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crizotinib + esomeprazole
- Development stage
- Phase 1
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Crizotinib + esomeprazole is the coadministration of **crizotinib**, a small-molecule tyrosine kinase inhibitor targeting anaplastic lymphoma kinase (ALK), ROS1, and MET, and **esomeprazole**, a proton pump inhibitor (PPI) that reduces gastric acid secretion. Crizotinib is primarily used for ALK-positive and ROS1-positive metastatic non-small cell lung cancer. Esomeprazole is commonly used to treat acid-related disorders. The combination is studied due to possible pharmacokinetic interactions, as crizotinib has pH-dependent solubility and esomeprazole raises gastric pH. Studies show coadministration results in a modest ~10% decrease in total crizotinib exposure but no significant change in peak exposure or safety profile, and no dose adjustment is considered necessary[1][2][3].
- Other names
- crizotinib + esomeprazole
02
Targets
ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)ATP4A (Potassium–transporting ATPase alpha chain 1)MST1R (Recepteur d'origine nantais)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)MET (Mesenchymal-epithelial transition factor receptor)
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