INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models
Fig 4
Efficacy of INCB054828 in tumor models with FGFR alterations.
(A) KATO III (FGFR2-amplified) gastric cancer model. Severe combined immunodeficiency mice bearing KATO III tumors were administered INCB054828 (0.03, 0.1, 0.3, or 1 mg/kg) or vehicle by gavage once daily for 10 days. The mean tumor size is plotted for each group of 8 mice. ***P < 0.001 vs vehicle. (B) KG1 (FGFROP2-FGFR1 fusion positive) AML model. Humanized NSG mice bearing KG1 tumors were administered INCB054828 (0.3 mg/kg) or vehicle by gavage once daily for 14 days. The mean tumor size is plotted for each group of 6 mice. *P < 0.05 vs vehicle by paired t-test. (C) RT-112 (FGFR3-TACC3 fusion positive) bladder carcinoma model. RNU immunocompromised rats bearing RT-112 tumors were administered INCB054828 (0.3 or 1 mg/kg) or vehicle by gavage once daily for 14 days. The mean tumor size is plotted for each group of 7 mice. **P < 0.01 vs vehicle. (D) CTG-0997 (FGFR2-TRA2B fusion positive) cholangiocarcinoma PDX model. Tumor bearing nu/nu mice were administered INCB054828 (0.3 or 1 mg/kg) or vehicle by gavage once daily for 42 days. The mean tumor size is plotted for each group of 12 mice. **P < 0.01 vs vehicle. S.E.M., standard error of the mean.