References
- Siegel RL, Miller KD, Jemal A. Cancer Statistics, 2017. CA Cancer J Clin. 2017;67:7–30.
- Morgensztern D, Ng SH, Gao F, et al. Trends in stage distribution for patients with non-small cell lung cancer: a national cancer database survey. J Thorac Oncol. 2010;5:29–33.
- Canadian Cancer Society’s Steering Committee. Canadian cancer statistics 2010. Toronto, ON: Canadian Cancer Society; 2010.
- Cihoric N, Savic S, Schneider S. et al. Prognostic role of FGFR1amplification in early-stage non-small cell lung cancer. Br J Cancer. 2014;110:2914–2922.
- Biello F, Burrafato G, Rijavec E, et al. Fibroblast Growth Factor Receptor (FGFR): a new target for non-small cell lung cancer therapy. Anticancer Agents Med Chem. 2016;16:1142–1154.
- Sleeman M, Fraser J, McDonald M, et al. Identification of a new fibroblast growth factor receptor, FGFR5. Gene. 2001;271:171–182.
- Chen Y, Li S, Berezin V, et al. The fibroblast growth factor receptor (FGFR) agonist FGF1 and the neural cell adhesion molecule-derived peptide FGL activate FGFR substrate 2alpha differently. J Neurosci Res. 2010;88:1882–1889.
- Chen Y, Li X, Eswarakumar VP, et al. Fibroblast growth factor (FGF) signaling through PI 3-kinase and Akt/PKB is required for embryoid body differentiation. Oncogene. 2000;19:3750–3756.
- Touat M, Ileana E, Postel-Vinay S, et al. Targeting FGFR signaling in cancer. Clin Cancer Res. 2015;21:2684–2694.
- 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. 2016. Epub ahead of print.
- 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;22:259–267.
- Seo AN, Jin Y, Lee HJ, et al. FGFR1 amplification is associated with poor prognosis and smoking in non-small-cell lung cancer. Virchows Arch. 2014;465:547–558.
- Slodkowska J, Sikora J, Roszkowski-Sliz K, et al. Expression of vascular endothelial growth factor and basic fibroblast growth factor receptors in lung cancer. Anal Quant Cytol Histol. 2000;22:398–402.
- Ware KE, Hinz TK, Kleczko E. et al. A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop. Oncogenesis. 2013;2;e39.
- Bello E, Colella G, Scarlato V, et al. E3810 is a potent dual inhibitor of VEGFR and FGFR that exert antitumor activity in multiple preclinical models. Cancer Res. 2011;71:1396–1405.
- Soria J-C, DeBraud F, Bahleda R, et al. Phase I/IIa study evaluating the safety, efficacy, pharmacokinetics, and pharmacodynamics of lucitanib in advanced solid tumors. Ann Oncol. 2014;25:2244–2251.
- Spigel DR, Cereda R, Litten JB, et al. A single arm, open-label, phase II study to assess the efficacy of lucitanib in patients with FGFR1-amplified squamous NSCLC (sqNSCLC). J Clin Oncol. 2014;32(Suppl):abstractTPS8119.
- NCT02109016. A study to assess the efficacy and safety of the VEGFR-FGFR inhibitor, Lucitanib, given to patients with advanced/metastatic lung cancer and FGF, VEGF, or PDGF related genetic alterations. [cited 2017 Apr7]. Available from:https://clinicaltrials.gov/ct2/show/NCT02109016?term=lucitanib+and+nsclc&rank=1
- Nishio M, Horai T, Horiike A, et al. Phase 1 study of lenvatinib combined with carboplatin and paclitaxel in patients with non-small-cell lung cancer. Br J Cancer. 2013;109:538–544.
- Havel L, Lee J-S, Lee KH, et al. E7080 (lenvatinib) in addition to best supportive care (BSC) versus BSC alone in third-line or greater nonsquamous, non-small cell lung cancer (NSCLC). J Clin Oncol. 2014;32(Suppl):abstract8043.
- NCT03006887. An open-label phase 1b trial of lenvatinib plus pembrolizumab in subjects with selected solid tumors. [cited 2017 Apr7]. Available from:https://clinicaltrials.gov/ct2/show/NCT03006887?term=lenvatinib+and+nsclc&rank=4
- NCT02501096. A multicenter, open-label phase 1b/2 trial of Lenvatinib (E7080) plus pembrolizumab in subjects with selected solid tumors. [cited 2017 Apr7]. Available from:https://clinicaltrials.gov/ct2/show/NCT02501096?term=lenvatinib+and+nsclc&rank=3
- NCT01877083. A multicenter, open-label phase 2 study of the safety and activity of lenvatinib (E7080) in subjects with KIF5B-RET-positive adenocarcinoma of the lung. [cited 2017 Apr7]. Available from:https://clinicaltrials.gov/ct2/show/NCT01877083?term=lenvatinib+and+nsclc&rank=5
- Lee SH, Lopes De Menezes D, Vora J, et al. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Clin Cancer Res. 2005;11:3633–3641.
- Lim SH, Sun JM, Choi YL, et al. Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study. Cancer. 2016;122:3024–3031.
- Fischer H, Taylor N, Allerstorfer S, et al. Fibroblast growth factor receptor-mediated signals contribute to the malignant phenotype of non-small cell lung cancer cells: therapeutic implications and synergism with epidermal growth factor receptor inhibition. Mol Cancer Ther. 2008;7:3408–3419.
- Das M, Padda SK, Frymoyer A, et al. Dovitinib and erlotinib in patients with metastatic non-small cell lung cancer: A drug-drug interaction. Lung Cancer. 2015;89:280–286.
- Semrad TJ, Kim EJ, Tanaka MS, et al. Phase II study of dovitinib in patients (Pts) progressing on anti-vascular endothelial growth factor (VEGF) therapy. J Clin Oncol. 2016;34(Suppl):abstract 616.
- Hilberg F, Roth GJ, Krssak M, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008;68:4774–4782.
- Okamoto I, Miyazaki M, Takeda M, et al. Tolerability of nintedanib (BIBF 1120) in combination with docetaxel: a phase 1 study in Japanese patients with previously treated non-small-cell lung cancer. J Thorac Oncol. 2015;10:346–352.
- Ellis PM, Kaiser R, Zhao Y, et al. Phase I open-label study of continuous treatment with BIBF 1120, a triple angiokinase inhibitor, and pemetrexed in pretreated non-small cell lung cancer patients. Clin Cancer Res. 2010;16:2881–2889.
- Daga H, Takeda K, Okada H, et al. Phase I study of nintedanib in combination with pemetrexed as second-line treatment of Japanese patients with advanced non-small cell lung cancer. Cancer Chem Pharmacol. 2015;76:1225–1233.
- Reck M, Kaiser R, Mellemgaard A. et al. Docetaxel plus nintedanib versus docetaxel plus placebo in patients with previously treated non-small-cell lung cancer (LUME-Lung 1): a phase 3, double-blind, randomized controlled trial. Lancet Oncol. 2014;15:143–155.
- Hanna NH, Kaiser R, Sullivan RN, et al. Nintedanib plus pemetrexed versus placebo plus pemetrexed in patients with relapsed or refractory, advanced non-small cell lung cancer (LUME-Lung 2): A randomized, double-blind, phase III trial. Lung Cancer. 2016;102:65–73.
- Ren M, Hong M, Liu G, et al. Novel FGFR inhibitor ponatinib suppresses the growth of non-small cell lung cancer cells overexpressing FGFR1. Oncol Rep. 2013;29:2181–2190.
- NCT 01761747. Phase II study of ponatinib in advanced lung and head and neck cancers with FGFR kinase alterations. [cited 2017 Apr7]. Available from: https://clinicaltrials.gov/ct2/show/record/NCT01761747?term=ponatinib+and+nsclc&rank=3
- NCT01935336. A phase II study of ponatinib in cohorts of patients with lung cancer preselected using different candidate predictive biomarkers. [cited 2017 Apr7]. Available from: https://clinicaltrials.gov/ct2/show/NCT01935336?term=ponatinib+and+nsclc&rank=2
- Dy GK, Mandrekar SJ, Nelson GD, et al. A randomized phase II study of gemcitabine and carboplatin with or without cediranib as first-line therapy in advanced non-small-cell lung cancer: north central cancer treatment group study N0528. J Thorac Oncol. 2013;8:79–88.
- Goss GD, Arnold A, Shepherd FA, et al. Randomized, double-blind trial of carboplatin and paclitaxel with either daily oral cediranib or placebo in advanced non-small-cell lung cancer: NCIC clinical trials group BR24 study. J Clin Oncol. 2010;28:49–55.
- Laurie SA, Solomon BJ, Seymour L, et al. Randomised, double-blind trial of carboplatin and paclitaxel with daily oral cediranib or placebo in patients with advanced non-small cell lung cancer: NCIC clinical trials group study BR29. Eur J Cancer. 2014;50:706–712.
- Göke A, Göke R, Ofner A, et al. The FGFR inhibitor NVP-BGJ398 induces NSCLC cell death by activating caspase-dependent pathways as well as Caspase-independent apoptosis. Anticancer Res. 2015;35:5873–5879.
- Nogova L, Sequist LV, Perez Garcia JM, 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;35:157–165.
- NCT02160041. Modular phase II study to link targeted therapy to patients with pathway activated tumors: module 6 - BGJ398 for patients with tumors with FGFR genetic alterations. [cited 2017 Apr7]. Available from: https://clinicaltrials.gov/ct2/show/NCT02160041?term=bgj398&rank=1
- 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(Suppl):abstract2500.
- Gavine PR, Mooney L, Kilgour E, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012;72:2045–2056.
- Delpuech O, Rooney C, Mooney L, et al. Identification of pharmacodynamic transcript biomarkers in response to FGFR inhibition by AZD4547. Mol Cancer Ther. 2016;15:2802–2813.
- Andre F, Ranson M, Dean E, et al. Results of a phase I study of AZD4547, an inhibitor of fibroblast growth factor receptor (FGFR), in patients with advanced solid tumors. Cancer Res. 2013;73(Suppl):abstract: LB-145.
- Paik PK, Shen R, Ferry D, et al. A phase 1b open-label multicenter study of AZD4547 in patients with advanced squamous cell lung cancers: preliminary antitumor activity and pharmacodynamic data. J Clin Oncol. 2014;32(Suppl):abstract:8035.
- NCT01824901. A phase I/randomized phase II study of docetaxel with or without AZD4547 in recurrent FGFR1-amplified squamous Non-Small Cell Lung Cancer. [cited 2017 Apr7]. Available from: https://clinicaltrials.gov/ct2/show/study/NCT01824901?term=azd4547+and+nsclc&rank=1
- Saka H, Kitagawa C, Kogure Y. et al.Safety, tolerability and pharmacokinetics of the fibroblast growth factor receptor inhibitor AZD4547 in Japanese patients with advanced solid tumours: a Phase I study. Invest New Drugs. 2017. Epub ahead of print.
- NCT02117167. Intergroup Trial UNICANCER UC 0105-1305/ IFCT 1301: SAFIR02_lung - evaluation of the efficacy of high throughput genome analysis as a therapeutic decision tool for patients with metastatic non-small cell lung cancer. [cited 2017 Apr 7]. Available from: https://clinicaltrials.gov/ct2/show/NCT02117167?term=azd4547+and+nsclc&rank=2
- NCT02664935. National lung matrix trial: multi-drug, genetic marker-directed, non-comparative, multi-centre, multi-arm phase II trial in non-small cell lung cancer. [cited 2017 Apr 7]. Available from: https://clinicaltrials.gov/ct2/show/NCT02664935?term=azd4547+and+nsclc&rank=3
- Nakanishi Y, Akiyama N, Tsukaguchi T, et al. The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014;13:2547–2558.
- Zanna C, Vaslin A, Henner Voss M, et al. Preliminary clinical pharmacokinetics and pharmacodynamics of Debio 1347 (CH5183284), a novel FGFR inhibitor. J Clin Oncol. 2015;33(Suppl):abstract:2540.
- Zhao G, Li WY, Chen D, et al. A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. Mol Cancer Ther. 2011;10:2200–2210.
- Wu D, Guo M, Philips MA, et al. Crystal Structure of the FGFR4/LY2874455 complex reveals insights into the pan-FGFR selectivity of LY2874455. Plos One. 2016;11.
- Tie J, Bang Y-J, Park YS, et al. Phase I study of LY2874455, a fibroblast growth factor (FGF) receptor inhibitor, in patients with advanced cancer. Cancer Res. 2014;74(19 Supplement):CT215.
- Tie J, Bang Y-J, Park YS, et al. Phase I study of LY2874455, a fibroblast growth factor (FGF) receptor inhibitor, in patients with advanced cancer. Cancer Res. 2016;76(14 Supplement):CT058.
- Hall TG, Yu Y, Eathiraj S, et al. Preclinical activity of ARQ 087, a novel inhibitor targeting FGFR dysregulation. Plos One. 2016;11.
- Papadopoulos KP, Tolcher AW, Patnaik A, et al. Phase 1, first-in-human study of ARQ 087, an oral pan-fibroblast growth factor receptor (FGFR) inhibitor, in patients (pts) with advanced solid tumors. J Clin Oncol. 2015;33(Suppl):abstract2545.
- Perera T, Jovcheva E, Vialard J, et al. JNJ-42756493 is an inhibitor of FGFR-1, 2, 3 and 4 with nanomolar affinity for targeted therapy. Cancer Res. 2014;74(19 Supplement):1738.
- Tabernero J, Bahleda R, Dienstmann R, et al. Phase I dose-escalation study of JNJ-42756493, an oral pan-Fibroblast Growth Factor Receptor inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2015;33:3401–3408.
- NCT02699606. A phase 2a study to evaluate the clinical efficacy of JNJ-42756493, a pan-Fibroblast Growth Factor Receptor (FGFR) tyrosine kinase inhibitor, in Asian patients with advanced non-small-cell lung cancer, urothelial cancer, gastric cancer, esophageal cancer or cholangiocarcinoma. [cited 2017 Apr 7]. Available from: https://clinicaltrials.gov/ct2/show/NCT02699606?term=JNJ%E2%80%9042756493&rank=10
- Ochiiwa H, Fujita H, Itoh K, et al. TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. Mol Cancer Ther. 2013;12(11 Supplement):A270.
- NCT02052778. A dose-finding phase 1 study of TAS-120 in patients with advanced solid tumors with or without Fibroblast Growth Factor/Receptor (FGF/FGFR)-related abnormalities followed by a phase 2 study in patients with advanced solid tumors or multiple myeloma with FGF/FGFR-related abnormalities. [cited 2017 Apr 7]. Available from: https://clinicaltrials.gov/ct2/show/NCT02052778?term=NCT02052778&rank=1
- Bai A, Meetze K, Vo NY, et al. GP369, an FGFR2-IIIb-specific antibody, exhibits potent antitumor activity against human cancers driven by activated FGFR2 signaling. Cancer Res. 2010;70:7630–7639.
- Trudel S, Bergsagel PL, Singhal S, et al. A phase I study of the safety and pharmacokinetics of escalating doses of MFGR1877S, a fibroblast growth factor receptor 3 (FGFR3) antibody, in patients with relapsed or refractory t(4;14)-positive multiple myeloma. Blood. 2012;120:4029.
- O’Donnell P, Goldman JW, Gordon MS, et al. A phase I dose escalation study of MFGR1877S, a human monoclonal anti-fibroblast growth factor 3 (FGFR3) antibody, in patients (pts) with advanced solid tumors. Eur J Cancer. 2012;48(Suppl. 6):621.
- Blackwell C, Sherk C, Fricko M, et al. Inhibition of FGF/FGFR autocrine signaling in mesothelioma with the FGF ligand trap, FP-1039/GSK3052230. Oncotarget. 2016;7:39861–39871.
- Tolcher AW, Papadopoulos KP, Patnaik A, et al. A phase I, first in human study of FP-1039(GSK3052230), a novel FGF ligand trap, in patients with advanced solid tumors. Ann Oncol. 2016;27:526–532.
- NCT01868022. Multi-arm, non-randomized, open-label phase IB study to evaluate GSK3052230 in combination with paclitaxel and carboplatin, or docetaxel or as single agent in subjects with solid malignancies and deregulated FGF pathway signaling. [cited 2017 Apr 7]. Available from: https://clinicaltrials.gov/ct2/show/NCT01868022?term=fp-1039&rank=4
- Yanochko GM, Vitsky A, Heyen JR, et al. Pan-FGFR inhibition leads to blockade of FGF23 signaling, soft tissue mineralization, and cardiovascular dysfunction. Toxicol Sci. 2013;135:451–464.
- Hierro C, Rodon J, Tabernero J. Fibroblast Growth Factor (FGF) Receptor/FGF Inhibitors: novel targets and strategies for optimization of response of solid tumors. Semin Oncol. 2015;42:801–819.
- Kotani H, Ebi H, Kitai H, et al. Co-active receptor tyrosine kinases mitigate the effect of FGFR inhibitors in FGFR1-amplified lung cancers with low FGFR1 protein expression. Oncogene. 2016;35:3587–3597.
- Wynes MW, Hinz TK, Gao D, et al. FGFR1 mRNA and protein expression, not gene copy number, predict FGFR TKI sensitivity across all lungca ncer histologies. Clin Cancer Res. 2014;20:3299–3309.
- Sohl CD, Ryan MR, Luo B, et al. Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles’ heel of targeted therapy. ACS Chem Biol. 2015;10:1319–1329.
- Wang L, Šuštić T, Leite De Oliveira R. et al.A functional genetic screen identifies the phosphoinositide 3-kinase Pathway as a determinant of resistance to fibroblast growth factor receptor inhibitors in FGFR mutant urothelial cell carcinoma. Eur Urol. 2017. Epub ahead of print.
- Azuma K, Kawahara A, Sonoda K, et al. FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor. Oncotarget. 2014;5:5908–5919.