Association of enzyme and transporter genotypes with the pharmacokinetics of imatinib

• Published in: Clinical pharmacology and therapeutics Vol. 80; no. 2; p. 192
• Main Authors: Gardner, Erin R, Burger, Herman, van Schaik, Ron H, van Oosterom, Allan T, de Bruijn, Ernst A, Guetens, Gunther, Prenen, Hans, de Jong, Floris A, Baker, Sharyn D, Bates, Susan E, Figg, William D, Verweij, Jaap, Sparreboom, Alex, Nooter, Kees
• Format: Journal Article
• Language: English
• Published: United States 01.08.2006
• Subjects: Adult; Aged; Aged, 80 and over; Alleles; ATP-Binding Cassette Transporters - genetics; Benzamides; Biological Transport, Active; Carrier Proteins - genetics; Carrier Proteins - metabolism; Cell Line, Tumor; Cohort Studies; Cytochrome P-450 Enzyme System - genetics; Female; Gastrointestinal Neoplasms - genetics; Gastrointestinal Neoplasms - metabolism; Gene Frequency; Genotype; Humans; Imatinib Mesylate; Isoenzymes - genetics; Male; Middle Aged; Pharmaceutical Preparations - metabolism; Phenotype; Piperazines - pharmacokinetics; Protein-Tyrosine Kinases - antagonists & inhibitors; Proto-Oncogene Proteins c-kit - genetics; Pyrimidines - pharmacokinetics; Stromal Cells - metabolism

Our objective was to explore the relationships between imatinib pharmacokinetics and 9 allelic variants in 7 genes coding for adenosine triphosphate-binding cassette transporters (ABCB1 and ABCG2) and enzymes (cytochrome P450 [CYP] 2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5) of putative relevance for...