Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.7.10.2 (
focal adhesion kinase
)
44,029
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Momelotinib is a potent and selective small-molecule inhibitor of
JAK1
/2 that is under investigation for the treatment of myeloproliferative neoplasms. In a phase 1/2 study in myelofibrosis patients, once-daily dosing of a 300-mg momelotinib capsule was selected for further development based on a favorable benefit:risk profile. A tablet formulation was recently developed for further clinical evaluation. In this study, the relative bioavailability of the tablet formulation versus the initial capsule formulation and the effect of food and omeprazole on the pharmacokinetics of a single-dose momelotinib tablet were evaluated in healthy subjects. The momelotinib tablet, 200 mg, provided plasma exposure equivalent to the 300-mg capsule. Plasma exposure of momelotinib increased less than dose-proportionally from 100 to 800 mg. Food intake modestly increased C
max
(38% and 28% increase for low- and high-fat meals, respectively) and AUC
inf
(16% and 28% increase for low- and high-fat meals, respectively) for the momelotinib tablet.
Omeprazole
reduced the exposure of the momelotinib tablet by 36% for C
max
and 33% for AUC
inf
. Neither the food effect nor the omeprazole effect on momelotinib exposure was considered clinically meaningful because of the safety and efficacy profile of momelotinib.
...
PMID:The Relative Bioavailability, Food Effect, and Drug Interaction With Omeprazole of Momelotinib Tablet Formulation in Healthy Subjects. 2902 42
