II. Mechanism

  1. Exert cytotoxic effects via transfer of alkyl group
    1. DNA alkylation (key to cellular lethality)
    2. Chemically react with many cellular constituents
  2. DNA cross linking is a primary role of agents
  3. Replicating cells are most susceptible to agents
  4. Alkylating Agents are not cell cycle specific

III. Types

  1. Bis (chloroethyl) amines
    1. Cyclophosphamide
    2. Mechlorethamine
    3. Chlorambucil
    4. Melphalan
  2. Nitrosoureas
    1. Carmustine (BCNU)
    2. Lomustine (CCNU)
    3. Semustine (Methyl-CCNU)
  3. Aziridines
    1. Thiotepa
    2. Triethylenemelamine
  4. Alkylsulfonates
    1. Busulfan
  5. Other drugs causing alkylation
    1. Procarbazine
    2. Dacarbazine
    3. Hexamethylmelamine
    4. Cisplatin

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