Alkylating agents

on 29.8.08 with 0 comments

  • most importantly, cyclophosphamide

  • mechanism of action

    • they damage DNA by attaching themselves to DNA—they alkylate DNA and cause DNA breaks

    • DNA repair enzymes are overwhelmed

    • DNA damage response leads to apoptosis in the presence of normal p53

    • this is cell-cycle-independent chemotherapy, so they are the mainstay of treatment for solid tumors

  • mechanism of resistance

    • decreased active drug uptake

    • mutant p53

    • overcome resistance by higher doses

  • toxicities

    • most importantly, highly mutagenic

    • wear gloves, don’t inhale them

    • must counsel re potential secondary cancers

Category: Pharmacology Notes



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