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Drug Evaluation

Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma

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Pages 309-316 | Received 02 Oct 2020, Accepted 11 Dec 2020, Published online: 04 Jan 2021

References

  • Turner N, Grose R. Fibroblast growth factor signalling: from development to cancer. Nat Rev Cancer. 2010 Feb;10(2):116–129.
  • Dodé C, Levilliers J, Dupont JM, et al. Loss-of-function mutations in FGFR1 cause autosomal dominant Kallmann syndrome. Nat Genet. 2003 Apr;33(4):463–465.
  • Rand V, Huang J, Stockwell T, et al. Sequence survey of receptor tyrosine kinases reveals mutations in glioblastomas. Proc Natl Acad Sci U S A. 2005 Oct 4;102(40):14344–14349.
  • Borad MJ, Champion MD, Egan JB, et al. Integrated genomic characterization reveals novel, therapeutically relevant drug targets in FGFR and EGFR pathways in sporadic intrahepatic cholangiocarcinoma. PLoS Genet. 2014 Feb;10(2):e1004135.
  • Abou-Alfa GK, Sahai V, Hollebecque A, et al. Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study. Lancet Oncol. 2020 May;21(5):671–684.
  • Hoy SM. Pemigatinib: first approval. Drugs. 2020 Jun;80(9):923–929.
  • Javle M, Lowery M, Shroff RT, et al. Phase II Study of BGJ398 in patients with FGFR-altered advanced cholangiocarcinoma. J Clin Oncol. 2018 Jan 20;36(3):276–282.
  • Chae YK, Ranganath K, Hammerman PS, et al. Inhibition of the fibroblast growth factor receptor (FGFR) pathway: the current landscape and barriers to clinical application. Oncotarget. 2017 Feb 28;8(9):16052–16074.
  • Bockorny B, Rusan M, Chen W, et al. RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade. Mol Cancer Ther. 2018 Jul;17(7):1526–1539.
  • Guagnano V, Kauffmann A, Wöhrle S, et al., FGFR Genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov. 2012;2(12): 1118–1133.
  • Mohammadi M, Froum S, Hamby JM, et al. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. Embo J. 1998 Oct 15;17(20):5896–5904.
  • Huynh H, Lee LY, Goh KY, et al. Infigratinib mediates vascular normalization, impairs metastasis, and improves chemotherapy in hepatocellular carcinoma. Hepatology. 2019 Mar;69(3):943–958.
  • Nogova L, Sequist LV, Garcia JMP, et al. Evaluation of BGJ398, a fibroblast growth factor receptor 1-3 kinase inhibitor, in patients with advanced solid tumors harboring genetic alterations in fibroblast growth factor receptors: results of a global phase I, dose-escalation and dose-expansion study. J clin oncol. 2017;35(2):157–165.
  • Gattineni J, Bates C, Twombley K, et al. FGF23 decreases renal NaPi-2a and NaPi-2c expression and induces hypophosphatemia in vivo predominantly via FGF receptor 1. Am J Physiol Renal Physiol. 2009 Aug;297(2):F282–91.
  • Wheler JJ, Atkins JT, Janku F, et al., Presence of both alterations in FGFR/FGF and PI3K/AKT/mTOR confer improved outcomes for patients with metastatic breast cancer treated with PI3K/AKT/mTOR inhibitors. Oncoscience. 2016;3(5–6): 164–172.
  • Hyman DM, Tran B, Jaime JC, et al. Phase Ib study of BGJ398 in combination with BYL719 in patients (pts) with select advanced solid tumors. J clin oncol. 2016;34(15_suppl):2500.
  • Graham RP, Barr Fritcher EG, Pestova E, et al. Fibroblast growth factor receptor 2 translocations in intrahepatic cholangiocarcinoma. Hum Pathol. 2014 Aug;45(8):1630–1638.
  • Javle M, Sadeghi S, Roychowdhury S, et al. SO-5 Efficacy of second-line chemotherapy in patients with advanced or metastatic cholangiocarcinoma and FGFR2 fusions: A retrospective analysis. Annals of Oncology. 2020 2020/07/01/;31:S219
  • Almquist DR, Javle M, Ciombor KK, et al. 726P - FGFR2 fusions and its effect of patient (pt) outcomes in intrahepatic cholangiocarcinoma (iCCA). Ann Oncol. 2019;30:v279. 2019/10/01/ .
  • Makawita S, K Abou-Alfa G, Roychowdhury S, et al. Infigratinib in patients with advanced cholangiocarcinoma with FGFR2 gene fusions/translocations: the PROOF 301 trial. Future Oncol. 2020 Jun;16(30):25.
  • Lito P, Rosen N, Solit DB. Tumor adaptation and resistance to RAF inhibitors. Nat Med. 2013 Nov;19(11):1401–1409.
  • Wilson FH, Johannessen CM, Piccioni F, et al. A functional landscape of resistance to ALK inhibition in lung cancer. Cancer Cell. 2015 Mar 9;27(3):397–408.
  • Datta J, Damodaran S, Parks H, et al. Akt activation mediates acquired resistance to fibroblast growth factor receptor inhibitor BGJ398. Mol Cancer Ther. 2017 Apr;16(4):614–624.
  • Hu Y, Lu H, Zhang J, et al. Essential role of AKT in tumor cells addicted to FGFR. Anticancer Drugs. 2014 Feb;25(2):183–188.
  • Malchers F, Ercanoglu M, Schütte D, et al. Mechanisms of primary drug resistance in FGFR1-amplified lung cancer. Clin Cancer Res. 2017 Sep 15;23(18):5527–5536.
  • Herrera-Abreu MT, Pearson A, Campbell J, et al. Parallel RNA interference screens identify EGFR activation as an escape mechanism in FGFR3-mutant cancer. Cancer Discov. 2013 Sep;3(9):1058–1071.
  • Byron SA, Chen H, Wortmann A, et al. The N550K/H mutations in FGFR2 confer differential resistance to PD173074, dovitinib, and ponatinib ATP-competitive inhibitors. Neoplasia. 2013 Aug;15(8):975–988.
  • Lau DK, Jenkins L, Weickhardt A. Mechanisms of acquired resistance to fibroblast growth factor receptor targeted therapy. Cancer Drug Resistance. 2019;2(3):568–579.
  • Goyal L, Saha SK, Liu LY, et al. Polyclonal secondary FGFR2 mutations drive acquired resistance to FGFR inhibition in patients with FGFR2 fusion-positive cholangiocarcinoma. Cancer Discov. 2017 Mar;7(3):252–263.
  • Patani H, Bunney TD, Thiyagarajan N, et al. Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use. Oncotarget. 2016;7(17):17.
  • 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 Jul;31(10)2.
  • Wang J, Mikse O, Liao RG, et al. Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells. Oncogene. 2015 Apr 23;34(17):2167–2177.
  • Abel EV, Basile KJ, Kugel CH 3rd, et al. Melanoma adapts to RAF/MEK inhibitors through FOXD3-mediated upregulation of ERBB3. J Clin Invest. 2013 May;123(5):2155–2168.
  • Cowell JK, Qin H, Hu T, et al. Mutation in the FGFR1 tyrosine kinase domain or inactivation of PTEN is associated with acquired resistance to FGFR inhibitors in FGFR1-driven leukemia/lymphomas. Int J Cancer. 2017 Nov 1;141(9):1822–1829.
  • Kim SH, Ryu H, Ock CY, et al. BGJ398, A pan-FGFR inhibitor, overcomes paclitaxel resistance in urothelial carcinoma with FGFR1 overexpression. Int J Mol Sci. 2018 Oct 15;19(10):10.
  • Boichuk S, Dunaev P, Galembikova A, et al. Inhibition of fibroblast growth factor receptor-signaling sensitizes imatinib-resistant gastrointestinal stromal tumors to low doses of topoisomerase II inhibitors. Anticancer Drugs. 2018 Jul;29(6):549–559.
  • Kelly CM, Shoushtari AN, Qin LX, et al. A phase Ib study of BGJ398, a pan-FGFR kinase inhibitor in combination with imatinib in patients with advanced gastrointestinal stromal tumor. Invest New Drugs. 2019 Apr;37(2):282–290.
  • Turkington RC, Longley DB, Allen WL, et al. Fibroblast growth factor receptor 4 (FGFR4): a targetable regulator of drug resistance in colorectal cancer. Cell Death Dis. 2014 Feb 6;5(2):e1046.
  • 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 Aug;9(8):1064–1079.
  • Valle J, Wasan H, Palmer DH, et al. Cisplatin plus gemcitabine versus gemcitabine for biliary tract cancer. N Engl J Med. 2010;362(14):1273–1281.
  • Mazzaferro V, El-Rayes BF, Droz Dit Busset M, et al. Derazantinib (ARQ 087) in advanced or inoperable FGFR2 gene fusion-positive intrahepatic cholangiocarcinoma. Br J Cancer. 2019 Jan;120(2):165–171.
  • Tran B, Meric-Bernstam F, Arkenau HT, et al. Efficacy of TAS-120, an irreversible fibroblast growth factor receptor inhibitor (FGFRi), in patients with cholangiocarcinoma and FGFR pathway alterations previously treated with chemotherapy and other FGFRi’s. Ann Oncol. 2018;29:ix49–ix50.
  • Park JO, Feng Y-H, Chen -Y-Y, et al. Updated results of a phase IIa study to evaluate the clinical efficacy and safety of erdafitinib in Asian advanced cholangiocarcinoma (CCA) patients with FGFR alterations. J clin oncol. 2019;37(15_suppl):4117.

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