H2-receptor antagonist influences dasatinib pharmacokinetics in a patient with Philadelphia-positive acute lymphoblastic leukemia.

Abstract

We recently reported in this journal that administration of acid suppressant such as an H2-receptor antagonist (H2RA) and a proton pump inhibitor can decrease the absorption of dasatinib from the gastrointestinal tract, thereby resulting in a significant decrease in its plasma concentration. Here, we report a patient treated with dasatinib and H2RA famotidine for whom the total area under the total plasma concentration-time curve (AUC(0-12)) of dasatinib dramatically increased after cessation of famotidine from 505.7 to 1,816.3 ng·h/mL. This is the first report to confirm the drug interaction between dasatinib and H2RA by using sequential pharmacokinetic profiling.

• Authors: Akihito Matsuoka, Naoto Takahashi, Masatomo Miura, Takenori Niioka, Kimihiro Kawakami, Takuya Matsunaga, Kenichi Sawada
• Journal: Cancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 70 Issue 2 Pg. 351-2 (Aug 2012) ISSN: 1432-0843 [Electronic] Germany
• PMID: 22678358 (Publication Type: Letter, Comment)

Chemical References

• Histamine H2 Antagonists
• Proton Pump Inhibitors
• Pyrimidines
• Thiazoles

Topics

• Female
• Histamine H2 Antagonists (pharmacology)
• Humans
• Leukemia, Myelogenous, Chronic, BCR-ABL Positive (metabolism)
• Male
• Precursor Cell Lymphoblastic Leukemia-Lymphoma (metabolism)
• Proton Pump Inhibitors (pharmacology)
• Pyrimidines (pharmacokinetics)
• Thiazoles (pharmacokinetics)