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.
Akihito
A
Matsuoka
Naoto
N
Takahashi
Masatomo
M
Miura
Takenori
T
Niioka
Kimihiro
K
Kawakami
Takuya
T
Matsunaga
Kenichi
K
Sawada
D005260:Female; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000378:metabolism*; D008297:Male; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000378:metabolism*; D054328:Proton Pump Inhibitors / Q000494:pharmacology*; D011743:Pyrimidines / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000493:pharmacokinetics*
D006635:Histamine H2 Antagonists; D054328:Proton Pump Inhibitors; D011743:Pyrimidines; D013844:Thiazoles