References
- I. S. Babina and N. C. Turner, Advances and challenges in targeting FGFR signalling in cancer, Nat. Rev. Cancer 17 (2017) 318–332; https://doi.org/10.1038/nrc.2017.8
- Q. Liang, J. Wang, L. Zhao, J. Hou, Y. Hu and J. Shi, Recent advances of dual FGFR inhibitors as a novel therapy for cancer, Eur. J. Med. Chem. 214 (2021) Article ID 113205; https://doi.org/10.1016/j.ejmech.2021.113205
- J. Zheng, W. Zhang, L. Li, Yi He, Y. Wei, Y. Dang, S. Nie and Z. Guo, Signaling pathway and small-molecule drug discovery of FGFR: A comprehensive review, Front. Chem. 10 (2022) Article ID 860985 (24 pages); https://doi.org/10.3389/fchem.2022.860985
- M. Goldfarb, J. Schoorlemmer, A. Williams, S. Diwakar, Q. Wang, X. Huang, J. Giza, D. Tchetchik, K. Kelley, A. Vega, G. Matthews, P. Rossi, D. M. Ornitz and E. D’Angelo, Fibroblast growth factor homologous factors control neuronal excitability through modulation of voltage-gated sodium channels, Neuron 55 (2007) 449–463; https://doi.org/10.1016/j.neuron.2007.07.006
- A. A. Belov and M. Mohammadi, Molecular mechanisms of fibroblast growth factor signaling in physiology and pathology, Cold Spring Harb. Perspect. Biol. 5 (2013) Article ID a015958 (24 pages); https://doi.org/10.1101/cshperspect.a015958
- D. M. Ornitz, FGFs, heparan sulfate and FGFRs: complex interactions essential for development, Bioessays 22 (2000) 108–112; https://doi.org/10.1002/(SICI)1521-1878(200002)22:2<108::AID-BIES2>3.0.CO;2-M
- I. Fernandes-Freitas and B. M. Owen, Metabolic roles of endocrine fibroblast growth factors, Curr. Opin. Pharmacol. 25 (2015) 30–35; https://doi.org/https://doi.org/10.1016/j.coph.2015.09.014
- N. K. Jain and K. S. Baghel, Selective cyclooxygenase-2 inhibitor etoricoxib attenuated hypoxic cancer milieu induced m2-polarization of macrophages and acquisition of pro-angiogenic and proinvasive attributes, Res. J. Pharm. Technol. 12 (2019) 5871–5877.
- N. Wang, J.-Y. Li, S. Li, X.-C. Guo, T. Wu, W.-F. Wang and D.-S. Li, Fibroblast growth factor 21 regulates foam cells formation and inflammatory response in Ox-LDL-induced THP-1 macrophages, Biomed. Pharmacother. 108 (2018) 1825–1834; https://doi.org/10.1016/j.biopha.2018.09.143
- A. Kommalapati, S. H. Tella, M. Borad, M. Javle and A. Mahipal, FGFR inhibitors in oncology: Insight on the management of toxicities in clinical practice, Cancers (Basel) 13(12) (2021) Article ID 2968 (18 pages); https://doi.org/10.3390/cancers13122968
- F.-T. Liu, N.-G. Li, Y.-M. Zhang, W.-C. Xie, S.-P. Yang, T. Lu and Z.-H. Shi, Recent advance in the development of novel, selective and potent FGFR inhibitors, Eur. J. Med. Chem. 186 (2020) Article ID 111884; https://doi.org/10.1016/j.ejmech.2019.111884
- R. J. Roskoski, The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder, Pharmacol. Res. 151 (2020) Article ID 104567 (91 pages); https://doi.org/10.1016/j.phrs.2019.104567
- D. M. Ornitz and N. Itoh, The fibroblast growth factor signaling pathway, WIREs Dev. Biol. 4(3) (2015) 215–266; https://doi.org/10.1002/wdev.176
- R. Dienstmann, J. Rodon, A. Prat, J. Perez-Garcia, B. Adamo, E. Felip, J. Cortes, A. J. Iafrate, P. Nuciforo and J. Tabernero, Genomic aberrations in the FGFR pathway: opportunities for targeted therapies in solid tumors, Ann. Oncol. 25 (2014) 552–563; https://doi.org/https://doi.org/10.1093/annonc/mdt419
- D. Roy Burman, S. Das, C. Das and R. Bhattacharya, Alternative splicing modulates cancer aggressiveness: role in EMT/metastasis and chemoresistance, Mol. Biol. Rep. 48 (2021) 897–914; https://doi.org/10.1007/s11033-020-06094-y
- K. Holzmann, T. Grunt, C. Heinzle, S. Sampl, H. Steinhoff, N. Reichmann, M. Kleiter, M. Hauck and B. Marian, Alternative splicing of fibroblast growth factor receptor IgIII loops in cancer, J. Nucleic Acids 2012 (2012) Article ID 950508 (13 pages); https://doi.org/10.1155/2012/950508
- K. S. Baghel, B. N. Tewari, R. Shrivastava, S. A. Malik, M. U.-D. Lone, N. K. Jain, C. Tripathi, R. K. Kanchan, S. Dixit, K. Singh, K. Mitra, M. P. S. Negi, M. Srivastava, S. Misra, M. L. B. Bhatt and S. Bhadauria, Macrophages promote matrix protrusive and invasive function of breast cancer cells via MIP-1β dependent upregulation of MYO3A gene in breast cancer cells, Oncoimmunology 5 (2016) e1196299 (18 pages); https://doi.org/10.1080/2162402X.2016.1196299
- M. A. Lemmon and J. Schlessinger, Cell signaling by receptor tyrosine kinases, Cell 141 (2010) 1117–1134; https://doi.org/10.1016/j.cell.2010.06.011
- S. Mandal, S. Bandyopadhyay, K. Tyagi and A. Roy, Recent advances in understanding the molecular role of phosphoinositide-specific phospholipase C gamma 1 as an emerging onco-driver and novel therapeutic target in human carcinogenesis, Biochim. Biophys. Acta Rev. Cancer 1876(2) (2021) Article ID 188619; https://doi.org/10.1016/j.bbcan.2021.188619
- M. Mossahebi-Mohammadi, M. Quan, J.-S. Zhang and X. Li, FGF signaling pathway: A key regulator of stem cell pluripotency, Front. Cell Dev. Biol. 8 (2020) Article ID 79 (10 pages); https://doi.org/10.3389/fcell.2020.00079
- H. R. Ferguson, M. P. Smith and C. Francavilla, Fibroblast growth factor receptors (FGFRs) and noncanonical partners in cancer signaling, Cells 10(5) (2021) Article ID 1201 (35 pages); https://doi.org/10.3390/cells10051201
- P. Dubey, R. Shrivastava, C. Tripathi, N. K. Jain, B. N. Tewari, M.-U.-D. Lone, K. S. Baghel, V. Kumar, S. Misra, S. Bhadauria and M. L. B. Bhatt, Cyclooxygenase-2 inhibition attenuates hypoxic cancer cells induced m2-polarization of macrophages, Cell. Mol. Biol. (Noisy-le-grand) 60 (2014) 10–15.
- N. K. Jain, M. Tailang, H. K. Jain, B. Chandrasekaran, B. M. Sahoo, A. Subramanian, N. Thangavel, A. Aldahish, K. Chidambaram, M. Alagusundaram, S. Kumar and P. Selvam, Therapeutic implications of current Janus kinase inhibitors as anti-COVID agents: A review, Front. Pharmacol. 14 (2023) Article ID 1135145; https://doi.org/10.3389/fphar.2023.1135145
- N. Su, M. Jin and L. Chen, Role of FGF/FGFR signaling in skeletal development and homeostasis: learning from mouse models, Bone Res. 2 (2014) Article ID 14003 (24 pages); https://doi.org/10.1038/boneres.2014.3
- M. Katoh, Fibroblast growth factor receptors as treatment targets in clinical oncology, Nat. Rev. Clin. Oncol. 16 (2019) 105–122; https://doi.org/10.1038/s41571-018-0115-y
- T. Helsten, S. Elkin, E. Arthur, B. N. Tomson, J. Carter and R. Kurzrock, The FGFR landscape in cancer: Analysis of 4,853 tumors by next-generation sequencing, Clin. Cancer Res. 22(1) (2016) 259–267; https://doi.org/10.1158/1078-0432.CCR-14-3212
- W. Gu, J. Yang, Y. Wang, J. Xu, X. Wang, F. Du, X. Hu, H. Guo, C. Song, R. Tao and X. Zhang, Comprehensive identification of FGFR1-4 alterations in 5 557 Chinese patients with solid tumors by next-generation sequencing, Am. J. Cancer Res. 11 (2021) 3893–3906.
- N. K. Jain, A. Agrawal, G. T. Kulkarni and M. Tailang, Molecular docking study on phytoconstituents of traditional ayurvedic drug Tulsi (Ocimum sanctum L.) against COVID-19 Mpro enzyme: An in silico study, Int. J. Pharm. Pharm. Sci. 14(4) (2022) 44–50; https://doi.org/10.22159/ijpps.2022v14i4.43181
- R. Porta, R. Borea, A. Coelho, S. Khan, A. Araújo, P. Reclusa, T. Franchina, N. Van Der Steen, P. Van Dam, J. Ferri, R. Sirera, A. Naing, D. Hong and C. Rolfo, FGFR a promising druggable target in cancer: Molecular biology and new drugs, Crit. Rev. Oncol. Hematol. 113 (2017) 256–267; https://doi.org/10.1016/j.critrevonc.2017.02.018
- M. Touat, E. Ileana, S. Postel-Vinay, F. André and J.-C. Soria, Targeting FGFR signaling in cancer, Clin. Cancer Res. 21(12) (2015) 2684–2694; https://doi.org/10.1158/1078-0432.CCR-14-2329
- L. M. de Almeida Carvalho, S. de Oliveira Sapori Avelar, A. Haslam, J. Gill and V. Prasad, Estimation of percentage of patients with fibroblast growth factor receptor alterations eligible for off-label use of erdafitinib, JAMA Netw. Open 2(11) (2019) e1916091 (10 pages); https://doi.org/10.1001/jamanetworkopen.2019.16091
- A. Weaver and J. B. Bossaer, Fibroblast growth factor receptor (FGFR) inhibitors: A review of a novel therapeutic class, J. Oncol. Pharm. Pract. 27(3) (2021) 702–710; https://doi.org/10.1177/1078155220983425
- L. Huang, S. Jiang and Y. Shi, Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020), J. Hematol. Oncol. 13(1) (2020) Article ID 143 (23 pages); https://doi.org/10.1186/s13045-020-00977-0
- R. Roskoski, Jr., Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes, Pharmacol. Res. 103 (2016) 26–48; https://doi.org/10.1016/j.phrs.2015.10.021
- K. S. Bhullar, N. O. Lagarón, E. M. McGowan, I. Parmar, A. Jha, B. P. Hubbard and H. P. V. Rupasinghe, Kinase-targeted cancer therapies: progress, challenges and future directions, Mol. Cancer 17 (2018) Article ID 48 (20 pages); https://doi.org/10.1186/s12943-018-0804-2
- R. Roskoski, Jr., Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update, Pharmacol. Res. 187 (2023) Article ID 106552 (21 pages); https://doi.org/10.1016/j.phrs.2022.106552
- P. R. Gavine, L. Mooney, E. Kilgour, A. P. Thomas, K. Al-Kadhimi, S. Beck, C. Rooney, T. Coleman, D. Baker, M. J. Mellor, A. N. Brooks and T. Klinowska, AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family, Cancer Res. 72 (2012) 2045–2056; https://doi.org/10.1158/0008-5472.CAN-11-3034
- J. A. Tucker, T. Klein, J. Breed, A. L. Breeze, R. Overman, C. Phillips and R. A. Norman, Structural insights into FGFR kinase isoform selectivity: diverse binding modes of AZD4547 and ponatinib in complex with FGFR1 and FGFR4, Structure 22 (2014) 1764–1774; https://doi.org/10.1016/j.str.2014.09.019
- A. Tyulyandina, D. Harrison, W. Yin, E. Stepanova, D. Kochenkov, E. Solomko, N. Peretolchina, F. Daeyaert, J.-B. Joos, K. Van Aken, M. Byakhov, E. Gavrilova, S. Tjulandin and I. Tsimafeyeu, Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies, Invest. New Drugs 35 (2017) 127–133; https://doi.org/10.1007/s10637-016-0404-1
- C. Herbert, U. Schieborr, K. Saxena, J. Juraszek, F. De Smet, C. Alcouffe, M. Bianciotto, G. Saladino, D. Sibrac, D. Kudlinzki, S. Sreeramulu, A. Brown, P. Rigon, J.-P. Herault, G. Lassalle, T. L. Blundell, F. Rousseau, A. Gils, J. Schymkowitz, P. Tompa, J.-M. Herbert, P. Carmeliet, F. L. Gervasio, H. Schwalbe and F. Bono, Molecular mechanism of SSR128129E, an extracellularly acting, small-molecule, allosteric inhibitor of FGF receptor signaling., Cancer Cell 23 (2013) 489–501; https://doi.org/10.1016/j.ccr.2013.02.018
- H. Patani, T. D. Bunney, N. Thiyagarajan, R. A. Norman, D. Ogg, J. Breed, P. Ashford, A. Potterton, M. Edwards, S. V. Williams, G. S. Thomson, C. S. M. Pang, M. A. Knowles, A. L. Breeze, C. Orengo, C. Phillips and M. Katan, Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use, Oncotarget 7 (2016) 24252–24268; https://doi.org/10.18632/oncotarget.8132
- T. P. S. Perera, E. Jovcheva, L. Mevellec, J. Vialard, D. De Lange, T. Verhulst, C. Paulussen, K. Van De Ven, P. King, E. Freyne, D. C. Rees, M. Squires, G. Saxty, M. Page, C. W. Murray, R. Gilissen, G. Ward, N. T. Thompson, D. R. Newell, N. Cheng, L. Xie, J. Yang, S. J. Platero, J. D. Karkera, C. Moy, P. Angibaud, S. Laquerre and M. V. Lorenzi, Discovery and pharmacological characterization of JNJ-42756493 (erdafitinib), a functionally selective small-molecule FGFR family inhibitor, Mol. Cancer Ther. 16 (2017) 1010–1020; https://doi.org/10.1158/1535-7163.MCT-16-0589
- R. Roskoski, Jr., Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update, Pharmacol. Res. 152 (2020) Article ID 104609; https://doi.org/10.1016/j.phrs.2019.104609
- M. Verstraete, A. Debucquoy, A. Gonnissen, R. Dok, S. Isebaert, E. Devos, W. McBride and K. Haustermans, In vitro and in vivo evaluation of the radiosensitizing effect of a selective FGFR inhibitor (JNJ-42756493) for rectal cancer, BMC Cancer 15 (2015) Article ID 946 (11 pages); https://doi.org/10.1186/s12885-015-2000-8
- Y. Loriot, A. Necchi, S. H. Park, J. Garcia-Donas, R. Huddart, E. Burgess, M. Fleming, A. Rezazadeh, B. Mellado, S. Varlamov, M. Joshi, I. Duran, S. T. Tagawa, Y. Zakharia, B. Zhong, K. Stuyckens, A. Santiago-Walker, P. De Porre, A. O’Hagan, A. Avadhani and A. O. Siefker-Radtke (for BLC2001 study group), Erdafitinib in locally advanced or metastatic urothelial carcinoma., N. Engl. J. Med. 381 (2019) 338–348; https://doi.org/10.1056/NEJMoa1817323
- A. O. Siefker-Radtke, A. Necchi, S. H. Park, J. García-Donas, R. A. Huddart, E. F. Burgess, M. T. Fleming, A. Rezazadeh Kalebasty, B. Mellado, S. Varlamov, M. Joshi, I. Duran, S. T. Tagawa, Y. Zakharia, S. Akapame, A. E. Santiago-Walker, M. Monga, A. O’Hagan and Y. Loriot (for BLC2001 study group), Efficacy and safety of erdafitinib in patients with locally advanced or metastatic urothelial carcinoma: long-term follow-up of a phase 2 study, Lancet Oncol. 23 (2022) 248–258; https://doi.org/10.1016/S1470-2045(21)00660-4
- X. Zheng, H. Wang, J. Deng, M. Yao, X. Zou, F. Zhang and X. Ma, Safety and efficacy of the pan-FGFR inhibitor erdafitinib in advanced urothelial carcinoma and other solid tumors: A systematic review and meta-analysis, Front. Oncol. 12 (2023) Article ID 907377 (16 pages); https://doi.org/10.3389/fonc.2022.907377
- A.-G. Dosne, E. Valade, N. Goeyvaerts, P. De Porre, A. Avadhani, A. O’Hagan, L. Y. Li, D. Ouellet and J. J. Perez Ruixo, Exposure-response analyses of erdafitinib in patients with locally advanced or metastatic urothelial carcinoma, Cancer Chemother. Pharmacol. 89 (2022) 151–164; https://doi.org/10.1007/s00280-021-04381-4
- A. Markham, Erdafitinib: First global approval, Drugs 79 (2019) 1017–1021; https://doi.org/10.1007/s40265-019-01142-9
- J. Tabernero, R. Bahleda, R. Dienstmann, J. R. Infante, A. Mita, A. Italiano, E. Calvo, V. Moreno, B. Adamo, A. Gazzah, B. Zhong, S. J. Platero, J. W. Smit, K. Stuyckens, M. Chatterjee-Kishore, J. Rodon, V. Peddareddigari, F. R. Luo and J.-C. Soria, 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. 33 (2015) 3401–3408; https://doi.org/10.1200/JCO.2014.60.7341
- R. Bahleda, A. Italiano, C. Hierro, A. Mita, A. Cervantes, N. Chan, M. Awad, E. Calvo, V. Moreno, R. Govindan, A. Spira, M. Gonzalez, B. Zhong, A. Santiago-Walker, I. Poggesi, T. Parekh, H. Xie, J. Infante and J. Tabernero, Multicenter phase i study of erdafitinib (JNJ-42756493), oral pan-fibroblast growth factor receptor inhibitor, in patients with advanced or refractory solid tumors, Clin. Cancer Res. 25 (2019) 4888–4897; https://doi.org/10.1158/1078-0432.CCR-18-3334
- E. Valade, A.-G. Dosne, H. Xie, R. Kleiman, L. Y. Li, J. J. Perez-Ruixo and D. Ouellet, Assessment of the effect of erdafitinib on cardiac safety: analysis of ECGs and exposure-QTc in patients with advanced or refractory solid tumors, Cancer Chemother. Pharmacol. 84 (2019) 621–633; https://doi.org/10.1007/s00280-019-03896-1
- T. Nishina, S. Takahashi, R. Iwasawa, H. Noguchi, M. Aoki and T. Doi, Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors, Invest. New Drugs 36 (2018) 424–434; https://doi.org/10.1007/s10637-017-0514-4
- E. Liow, N. Howard, C.-H. Jung, B. Pope, B. K. Campbell, A. Nguyen, M. Kerger, J. B. Ruddle, A. Anton, B. Thomas, K. Chu, P. Dundee, J. S. Peters, A. J. Costello, A. S. Ryan, C. M. Hovens, B. Tran and N. M. Corcoran, Phase 2 study of neoadjuvant FGFR inhibition and androgen deprivation therapy prior to prostatectomy, Clin. Genitourin. Cancer 20 (2022) 452–458; https://doi.org/10.1016/j.clgc.2022.05.007
- E. Scheers, C. Borgmans, C. Keung, H. Bohets, I. Wynant, I. Poggesi, F. Cuyckens, L. Leclercq and R. N. V. S. Mamidi, Metabolism and disposition in rats, dogs, and humans of erdafitinib, an orally administered potent pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, Xenobiotica 51 (2021) 177–193; https://doi.org/10.1080/00498254.2020.1821123
- I. Poggesi, L. Y. Li, J. Jiao, P. Hellemans, F. Rasschaert, L. de Zwart, J. Snoeys, M. De Meulder, R. N. V. S. Mamidi and D. Ouellet, Effect of fluconazole and itraconazole on the pharmacokinetics of erdafitinib in healthy adults: A randomized, open-label, drug-drug interaction study, Eur. J. Drug Metab. Pharmacokin. 45 (2020) 101–111; https://doi.org/10.1007/s13318-019-00581-9
- L. Y. Li, Y. Guo, M. Gonzalez and D. Ouellet, Effect of plasma protein binding on the pharmacokinetics of erdafitinib: Results of an integrated cross-study analysis, J. Clin. Pharmacol. 60 (2020) 391–399; https://doi.org/10.1002/jcph.1529
- L. Wu, C. Zhang, C. He, D. Qian, L. Lu, Y. Sun, M. Xu, J. Zhuo, P. C. C. Liu, R. Klabe, R. Wynn, M. Covington, K. Gallagher, L. Leffet, K. Bowman, S. Diamond, H. Koblish, Y. Zhang, M. Soloviev, G. Hollis, T. C. Burn, P. Scherle, S. Yeleswaram, R. Huber and W. Yao, Discovery of pemigatinib: A potent and selective fibroblast growth factor receptor (FGFR) inhibitor, J. Med. Chem. 64 (2021) 10666–10679; https://doi.org/10.1021/acs.jmedchem.1c00713
- P. C. C. Liu, H. Koblish, L. Wu, K. Bowman, S. Diamond, D. DiMatteo, Y. Zhang, M. Hansbury, M. Rupar, X. Wen, P. Collier, P. Feldman, R. Klabe, K. A. Burke, M. Soloviev, C. Gardiner, X. He, A. Volgina, M. Covington, B. Ruggeri, R. Wynn, T. C. Burn, P. Scherle, S. Yeleswaram, W. Yao, R. Huber and G. Hollis, INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models, PLoS One 15 (2020) e0231877 (16 pages); https://doi.org/10.1371/journal.pone.0231877
- Q. Lin, X. Chen, L. Qu, M. Guo, H. Wei, S. Dai, L. Jiang and Y. Chen, Characterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants, Commun. Chem. 5 (2022) Article ID 100 (7 pages); https://doi.org/10.1038/s42004-022-00718-z
- V. Subbiah, N. O. Iannotti, M. Gutierrez, D. C. Smith, L. Féliz, C. F. Lihou, C. Tian, I. M. Silverman, T. Ji and M. Saleh, FIGHT-101, a first-in-human study of potent and selective FGFR 1-3 inhibitor pemigatinib in pan-cancer patients with FGF/FGFR alterations and advanced malignancies, Ann. Oncol. 33(5) (2022) 522–533; https://doi.org/10.1016/j.annonc.2022.02.001
- M. Saleh, M. E. Gutierrez, V. Subbiah, D. C. Smith, E. Asatiani, C. F. Lihou, H. Zhen, S. Yeleswaram, T. Ji and J. Nemunaitis, Abstract CT111: Preliminary results from a phase 1/2 study of INCB054828, a highly selective fibroblast growth factor receptor (FGFR) inhibitor, in patients with advanced malignancies, Cancer Res. 77(13, Suppl.) (2017) CT111; https://doi.org/10.1158/1538-7445.AM2017-CT111
- X. Gong, T. Ji, X. Liu, X. Chen and S. Yeleswaram, Evaluation of the clinical cardiac safety of pemigatinib, a fibroblast growth factor receptor inhibitor, in participants with advanced malignancies, Pharmacol. Res. Perspect. 10 (2022) e00906 (8 pages); https://doi.org/10.1002/prp2.906
- G. K. Abou-Alfa, V. Sahai, A. Hollebecque, G. Vaccaro, D. Melisi, R. Al-Rajabi, A. S. Paulson, M. J. Borad, D. Gallinson, A. G. Murphy, D.-Y. Oh, E. Dotan, D. V Catenacci, E. Van Cutsem, T. Ji, C. F. Lihou, H. Zhen, L. Féliz and A. Vogel, Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study, Lancet Oncol. 21 (2020) 671–684; https://doi.org/10.1016/S1470-2045(20)30109-1
- S. M. Hoy, Pemigatinib: First approval, Drugs 80 (2020) 923–929; https://doi.org/10.1007/s40265-020-01330-y
- U.S. Food & Drug Adminstration, FDA Approves Pemigatinib for Relapsed or Refractory Myeloid/Lymphoid Neoplasms with FGFR1 Rearrangement, USFDA, Aug 29, 2022; https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-pemigatinib-relapsed-or-refractory-myeloidlymphoid-neoplasms-fgfr1-rearrangement; last access date Oct 10, 2023
- C. Kang, Infigratinib: First approval, Drugs 81 (2021) 1355–1360; https://doi.org/10.1007/s40265-021-01567-1
- Y. Y. Syed, Futibatinib: First approval, Drugs 82 (2022) 1737–1743; https://doi.org/10.1007/s40265-022-01806-z
- K. Bibeau, L. Féliz, C. F. Lihou, H. Ren and G. K. Abou-Alfa, Progression-free survival in patients with cholangiocarcinoma with or without FGF/FGFR alterations: A FIGHT-202 post hoc analysis of prior systemic therapy response, JCO Prec. Oncol. 6 (2022) e2100414; https://doi.org/10.1200/PO.21.00414
- T. S. Bekaii-Saab, J. W. Valle, E. Van Cutsem, L. Rimassa, J. Furuse, T. Ioka, D. Melisi, T. Macarulla, J. Bridgewater, H. Wasan, M. J. Borad, G. K. Abou-Alfa, P. Jiang, C. F. Lihou, H. Zhen, E. Asatiani, L. Féliz and A. Vogel, FIGHT-302: first-line pemigatinib vs gemcitabine plus cisplatin for advanced cholangiocarcinoma with FGFR2 rearrangements, Future Oncol. 16 (2020) 2385–2399; https://doi.org/10.2217/fon-2020-0429
- S. Verstovsek, A. M. Vannucchi, A. Rambaldi, J. R. Gotlib, A. J. Mead, A. Hochhaus, J.-J. Kiladjian, J. C. Hernandez Boluda, E. Asatiani, C. Lihou, H. Zhen and A. Reiter, Interim results from Fight-203, a phase 2, open-label, multicenter study evaluating the efficacy and safety of pemigatinib (INCB054828) in patients with myeloid/lymphoid neoplasms with rearrangement of fibroblast growth factor receptor 1 (FGFR1), Blood 132(Suppl. 1) (2018) Article ID 690; https://doi.org/10.1182/blood-2018-99-110388
- J. Gotlib, J.-J. Kiladjian, A. Vannucchi, A. Rambaldi, A. Reiter, W. Shomali, T. I. George, J. L. Patel, P. Colucci, C. Walker, H. Zhen and S. Verstovsek, A phase 2 study of pemigatinib (FIGHT-203; INCB054828) in patients with myeloid/lymphoid neoplasms (MLNs) with fibroblast growth factor receptor 1 (FGFR1) rearrangement (MLN FGFR1), Blood 138(Suppl. 1) (2021) Article ID 385; https://doi.org/10.1182/blood-2021-148103
- T. Ji, X. Chen, X. Liu and S. Yeleswaram, Population pharmacokinetics analysis of pemigatinib in patients with advanced malignancies, Clin. Pharmacol. Drug Dev. 11 (2022) 454–466; https://doi.org/10.1002/cpdd.1038
- T. Ji, K. Rockich, N. Epstein, H. Overholt, P. Wang, X. Chen, N. Punwani and S. Yeleswaram, Evaluation of the pharmacokinetics of pemigatinib in patients with impaired hepatic or renal function, Br. J. Clin. Pharmacol. 88 (2022) 237–247; https://doi.org/10.1111/bcp.14954
- T. Ji, K. Rockich, N. Epstein, H. Overholt, P. Wang, X. Chen, N. Punwani and S. Yeleswaram, Evaluation of drug-drug interactions of pemigatinib in healthy participants, Eur. J. Clin. Pharmacol. 77 (2021) 1887–1897; https://doi.org/10.1007/s00228-021-03184-z
- V. Guagnano, P. Furet, C. Spanka, V. Bordas, M. Le Douget, C. Stamm, J. Brueggen, M. R. Jensen, C. Schnell, H. Schmid, M. Wartmann, J. Berghausen, P. Drueckes, A. Zimmerlin, D. Bussiere, J. Murray and D. Graus Porta, Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase, J. Med. Chem. 54 (2011) 7066–7083; https://doi.org/10.1021/jm2006222
- V. Guagnano, A. Kauffmann, S. Wöhrle, C. Stamm, M. Ito, L. Barys, A. Pornon, Y. Yao, F. Li, Y. Zhang, Z. Chen, C. J. Wilson, V. Bordas, M. Le Douget, L. A. Gaither, J. Borawski, J. E. Monahan, K. Venkatesan, T. Brummendorf, D. M. Thomas, C. Garcia-Echeverria, F. Hofmann, W. R. Sellers and D. Graus-Porta, FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor, Cancer Discov. 2 (2012) 1118–1133; https://doi.org/10.1158/2159-8290.CD-12-0210
- L. Nogova, L. V. Sequist, J. M. Perez Garcia, F. Andre, J.-P. Delord, M. Hidalgo, J. H. M. Schellens, P. A. Cassier, D. R. Camidge, M. Schuler, U. Vaishampayan, H. Burris, G. G. Tian, M. Campone, Z. A. Wainberg, W.-T. Lim, P. LoRusso, G. I. Shapiro, K. Parker, X. Chen, S. Choudhury, F. Ringeisen, D. Graus-Porta, D. Porter, R. Isaacs, R. Buettner and J. Wolf, 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. 35 (2017) 157–165; https://doi.org/10.1200/JCO.2016.67.2048
- C. M. Kelly, A. N. Shoushtari, L.-X. Qin, S. P. D’Angelo, M. A. Dickson, M. M. Gounder, M. L. Keohan, C. Mcfadyen, A. Sjoberg, S. Singer, R. P. DeMatteo, S. Hwang, M. H. Heinemann, J. H. Francis, C. R. Antonescu, P. Chi and W. D. Tap, 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 37 (2019) 282–290; https://doi.org/10.1007/s10637-018-0648-z
- M. Javle, M. Lowery, R. T. Shroff, K. H. Weiss, C. Springfeld, M. J. Borad, R. K. Ramanathan, L. Goyal, S. Sadeghi, T. Macarulla, A. El-Khoueiry, R. K. Kelley, I. Borbath, S. P. Choo, D.-Y. Oh, P. A. Philip, L.-T. Chen, T. Reungwetwattana, E. V. Cutsem, K.-H. Yeh, K. Ciombor, R. S. Finn, A. Patel, S. Sen, D. Porter, R. Isaacs, A. X. Zhu, G. K. Abou-Alfa and T. Bekaii-Saab, Phase II study of BGJ398 in patients with fgfr-altered advanced cholangiocarcinoma, J. Clin. Oncol. 36 (2018) 276–282; https://doi.org/10.1200/JCO.2017.75.5009
- M. Javle, S. Roychowdhury, R. K. Kelley, S. Sadeghi, T. Macarulla, K. H. Weiss, D.-T. Waldschmidt, L. Goyal, I. Borbath, A. El-Khoueiry, M. J. Borad, W. P. Yong, P. A. Philip, M. Bitzer, S. Tanasanvimon, A. Li, A. Pande, H. S. Soifer, S. P. Shepherd, S. Moran, A. X. Zhu, T. S. Bekaii-Saab and G. K. Abou-Alfa, Infigratinib (BGJ398) in previously treated patients with advanced or metastatic cholangiocarcinoma with FGFR2 fusions or rearrangements: mature results from a multicentre, open-label, single-arm, phase 2 study, Lancet Gastroenterol. Hepatol. 6 (2021) 803–815; https://doi.org/10.1016/S2468-1253(21)00196-5
- S. Makawita, G. K Abou-Alfa, S. Roychowdhury, S. Sadeghi, I. Borbath, L. Goyal, A. Cohn, A. Lamarca, D.-Y. Oh, T. Macarulla, R. T Shroff, M. Howland, A. Li, T. Cho, A. Pande and M. Javle, Infigratinib in patients with advanced cholangiocarcinoma with FGFR2 gene fusions/translocations: the PROOF 301 trial, Future Oncol. 16 (2020) 2375–2384; https://doi.org/10.2217/fon-2020-0299
- Y. Lyou, P. Grivas, J. E. Rosenberg, J. Hoffman-Censits, D. I. Quinn, D. P. Petrylak, M. Galsky, U. Vaishampayan, U. De Giorgi, S. Gupta, H. Burris, J. Rearden, A. Li, H. Wang, M. Reyes, S. Moran, S. Daneshmand, D. Bajorin and S. K. Pal, Hyperphosphatemia secondary to the selective fibroblast growth factor receptor 1-3 inhibitor infigratinib (BGJ398) is associated with antitumor efficacy in fibroblast growth factor receptor 3-altered advanced/metastatic urothelial carcinoma, Eur. Urol. 78 (2020) 916–924; https://doi.org/https://doi.org/10.1016/j.eururo.2020.08.002
- S. K. Pal, D. M. Somford, P. Grivas, S. S. Sridhar, S. Gupta, J. Bellmunt, G. Sonpavde, M. T. Fleming, S. P. Lerner, Y. Loriot, J. Hoffman-Censits, B. P. Valderrama, C. Andresen, M. J. Schnabel, S. Cole and S. Daneshmand, Targeting FGFR3 alterations with adjuvant infigratinib in invasive urothelial carcinoma: the phase III PROOF 302 trial, Future Oncol. 18 (2022) 2599–2614; https://doi.org/10.2217/fon-2021-1629
- A. B. Lassman, J. M. Sepúlveda-Sánchez, T. F. Cloughesy, M. J. Gil-Gil, V. K. Puduvalli, J. J. Raizer, F. Y. F. De Vos, P. Y. Wen, N. A. Butowski, P. M. J. Clement, M. D. Groves, C. Belda-Iniesta, P. Giglio, H. S. Soifer, S. Rowsey, C. Xu, F. Avogadri, G. Wei, S. Moran and P. Roth, Infigratinib in patients with recurrent gliomas and FGFR alterations: A multicenter phase II study, Clin. Cancer Res. 28 (2022) 2270–2277; https://doi.org/10.1158/1078-0432.CCR-21-2664
- N. S. Al-Shakliah, M. W. Attwa, A. A. Kadi and H. AlRabiah, Identification and characterization of in silico, in vivo, in vitro, and reactive metabolites of infigratinib using LC-ITMS: bioactivation pathway elucidation and in silico toxicity studies of its metabolites, RSC Adv. 10 (2020) 16231–16244; https://doi.org/10.1039/C9RA10871H
- H. Sootome, H. Fujita, K. Ito, H. Ochiiwa, Y. Fujioka, K. Ito, A. Miura, T. Sagara, S. Ito, H. Ohsawa, S. Otsuki, K. Funabashi, M. Yashiro, K. Matsuo, K. Yonekura and H. Hirai, Futibatinib is a novel irreversible FGFR 1-4 inhibitor that shows selective antitumor activity against FGFR-deregulated tumors, Cancer Res. 80 (2020) 4986–4997; https://doi.org/10.1158/0008-5472.CAN-19-2568
- M. Kalyukina, Y. Yosaatmadja, M. J. Middleditch, A. V Patterson, J. B. Smaill and C. J. Squire, TAS-120 cancer target binding: defining reactivity and revealing the first fibroblast growth factor receptor 1 (FGFR1) irreversible structure, ChemMedChem 14 (2019) 494–500; https://doi.org/10.1002/cmdc.201800719
- R. Bahleda, F. Meric-Bernstam, L. Goyal, B. Tran, Y. He, I. Yamamiya, K. A. Benhadji, I. Matos and H.-T. Arkenau, Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1-4 inhibitor in patients with advanced solid tumors, Ann. Oncol. 31(10) (2020) 1405–1412; https://doi.org/10.1016/j.annonc.2020.06.018
- F. Meric-Bernstam, R. Bahleda, C. Hierro, M. Sanson, J. Bridgewater, H.-T. Arkenau, B. Tran, R. K. Kelley, J. O. Park, M. Javle, Y. He, K. A. Benhadji and L. Goyal, Futibatinib, an irreversible FGFR1-4 inhibitor, in patients with advanced solid tumors harboring FGF/FGFR aberrations: A phase i dose-expansion study, Cancer Discov. 12 (2022) 402–415; https://doi.org/10.1158/2159-8290.CD-21-0697
- L. Goyal, F. Meric-Bernstam, A. Hollebecque, C. Morizane, J. W. Valle, T. B. Karasic, T. A. Abrams, R. K. Kelley, P. Cassier, J. Furuse, H.-J. Klümpen, H.-M. Chang, L.-T. Chen, Y. Komatsu, K. Masuda, D. Ahn, Y. He, N. Soni, K. A. Benhadji and J. A. Bridgewater, Abstract CT010: Primary results of phase 2 FOENIX-CCA2: The irreversible FGFR1-4 inhibitor futibatinib in intrahepatic cholangio-carcinoma (iCCA) with FGFR2 fusions/rearrangements, Cancer Res. 81 (2021) CT010–CT010; https://doi.org/10.1158/1538-7445.AM2021-CT010
- I. Yamamiya, A. Hunt, F. Yamashita, D. Sonnichsen, T. Muto, Y. He and K. A. Benhadji, Evaluation of the mass balance and metabolic profile of futibatinib in healthy participants, Clin. Pharmacol. Drug Dev. 12 (2023) 927–939; https://doi.org/10.1002/cpdd.1271
- I. Yamamiya, A. Hunt, F. Yamashita, D. Sonnichsen, Y. He and K. A. Benhadji, Evaluation of potential food effects and drug interactions with lansoprazole in healthy adult volunteers receiving futibatinib, Clin. Pharmacol. Drug Dev. 12(3) (2022) 294–303; https://doi.org/10.1002/cpdd.1196
- I. Yamamiya, A. Hunt, T. Takenaka, D. Sonnichsen, M. Mina, Y. He, K. A. Benhadji and L. Gao, Evaluation of the cytochrome P450 3A and P-glycoprotein drug-drug interaction potential of futibatinib, Clin. Pharmacol. Drug Dev. 12(10) (2023) 966–978; https://doi.org/10.1002/cpdd.1259
- I. Yamamiya, A. Hunt, F. Yamashita, D. Sonnichsen, Y. He and K. A. Benhadji, Evaluation of potential food effects and drug interactions with lansoprazole in healthy adult volunteers receiving futibatinib, Clin. Pharmacol. Drug Dev. 12(3) (2023) 294–303; https://doi.org/10.1002/cpdd.1196
- A. Jain, M. J. Borad, R. K. Kelley, Y. Wang, R. Abdel-Wahab, F. Meric-Bernstam, K. A. Baggerly, A. O. Kaseb, H. O. Al-Shamsi, D. H. Ahn, T. DeLeon, A. G. Bocobo, T. Bekaii-Saab, R. T. Shroff and M. Javle, Cholangiocarcinoma with FGFR genetic aberrations: A unique clinical phenotype, JCO Prec. Oncol. 2 (2018) 1–12; https://doi.org/10.1200/PO.17.00080
- P. C. Lee, A. Hendifar, A. Osipov, M. Cho, D. Li and J. Gong, Targeting the fibroblast growth factor receptor (FGFR) in advanced cholangiocarcinoma: Clinical trial progress and future considerations, Cancers (Basel) 13(7) (2021) Article ID 1706; https://doi.org/10.3390/cancers13071706
- A. Saborowski, U. Lehmann and A. Vogel, FGFR inhibitors in cholangiocarcinoma: what’s now and what’s next?, Ther. Adv. Med. Oncol. 12 (2020) 1–12; https://doi.org/10.1177/1758835920953293
- V. Mazzaferro, B. F. El-Rayes, M. Droz Dit Busset, C. Cotsoglou, W. P. Harris, N. Damjanov, G. Masi, L. Rimassa, N. Personeni, F. Braiteh, V. Zagonel, K. P. Papadopoulos, T. Hall, Y. Wang, B. Schwartz, J. Kazakin, S. Bhoori, F. de Braud and W. L. Shaib, Derazantinib (ARQ 087) in advanced or inoperable FGFR2 gene fusion-positive intrahepatic cholangiocarcinoma, Br. J. Cancer 120 (2019) 165–171; https://doi.org/10.1038/s41416-018-0334-0
- J. Gandhi, J.-F. Chen and H. Al-Ahmadie, Urothelial carcinoma: Divergent differentiation and morphologic subtypes, Surg. Pathol. Clin. 15 (2022) 641–659; https://doi.org/10.1016/j.path.2022.07.003
- Z. B. Zengin, A. Chehrazi-Raffle, N. J. Salgia, R. Muddasani, S. Ali, L. Meza and S. K. Pal, Targeted therapies: Expanding the role of FGFR3 inhibition in urothelial carcinoma, Urol. Oncol. 40 (2022) 25–36; https://doi.org/10.1016/j.urolonc.2021.10.003
- C. N. Sternberg, D. P. Petrylak, J. Bellmunt, H. Nishiyama, A. Necchi, H. Gurney, J.-L. Lee, M. S. van der Heijden, E. Rosenbaum, N. Penel, S.-T. Pang, J.-R. Li, X. García Del Muro, F. Joly, Z. Pápai, W. Bao, P. Ellinghaus, C. Lu, M. Sierecki, S. Coppieters, K. Nakajima, T. C. Ishida and D. I. Quinn, FORT-1: Phase II/III study of rogaratinib versus chemotherapy in patients with locally advanced or metastatic urothelial carcinoma selected based on FGFR1/3 mRNA expression, J. Clin. Oncol. 41 (2023) 629–639; https://doi.org/10.1200/JCO.21.02303
- B. J. Bain, Myeloid and lymphoid neoplasms with eosinophilia and abnormalities of PDGFRA, PDGFRB or FGFR1, Haematologica 95(5) (2010) 696–698; https://doi.org/10.3324/haematol.2009.021675
- S. Yue, Y. Li, X. Chen, J. Wang, M. Li, Y. Chen and D. Wu, FGFR-TKI resistance in cancer: current status and perspectives, J. Hematol. Oncol. 14 (2021) Article ID 23 (14 pages); https://doi.org/10.1186/s13045-021-01040-2
- M. H. Voss, C. Hierro, R. S. Heist, J. M. Cleary, F. Meric-Bernstam, J. Tabernero, F. Janku, L. Gandhi, A. J. Iafrate, D. R. Borger, N. Ishii, Y. Hu, Y. Kirpicheva, V. Nicolas-Metral, A. Pokorska-Bocci, A. Vaslin Chessex, C. Zanna, K. T. Flaherty and J. Baselga, A phase I, open-label, multicenter, dose-escalation study of the oral selective FGFR inhibitor Debio 1347 in patients with advanced solid tumors harboring FGFR gene alterations, Clin. Cancer Res. 25 (2019) 2699–2707; https://doi.org/10.1158/1078-0432.CCR-18-1959
- Y. Chiba, K. Sudo, Y. Kojima, H. Okuma, S. Kohsaka, R. Machida, M. Ichimura, K. Anjo, K. Kurishita, N. Okita, K. Nakamura, I. Kinoshita, M. Takahashi, J. Matsubara, H. Kusaba, K. Yonemori and M. Takahashi, A multicenter investigator-initiated phase 2 trial of E7090 in patients with advanced or recurrent solid tumor with fibroblast growth factor receptor (FGFR) gene alteration: FORTUNE trial, BMC Cancer 22 (2022) Article ID 869 (7 pages); https://doi.org/10.1186/s12885-022-09949-8
- G. E. Konecny, N. Finkler, A. A. Garcia, D. Lorusso, P. S. Lee, R. P. Rocconi, P. C. Fong, M. Squires, K. Mishra, A. Upalawanna, Y. Wang and R. Kristeleit, Second-line dovitinib (TKI258) in patients with FGFR2-mutated or FGFR2-non-mutated advanced or metastatic endometrial cancer: a nonrandomised, open-label, two-group, two-stage, phase 2 study, Lancet Oncol. 16 (2015) 686–694; https://doi.org/10.1016/S1470-2045(15)70159-2
- H. Kanzaki, T. Chiba, J. Ao, K. Koroki, K. Kanayama, S. Maruta, T. Maeda, Y. Kusakabe, K. Kobayashi, N. Kanogawa, S. Kiyono, M. Nakamura, T. Kondo, T. Saito, R. Nakagawa, S. Ogasawara, E. Suzuki, Y. Ooka, R. Muroyama, S. Nakamoto, S. Yasui, A. Tawada, M. Arai, T. Kanda, H. Maruyama, N. Mimura, J. Kato, Y. Zen, M. Ohtsuka, A. Iwama and N. Kato, The impact of FGF19/FGFR4 signaling inhibition in antitumor activity of multi-kinase inhibitors in hepatocellular carcinoma, Sci. Rep. 11 (2021) Article ID 5303 (12 pages); https://doi.org/10.1038/s41598-021-84117-9
- A. Raja, I. Park, F. Haq and S.-M. Ahn, FGF19-FGFR4 signaling in hepatocellular carcinoma, Cells 8(6) (2019) Article ID 536 (16 pages); https://doi.org/10.3390/cells8060536
- S. L. Chan, M. Schuler, Y.-K. Kang, C.-J. Yen, J. Edeline, S. P. Choo, C.-C. Lin, T. Okusaka, K.-H. Weiss, T. Macarulla, S. Cattan, J.-F. Blanc, K.-H. Lee, M. Maur, S. Pant, M. Kudo, E. Assenat, A. X. Zhu, T. Yau, H. Y. Lim, J. Bruix, A. Geier, C. Guillen-Ponce, A. Fasolo, R. S. Finn, J. Fan, A. Vogel, S. Qin, M. Riester, V. Katsanou, M. Chaudhari, T. Kakizume, Y. Gu, D. G. Porta, A. Myers and J.-P. Delord, A first-in-human phase 1/2 study of FGF401 and combination of FGF401 with spartalizumab in patients with hepatocellular carcinoma or biomarker-selected solid tumors, J. Exp. Clin. Cancer Res. 41 (2022) Article ID 189 (19 pages); https://doi.org/10.1186/s13046-022-02383-5
- L. Goyal, L. Shi, L. Y. Liu, F. Fece de la Cruz, J. K. Lennerz, S. Raghavan, I. Leschiner, L. Elagina, G. Siravegna, R. W. S. Ng, P. Vu, K. C. Patra, S. K. Saha, R. N. Uppot, R. Arellano, S. Reyes, T. Sagara, S. Otsuki, B. Nadres, H. A. Shahzade, I. Dey-Guha, I. J. Fetter, I. Baiev, E. E. V. Seventer, J. E. Murphy, C. R. Ferrone, K. K. Tanabe, V. Deshpande, J. J. Harding, R. Yaeger, R. K. Kelley, A. Bardelli, A. J. Iafrate, W. C. Hahn, C. H. Benes, D. T. Ting, H. Hirai, G. Getz, D. Juric, A. X. Zhu, R. B. Corcoran and N. Bardeesy, TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion-positive intrahepatic cholangiocarcinoma, Cancer Discov. 9 (2019) 1064–1079; https://doi.org/10.1158/2159-8290.CD-19-0182