Work

191: The role of human CYP2B6 polymorphism in the bioactivation of cyclophosphamide using cDNA expressed enzymes

Year: 2007

Type: article

Abstract: Cyclophosphamide (CPA) is used for the treatment of many tumors and as a part of the conditioning regimen prior to stem cell transplantation. CPA is a prodrug that is activated through cytochrome P450 2B6 (CYP2B6) in the liver. A high degree of inter- and intra-individual variation in CPA pharmacokinetics has been reported. We have investigated the formation of its active metabolite 4-hydroxycyclophosphamide (4-OH-CPA) in vitro using three different mutants of recombinant 2B6. The rate of formation of 4-OH-CPA was correlated to the enzyme activity for different mutations.

Source: Transplantation and Cellular Therapy

DOI: 10.1016/j.bbmt.2006.12.195

Authors: P. Afsharian, Y. Terelius, M. Hidestrand, M. Ingelman-Sundberg, M. Hassan, S. Lundgren

Institutions: Karolinska Institutet, Medivir (Sweden), Karolinska University Hospital

Language: English

Topic: Pharmacogenetics and Drug Metabolism

Subfield: Pharmacology

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $3,650