CH5183284

10/05/2023 - "In vivo studies using four ARPC PDX models showed that combination ENZA and CH5183284 significantly suppressed tumor growth. "
01/01/2019 - "A Phase I, Open-Label, Multicenter, Dose-escalation Study of the Oral Selective FGFR Inhibitor Debio 1347 in Patients with Advanced Solid Tumors Harboring FGFR Gene Alterations."
11/01/2014 - "Because of its unique binding mode, CH5183284/Debio 1347 can inhibit FGFR2 harboring one type of the gatekeeper mutation that causes resistance to other FGFR inhibitors and block FGFR2 V564F-driven tumor growth. "
01/01/2019 - "SIGNIFICANCE: ATP-competitive FGFR inhibitors (BGJ398, Debio 1347) show efficacy in FGFR2-altered ICC; however, acquired FGFR2 kinase domain mutations cause drug resistance and tumor progression. "
11/01/2014 - "Consistent with its high selectivity for FGFR enzymes, CH5183284/Debio 1347 displayed preferential antitumor activity against cancer cells with various FGFR genetic alterations in a panel of 327 cancer cell lines and in xenograft models. "

03/01/2015 - "Rat-2_F3-B cells showed in vitro and in vivo sensitivity in the selective FGFR inhibitor CH5183284/Debio 1347, indicating that FGFR3 kinase activity is critical for tumorigenesis. "

01/01/2019 - "Eligible patients received oral Debio 1347 at escalating doses once daily until disease progression or intolerable toxicity. "

01/01/2019 - "ATP-competitive fibroblast growth factor receptor (FGFR) kinase inhibitors, including BGJ398 and Debio 1347, show antitumor activity in patients with intrahepatic cholangiocarcinoma (ICC) harboring activating FGFR2 gene fusions. "

06/01/2023 - "We report two cases of fibroblast growth factor receptor (FGFR) inhibitor-associated retinopathy, including the first case of Debio 1347 associated retinopathy manifesting with bilateral serous retinal detachments along the superotemporal arcades and a case of erdafitinib associated retinopathy manifesting with classic foveal serous retinal detachments. "