Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 16.02.2021

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Busulfan is a bifunctional alkylan, a sulfonic acid alkyl ester, which alkylates nucleic acids and proteins in the cell by splitting off the methanesulfone groups. Busulfan can be applied orally as well as intravenously.

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Busulfan is orally approved for the palliative treatment of chronic myeloid leukemia (CL). This therapy is largely abandoned today, as the tyrosine kinase inhibitor Imatinib provides a much better therapeutic principle.

The preferred field of application of Busulfan today is the conditioning treatment prior to stem cell transplantation. For this purpose the drug is typically used in combination with cyclophosphamide.

Undesirable effects
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Liver dysfunction: hyperbilirubinemia, icterus, hepatic vein occlusion, fibrosis with hepatocellular necrosis

Interstitial pneumonia (J84.9)

Pulmonary fibrosis (busulfan lung - Pearl M 1977) (J84.9)

Pericardial fibrosis (Terpstra W et al 1989)(I31.9)

Cataract formation (Honda A et al 1993)

Hyperpigmentation of the skin (Simonart T et al. 1999)

Enhancement of local radiotherapeutic effects -s.a. under Radiation Recall (Vassal G et al. 1989)

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  1. Dahlgren S et al (1972) Clinical and morphological side-effects of busulfan (Myleran) treatment. Acta Med Scand 192:129-135.
  2. Honda A et al (1993) Nippon Ganka Gakkai Zasshi 97:1242-1245.
  3. Pearl M (1977) Busulfan lung. On J Dis Child 131:650-652.
  4. Terpstra W et al (1989) Pericardial fibrosis following busulfan treatment. Neth J Med 35:249-252.
  5. Simonart T et al (1999) Hyperpigmentation inducite par le busulfan: une observation avec ├ętude ultrastructurale [Hyperpigmentation induced by busulfan: a case with ultrastructure examination]. Ann Dermatol Venereol 126:439-440.
  6. Vassal G et al (1989) Enhanced cutaneous radiation effects following high-dose busulfan therapy. Cancer chemother Pharmacol 23:117-118.


Last updated on: 16.02.2021