Updated: 6/5/2018

Alkylating Agents

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 Overview

 

Drugs Mechanism of Action Toxicity
Cyclophosphamide and ifosfamide Crosslinks DNA Hemorrhagic cytitis and myelosupression
Nitrosoureas Crosslinks DNA Dizziness and ataxia
Busulfan Alkylates DNA Pulmonary fibrosis and hyperpigmentation

 

Cyclophosphamide and Ifosfamide
  • Mechanism
    • covalently crosslinks DNA
      • at guanine N7 position
      • between strands and within strands
    • requires bioactivation by liver
  • Clinical use
    • non-Hodgkin's lymphoma
    • breast cancer
    • ovarian cancer
    • immunosuppression
  • Toxicity
    • hemorrhagic cystitis 
      • prevent with mesna or N-acetylcysteine
        • thiol group binds acrolein, a toxic metabolite
    • myelosuppression
Nitrosoureas (Carmustine, Lomustine, Semustine, and Streptozocin)
  • Mechanism
    • crosslinks DNA
    • crosses BBB and enters CNS
    • requires bioactivation
  • Clinical use
    • brain tumors
      • including glioblastoma multiforme
  • Toxicity
    • CNS toxicity
      • dizziness
      • ataxia
Busulfan
  • Mechanism
    • alkylates DNA
  • Clinical use
    • CML
      • was gold standard before imatinib was discovered
    • hematopoietic stem cell transplants
      • used for bone marrow ablation
  • Toxicity
    • pulmonary fibrosis
    • hyperpigmentation
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Questions (2)
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(M1.ON.13.119) A 52-year-old male with follicular non-Hodgkin lymphoma undergoes chemotherapy. He develops suprapubic pain and hematuria. Which of the following compounds is most likely responsible for this patient's symptoms? Tested Concept

QID: 101429
1

Cyclophosphamide

83%

(59/71)

2

Cisplatin

6%

(4/71)

3

Mesna

3%

(2/71)

4

Bleomycin

6%

(4/71)

5

Carmustine

1%

(1/71)

M 4 E

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