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Busulfan

I Buggia1, F Locatelli, M B Regazzi

  • 1Department of Pharmacology, Istitato di Ricovero e Cura a Carattere Scientifico, Policlinico S. Matteo, Pavia, Italy.

The Annals of Pharmacotherapy
|September 1, 1994
PubMed
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Busulfan is effective for chronic myelogenous leukemia (CML) and as a high-dose preparative regimen for bone marrow transplantation (BMT). Understanding busulfan pharmacokinetics can improve outcomes and reduce toxicity through therapeutic drug monitoring.

Area of Science:

  • Pharmacology
  • Oncology
  • Hematology

Background:

  • Busulfan is a widely used chemotherapy agent.
  • Its use spans chronic myelogenous leukemia (CML) treatment and conditioning regimens for bone marrow transplantation (BMT).

Purpose of the Study:

  • To review pharmacokinetics, efficacy, safety, and toxicity of busulfan in pediatric and adult patients.
  • To evaluate the relationship between busulfan plasma concentrations and its clinical effects.

Main Methods:

  • Systematic review of English-language literature from 1953-1993.
  • Emphasis on pharmacologic studies and clinical trials in myeloproliferative disorders and BMT conditioning regimens.
  • Evaluation of pediatric and adult data, focusing on concentration-effect and concentration-toxicity relationships.

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Main Results:

  • Busulfan is effective at conventional doses for CML.
  • High-dose busulfan, often with cyclophosphamide, is a standard preparative regimen for BMT.
  • Age-dependent pharmacokinetics of high-dose busulfan noted; children have lower systemic exposure.
  • Toxicity (neutropenia, veno-occlusive disease, seizures) correlates with busulfan exposure.

Conclusions:

  • Busulfan is a safe and effective drug for CML treatment.
  • High-dose busulfan is crucial for myeloablative BMT conditioning.
  • Further understanding of busulfan pharmacokinetics and metabolism can optimize treatment outcomes.
  • Therapeutic drug monitoring to assess maximal tolerated exposure can reduce regimen-related toxicities.