2015 Antineoplastics

I. Crosslinking agents


One major distinguishing feature among alkylating agents is the rate at which the parent drug is converted to a strong electrophile. For some drugs (e.g. MECHLORETHAMINE), the reaction is virtually instantaneous --- these agents are given IV to minimize blistering and GI effects. Other agents (such as CYCLOPHOSPHAMIDE, BUSULFAN, and MELPHALAN) must be activated in various tissues, and they can be given orally.
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Mechlorethamine structure

MECHLORETHAMINE: instantaneous activation upon contact with water à vesicant (common toxicity of many cytotoxic agents)



Cyclophosphamide activation

Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 11-apr-15 9:39 AM