Futibatinib for
            <i>FGFR2</i>
            -Rearranged Intrahepatic Cholangiocarcinoma

Goyal, Lipika; Meric‐Bernstam, Funda; Hollebecque, Antoine; Valle, Juan W.; Morizane, Chigusa; Karasic, Thomas B.; Abrams, Thomas A.; Furuse, Junji; Kelley, Robin K.; Cassier, Philippe; Klümpen, Heinz‐Josef; Chang, Heung-Moon; Chen, Li-Tzong; Tabernero, Josep; Oh, Do‐Youn; Mahipal, Amit; Moehler, Markus; Mitchell, Edith P.; Komatsu, Yoshito; Masuda, Koichi; Ahn, Daniel H.; Epstein, Robert S.; Halim, Abdel; Fu, Yao; Salimi, Tehseen; Wacheck, Volker; He, Yaohua; Liu, Mei; Benhadji, Karim A.; Bridgewater, John

doi:10.1056/nejmoa2206834

Cited by 215 publications

(201 citation statements)

References 40 publications

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“…Many of these clinical trials aim to evaluate progression-free survival (FPS), tolerability, and safety. The clinical trials reported in Table 2 show the inhibition of FGFR in different types of cancer, such as in cholangiocarcinoma [ 214 , 215 , 216 ]; in these studies, selective inhibitors of FGFR 1-4 were used, such as Futibatinib and Pemigatinib, demonstrating their efficacy. Regarding the safety, the most common adverse effect of the use of such drugs is hyperphosphatemia, probably attributable to the function of FGF23 and FGFR signaling in phosphate homeostasis.…”

Section: Bfgf and Cancermentioning

confidence: 99%

Role of Basic Fibroblast Growth Factor in Cancer: Biological Activity, Targeted Therapies, and Prognostic Value

Ardizzone

Bova

Casili

et al. 2023

Cells

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Cancer is the leading cause of death worldwide; thus, it is necessary to find successful strategies. Several growth factors, such as vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF, FGF2), and transforming growth factor beta (TGF-β), are involved in the main processes that fuel tumor growth, i.e., cell proliferation, angiogenesis, and metastasis, by activating important signaling pathways, including PLC-γ/PI3/Ca2+ signaling, leading to PKC activation. Here, we focused on bFGF, which, when secreted by tumor cells, mediates several signal transductions and plays an influential role in tumor cells and in the development of chemoresistance. The biological mechanism of bFGF is shown by its interaction with its four receptor subtypes: fibroblast growth factor receptor (FGFR) 1, FGFR2, FGFR3, and FGFR4. The bFGF–FGFR interaction stimulates tumor cell proliferation and invasion, resulting in an upregulation of pro-inflammatory and anti-apoptotic tumor cell proteins. Considering the involvement of the bFGF/FGFR axis in oncogenesis, preclinical and clinical studies have been conducted to develop new therapeutic strategies, alone and/or in combination, aimed at intervening on the bFGF/FGFR axis. Therefore, this review aimed to comprehensively examine the biological mechanisms underlying bFGF in the tumor microenvironment, the different anticancer therapies currently available that target the FGFRs, and the prognostic value of bFGF.

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Section: Bfgf and Cancermentioning

confidence: 99%

Role of Basic Fibroblast Growth Factor in Cancer: Biological Activity, Targeted Therapies, and Prognostic Value

Ardizzone

Bova

Casili

et al. 2023

Cells

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show abstract

“…Cholangiocarcinoma has poor prognosis and scarce treatment options (King and Javle 2021 ). Futibatinib has been approved for unresectable, locally advanced, or metastatic intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor (FGFR)-2 gene fusions or other rearrangements in patients previously treated with non-FGFR therapies (Goyal et al 2023 ). Futibatinib was granted a priority review, accelerated approval, and breakthrough designation.…”

Section: Oncologymentioning

confidence: 99%

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

Kaykı-Mutlu

Aksoyalp

Wojnowski

et al. 2023

Naunyn-Schmiedeberg's Arch Pharmacol

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While new drug approvals by the U.S. Food and Drug Administration (FDA) had remained stable or even increased in the first 2 years of the COVID-19 pandemic, the 37 newly approved drugs in 2022 are considerably less than the 53 and 50 new drugs approved in 2020 and 2021, respectively, and less than the rolling 10-year average of 43. As in previous years of this annual review, we assign these new drugs to one of three levels of innovation: first drug against a condition (“first-in-indication”), first drug using a novel molecular mechanism (“first-in-class”), and “next-in-class,” i.e., a drug using an already exploited molecular mechanism. We identify two “first-in-indication” (ganaxolon and teplizumab), 20 (54%) “first-in-class,” and 17 (46%) “next-in-class” drugs. By treatment area, rare diseases and cancer drugs were once again the most prevalent (partly overlapping) therapeutic areas. Other continuing trends were the use of accelerated regulatory approval pathways and the reliance on biopharmaceuticals (biologics).

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“…These results indicated that erdafitinib demonstrated significant efficacy and safety in the treatment of advanced CCA with FGFR mutations/fusions. A phase II, openlabel, multicenter study indicated that futibatinib, a highly selective and irreversible FGFR1/2/3/4 inhibitor, significantly improved clinical outcomes for the advanced iCCA patients with FGFR2 gene fusion-rearrangement progressing after one or more previous lines of systemic therapy (27).…”

Section: Fgfrmentioning

confidence: 99%

Revisiting targeted therapy and immunotherapy for advanced cholangiocarcinoma

Xing

Zhang

et al. 2023

Front. Immunol.

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Cholangiocarcinoma (CCA) is a rare and aggressive type of malignant tumor. In the past few years, there has been an increase in the incidence of CCA. Surgery is the only effective treatment but is only suitable for a small percentage of patients. Comprehensive treatment is the normal therapy for terminal CCA patients, depending basically on gemcitabine and cisplatin combination chemotherapy. In the past decade, the emergence of next-generation sequencing technology can be used for the identification of important molecular features of CCA, and several studies have demonstrated that different CCA subtypes have unique genetic aberrations. Targeting fibroblast growth factor receptor (FGFR), isocitrate dehydrogenase (IDH) and epidermal growth factor receptor 2 (EGFR2) are emerging targeted therapies. In addition, researches have indicated that immunotherapy has a key function in CCA. There is ongoing research on programmed cell death protein 1 inhibitors (PD-1), chimeric antigen receptor T cells (CAR-T) and tumor-infiltrating leukocyte (TILs). Researches have shown that targeted therapy, immunotherapy, and conventional chemotherapy in CCA had certain mechanistic links, and the combination of those can greatly improve the prognosis of advanced CCA patients. This study aimed to review the research progress of targeted therapy and immunotherapy for CCA.

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Futibatinib for FGFR2 -Rearranged Intrahepatic Cholangiocarcinoma

Cited by 215 publications

References 40 publications

Role of Basic Fibroblast Growth Factor in Cancer: Biological Activity, Targeted Therapies, and Prognostic Value

Role of Basic Fibroblast Growth Factor in Cancer: Biological Activity, Targeted Therapies, and Prognostic Value

A year in pharmacology: new drugs approved by the US Food and Drug Administration in 2022

Revisiting targeted therapy and immunotherapy for advanced cholangiocarcinoma

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