Basilea reports updated interim results for iCCA patients with FGFR2 mutations and amplifications from phase 2 study FIDES-01 at ASCO GI Cancers Symposium - Seite 2
Derazantinib poster presented at the 2022 ASCO GI Cancers Symposium | ||
Abstract # |
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427 |
M. M. Javle, G. K. Abou-Alfa, T. Macarulla, N. Personeni, F. Bergamo, D. Malka, A. Vogel, J. Adeva, J. Knox, J. Evans, W. P. Harris, M. Dimova-Dobreva, M. Saulay, M.
Engelhardt, S. Braun, M. Droz dit Busset, M. J. Borad Efficacy of derazantinib in intrahepatic cholangiocarcinoma patients with FGFR2 mutations or amplifications: Interim results from the phase 2 study FIDES-01. |
For further information please visit https://conferences.asco.org/gi/abstracts.
About derazantinib
Derazantinib is an investigational orally administered small-molecule FGFR inhibitor with strong activity against FGFR1, 2, and 3.3 FGFR kinases are key drivers of cell proliferation, differentiation and migration. FGFR genetic aberrations, e.g. gene fusions, mutations or amplifications, have been identified as potentially important therapeutic targets for various cancers, including intrahepatic cholangiocarcinoma (iCCA), urothelial, breast, gastric and lung cancers.4 In these cancers, FGFR genetic aberrations are found in a range of 5% to 30%.5
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Derazantinib also inhibits the colony-stimulating-factor-1-receptor kinase (CSF1R).3, 6 CSF1R-mediated signaling is important for the maintenance of tumor-promoting
macrophages and therefore has been identified as a potential target for anti-cancer drugs.7 Pre-clinical data has shown that tumor macrophage depletion through CSF1R blockade renders
tumors more responsive to T-cell checkpoint immunotherapy, including approaches targeting PD-L1/PD-1.8, 9
Derazantinib has demonstrated antitumor activity and a manageable safety profile in a previous biomarker-driven phase 1/2 study in iCCA patients,10 and has received U.S. and EU orphan
drug designation for iCCA. Basilea is currently conducting three clinical studies with derazantinib. The first study, FIDES-01, is a phase 2 study in patients with inoperable or advanced iCCA. It
comprises one cohort of patients with FGFR2 gene fusions and another cohort of patients with mutations or amplifications.1 The second study, FIDES-02, is a phase 1/2 study evaluating
derazantinib alone and in combination with Roche's PD-L1 checkpoint inhibitor, atezolizumab, in patients with advanced urothelial cancer, including metastatic, or recurrent surgically unresectable
disease, expressing FGFR genetic aberrations.11 The third study, FIDES-03, is a phase 1/2 study evaluating derazantinib alone and in combination with Lilly’s anti-VEGFR2 antibody
ramucirumab and paclitaxel, or with Roche’s PD-L1 checkpoint inhibitor atezolizumab, in patients with advanced gastric cancer with FGFR genetic aberrations.12 Basilea has in-licensed
derazantinib from ArQule Inc., a wholly-owned subsidiary of Merck & Co., Inc., Kenilworth, N.J., U.S.A.