Nitrosoureas

Summary

The nitrosoureas carmustine and lomustine are alkylating agents that crosslink DNA after being bioactivated by P450 enzymes in the liver. These drugs have a unique ability to cross the blood-brain barrier, making them useful for treating brain tumors, but this ability can also lead to CNS toxicity in patients taking these medications. 

Key Points

• Nitrosoureas
  • Drugs
    • Carmustine
    • Lomustine
  • Mechanism
    • Crosslinks DNA
      • Requires bioactivation by liver (P450)
      • Crosses blood-brain barrier (BBB) into the CNS
  • Clinical Use
    • Brain tumors
      • Because it crosses BBB
      • Including glioblastoma multiforme 
  • Adverse Effects
    • CNS toxicity
      • Symptoms including ataxia, convulsions, dizziness