INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models
Fig 3
Pharmacokinetics and pharmacodynamics of INCB054828 in the mouse.
(A) Pharmacokinetic profile of INCB054828 in the mouse. Plasma was collected over time from mice administered a single oral dose of INCB054828 for determination of total INCB054828 concentration. (B) Pharmacokinetic-pharmacodynamic analyses in KATO III tumors. Tumors and plasma were harvested from KATO III tumor-bearing mice following a single oral administration of INCB054828. Plasma was subjected to analytical analysis and phospho-FGFR2 in tumor homogenate was determined by ELISA. (C) Phosphate levels in the serum of mice following administration of INCB054828. 24 hours after a single oral administration of INCB054828 to C57BL/6 mice, blood was collected and the plasma submitted for analysis of inorganic phosphate.