and Other Antibiotics

Bind with DNA to block RNA production.

  • doxorubicin, daunorubicin, idarubicin, dactinomycin, mitomycin, mitoxantrone and bleomycin.

Cell Cycle Specific

  • Drugs that inhibit or kill during a specific phase of the cell cycle.
  • Schedule dependant – maintain a cytotoxic level of drug for a period of time to allow tumour to ‘cycle’ through.
  • Generally produces the greatest cell kill if the amount of drug is divided and given in repeated fractions instead of single large dose.
  • More effective against tumours with high growth fraction.


Inhibit specific enzymes involved in DNA/RNA replication (S phase).
Similar to normal substances within the cell. When the cells incorporate these substances into the cellular metabolism they are unable to divide.

  • Folic acid antagonist: Methotrexate.
  • Pyrimidine antagonist: 5-Fluorouracil, Foxuridine, Cytarabine, Capecitabine, and Gemcitabine.
  • Purine antagonist: 6-Mercaptopurine and 6-Thioguanine.
  • Adenosine deaminase inhibitor: Cladribine, Fludarabine, Nelarabine and Pentostatin.

Topoisomerase inhibitors

Interfere with the action of topoisomerase enzymes (topoisomerase I and II) which control the manipulation of DNA necessary for replication.

  • Topoisomerase I inhibitors: Ironotecan, topotecan.
  • Topoisomerase II inhibitors: Amsacrine, etoposide, etoposide phosphate, teniposide.

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