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01.12.2022 | AdisInsight Report

Futibatinib: First Approval

verfasst von: Yahiya Y. Syed

Erschienen in: Drugs | Ausgabe 18/2022

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Abstract

Futibatinib (Lytgobi^®) is an oral, covalently binding, irreversible inhibitor of fibroblast growth factor receptor (FGFR)1–4 that is being developed by Taiho Oncology and Taiho Pharmaceutical for the treatment of cancers, including cholangiocarcinoma, breast cancer, gastric cancer, urothelial cancer, oesophageal cancer and non-small cell lung cancer. Futibatinib was approved in the USA on 30 September 2022 for the treatment of adult patients with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harbouring FGFR2 gene fusions or other rearrangements. This article summarizes the milestones in the development of futibatinib leading to this first approval.

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Haugsten EM, Wiedlocha A, Olsnes S, et al. Roles of fibroblast growth factor receptors in carcinogenesis. Mol Cancer Res. 2010;8(11):1439–52.CrossRef

Helsten T, Elkin S, Arthur E, et al. The FGFR landscape in cancer: analysis of 4,853 tumors by next-generation sequencing. Clin Cancer Res. 2016;22(1):259–67.CrossRef

Krook MA, Reeser JW, Ernst G, et al. Fibroblast growth factor receptors in cancer: genetic alterations, diagnostics, therapeutic targets and mechanisms of resistance. Br J Cancer. 2021;124(5):880–92.CrossRef

Bahleda R, Meric-Bernstam F, Goyal L, et al. Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1–4 inhibitor in patients with advanced solid tumors. Ann Oncol. 2020;31(10):1405–12.CrossRef

Taiho Oncology. LYTGOBI® (futibatinib) tablets, for oral use: US prescribing information. 2022. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214801s000lbl.pdf. Accessed 21 Oct 2022.

European Medicines Agency. Medicines for human use under evaluation. 2022. https://www.ema.europa.eu/en/medicines/medicines-human-use-under-evaluation. Accessed 21 Oct 2022.

Taiho Pharmaceutical Co. Taiho Pharmaceutical submits new drug application of FGFR inhibitor futibatinib (TAS-120) for biliary tract cancer [media release]. 28 Jul 2022. http://www.taiho.co.jp.

National Comprehensive Cancer Network. NCCN Oncology Research Program to oversee trials of the FGFR inhibitor futibatinib in tumors with aberrant FGFR expression, in collaboration with Taiho Oncology [media release]. 27 Jan 2020. http://www.nccn.org.

National Comprehensive Cancer Network. NCCN Oncology Research Program announces projects selected for funding to study futibatinib in tumors with aberrant FGFR expression, in collaboration with Taiho Oncology [media release]. 23 Jul 2020. http://www.nccn.org.

10.

Sootome H, Fujita H, Ito K, et al. Futibatinib Is a novel irreversible FGFR 1–4 inhibitor that shows selective antitumor activity against FGFR-deregulated tumors. Cancer Res. 2020;80(22):4986–97.CrossRef

11.

Kalyukina M, Yosaatmadja Y, Middleditch MJ, et al. TAS-120 cancer target binding: defining reactivity and revealing the first fibroblast growth factor receptor 1 (FGFR1) irreversible structure. ChemMedChem. 2019;14(4):494–500.CrossRef

12.

Sootome H, Miura A, Komori T, et al. Futibatinib (TAS-120) plus chemotherapy demonstrates a synergistic effect across various FGFR-deregulated cancer cell lines and xenograft models [abstract no. 564]. Cancer Res. 2020;80(Suppl 16).

13.

Miura A, Sootome H, Komori T, et al. Synergistic antitumor activity of futibatinib (TAS-120), a FGFR1-4 inhibitor, and PI3K pathway inhibitors [abstract no. 659]. Cancer Res. 2020;80(Suppl 16).

14.

Iwasaki J, Kuramoto T, Komori T. Synergistic antitumor activity of futibatinib, an FGFR1-4 inhibitor, and TAS-117, a selective AKT inhibitor, in FGFR-deregulated cancer models [abstract no. 661]. Cancer Res. 2020;80(Suppl 16).

15.

Goyal L, Shi L, Liu LY, et al. TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion–positive intrahepatic cholangiocarcinoma. Cancer Discov. 2019;9(8):1064–79.CrossRef

16.

Cleary JM, Raghavan S, Wu Q, et al. FGFR2 extracellular domain in-frame deletions are therapeutically targetable genomic alterations that function as oncogenic drivers in cholangiocarcinoma. Cancer Discov. 2021;11(10):2488–505.CrossRef

17.

Hollebecque A, Bridgewater JA, Meric-Bernstam F, et al. Assessment of futibatinib exposure-response (E-R) relationships in patients with advanced solid tumors, including cholangiocarcinoma (CCA) [abstract no. 52P]. Ann Oncol. 2021;32(Suppl 5):S378.CrossRef

18.

Morizane C, Kojima T, Kuboki Y, et al. Phase I study of the irreversible FGFR inhibitor (i) futibatinib (FBN; TAS-120) in Japanese patients (pts) with advanced (adv) solid tumours [abstract no. 544P]. Ann Oncol. 2020;31(Suppl 4):S475.CrossRef

19.

Goyal L, Meric-Bernstam F, Hollebecque A, et al. Primary results of phase 2 FOENIX-CCA2: the irreversible FGFR1-4 inhibitor futibatinib in intrahepatic cholangiocarcinoma (iCCA) with FGFR2 fusions/rearrangements [abstract no. CT010]. Cancer Res. 2021;81(Suppl 13).

20.

Goyal L, Meric-Bernstam F, Hollebecque A, et al. Updated results of the FOENIX-CCA2 trial: efficacy and safety of futibatinib in intrahepatic cholangiocarcinoma (iCCA) harboring FGFR2 fusions/ rearrangements [abstract no. 4009]. J Clin Oncol. 2022;40(Suppl 16).

21.

Valle JW, Hollebecque A, Furuse J, et al. FOENIX-CCA2 quality of life data for futibatinib-treated intrahepatic cholangiocarcinoma (iCCA) patients with FGFR2 fusions/rearrangements [abstract no. 4097]. J Clin Oncol. 2021;39(Suppl 15).

22.

Borad MJ, Paine A, Wacheck V, et al. Indirect treatment comparison of futibatinib with chemotherapy and pemigatinib in cholangiocarcinoma with FGFR2 fusions/rearrangements [abstract no. 440]. J Clin Oncol. 2022;40(Suppl 4).

23.

Meric-Bernstam F, Bahleda R, Hierro C, et al. Futibatinib, an irreversible FGFR1-4 inhibitor, in patients with advanced solid tumors harboring FGF/FGFR aberrations: a phase I dose-expansion study. Cancer Discov. 2022;12(2):402–15.CrossRef

24.

Kuboki Y, Shitara K, Morizane C, et al. Phase I study of the irreversible FGFR inhibitor futibatinib in Japanese patients with advanced solid tumors: updated dose expansion results and activity in gastric cancer [abstract no. 1383P]. Ann Oncol. 2021;32(Suppl 5):S1047–8.CrossRef

25.

Muro K, Kato K, Chin K, et al. Phase Ib study of futibatinib plus pembrolizumab in patients with advanced or metastatic solid tumors: tolerability results and antitumor activity in esophageal carcinoma [abstract no. 1241P]. Ann Oncol. 2022;33(Suppl 7):S1116.CrossRef

26.

Damodaran S, Unni N, Giridhar KV, et al. Futibatinib in combination with fulvestrant in patients with metastatic breast cancer (MBC) harboring high-level FGFR1 amplification: preliminary data from a phase 2 study [abstract no. P1-18-35]. Cancer Res. 2022;82(Suppl 4).

27.

Koshkin VS, Sonpavde GP, Hwang C, et al. Futibatinib plus pembrolizumab in patients (pts) with advanced or metastatic urothelial carcinoma (mUC): preliminary safety results from a phase 2 study [abstract no. 501]. J Clin Oncol. 2022;40(Suppl 6).

28.

Meric-Bernstam F, Furuse J, Oh D, et al. Pooled analysis safety profile of futibatinib in patients with advanced solid tumors, including intrahepatic cholangiocarcinoma (iCCA) [abstract no. 51P]. Ann Oncol. 2021;32(Suppl 5):S378.CrossRef

29.

Taiho Oncology. FDA approves Taiho's LYTGOBI® (futibatinib) tablets for previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma [media release]. 30 Sep 2022 2022. http://www.taihooncology.com.

Titel: Futibatinib: First Approval
verfasst von: Yahiya Y. Syed
Publikationsdatum: 01.12.2022
Verlag: Springer International Publishing
Erschienen in: Drugs / Ausgabe 18/2022
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI: https://doi.org/10.1007/s40265-022-01806-z

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Futibatinib: First Approval

Abstract

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Abstract

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