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

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.
AuthorsAkihito Matsuoka, Naoto Takahashi, Masatomo Miura, Takenori Niioka, Kimihiro Kawakami, Takuya Matsunaga, Kenichi Sawada
JournalCancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 70 Issue 2 Pg. 351-2 (Aug 2012) ISSN: 1432-0843 [Electronic] Germany
PMID22678358 (Publication Type: Comment, Letter)
Chemical References
  • Histamine H2 Antagonists
  • Proton Pump Inhibitors
  • Pyrimidines
  • Thiazoles
  • 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)

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