Alkylating Agent

Aka: Alkylating Agent, Nitrosourea Compound, Nitrogen Mustard Antineoplastic Compound, Aziridine, Alkylsulfonate, Mesylate, Triazene Antineoplastic, Platinum Antineoplastic Compound, Platinum Analog Chemotherapeutic Agent

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II. Mechanism

  1. Alkylating Agents are not Cell Cycle specific
  2. Exert cytotoxic effects via transfer of unstable alkyl group
    1. DNA alkylation (key to cellular lethality, esp. DNA cross linking)
    2. Chemically react with other cellular constituents (e.g. Proteins)
  3. Replicating cells and rapidly growing cells are most susceptible to agents (related to adverse effects)
    1. Blood cell precursors
    2. Hair cells
    3. Gastrointestinal cells
  4. Cancer resistance mechanisms
    1. Decreased Chemotherapeutic Drug uptake
    2. Repair of DNA damage

III. Medications

  1. Nitrogen Mustard Antineoplastic Compounds (Bis -chloroethyl- amines)
    1. Bendamustine
    2. Chlorambucil
    3. Cyclophosphamide (prodrug, activated in liver)
    4. Ifosfamide (prodrug, activated in liver)
    5. Mechlorethamine
    6. Melphalan
  2. Nitrosourea Compounds
    1. Carmustine (BCNU)
    2. Lomustine (CCNU)
    3. Semustine (Methyl-CCNU)
    4. Streptozocin
  3. Aziridines (Ethyleneimine)
    1. Thiotepa
    2. Triethylenemelamine
  4. Mesylate (Alkylsulfonate)
    1. Busulfan
  5. Triazene Antineoplastic
    1. Procarbazine
    2. Dacarbazine
    3. Temozolamide
  6. Platinum Analogs
    1. Carboplatin
    2. Cisplatin
    3. Oxaliplatin
  7. Other drugs causing alkylation
    1. Hexamethylmelamine
    2. Trabectedin

IV. References

  1. Olson (2020) Clinical Pharmacology, Medmaster, Miami, Fl, p. 126
  2. Amjad (2023) Cancer Chemotherapy, StatPearls, Treasure Island, Fl, accessed 2/1/3/2024
    1. https://www.ncbi.nlm.nih.gov/books/NBK564367/

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