Article ; Online: Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
2022 Volume 155, Page(s) 113695
Abstract: Afatinib is an oral small-molecule kinase inhibitor (SMKI) approved for treatment of metastatic non-small cell lung cancer (NSCLC) with an epidermal growth factor receptor (EGFR) driver mutation. Although oral administration is convenient, most SMKIs ... ...
Abstract | Afatinib is an oral small-molecule kinase inhibitor (SMKI) approved for treatment of metastatic non-small cell lung cancer (NSCLC) with an epidermal growth factor receptor (EGFR) driver mutation. Although oral administration is convenient, most SMKIs experience pH-dependent solubility. A drug-drug interaction between afatinib and proton-pump inhibitors (PPIs) has, however, never been studied in humans. Hence, we performed a randomized, three-period cross-over study. Afatinib (30 mg or 40 mg) was administered without PPI (period A), concomitantly with esomeprazole (period B) and three hours after esomeprazole intake (period C). Primary objective was the area under the curve (AUC |
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MeSH term(s) | Humans ; Carcinoma, Non-Small-Cell Lung/pathology ; Afatinib/therapeutic use ; Erlotinib Hydrochloride ; Esomeprazole ; Gefitinib/therapeutic use ; Cross-Over Studies ; Biological Availability ; Proton Pump Inhibitors/adverse effects ; Lung Neoplasms/pathology ; ErbB Receptors/genetics ; Protein Kinase Inhibitors/adverse effects ; Mutation |
Chemical Substances | Afatinib (41UD74L59M) ; Erlotinib Hydrochloride (DA87705X9K) ; Esomeprazole (N3PA6559FT) ; Gefitinib (S65743JHBS) ; Proton Pump Inhibitors ; ErbB Receptors (EC 2.7.10.1) ; Protein Kinase Inhibitors |
Language | English |
Publishing date | 2022-09-19 |
Publishing country | France |
Document type | Randomized Controlled Trial ; Journal Article |
ZDB-ID | 392415-4 |
ISSN | 1950-6007 ; 0753-3322 ; 0300-0893 |
ISSN (online) | 1950-6007 |
ISSN | 0753-3322 ; 0300-0893 |
DOI | 10.1016/j.biopha.2022.113695 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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