First-in-human phase I study of E7090, a novel selective fibroblast growth factor receptor inhibitor, in patients with advanced solid tumors.
Administration, Oral
Adult
Aged
Antineoplastic Agents
/ administration & dosage
Drug Administration Schedule
Female
Humans
Japan
Male
Maximum Tolerated Dose
Middle Aged
Neoplasms
/ drug therapy
Protein Kinase Inhibitors
/ administration & dosage
Receptors, Fibroblast Growth Factor
/ antagonists & inhibitors
fibroblast growth factor
maximum tolerated dose
pharmacokinetics
phase I clinical trial
safety
Journal
Cancer science
ISSN: 1349-7006
Titre abrégé: Cancer Sci
Pays: England
ID NLM: 101168776
Informations de publication
Date de publication:
Feb 2020
Feb 2020
Historique:
received:
12
09
2019
revised:
24
11
2019
accepted:
25
11
2019
pubmed:
5
12
2019
medline:
20
2
2020
entrez:
5
12
2019
Statut:
ppublish
Résumé
Fibroblast growth factor receptors (FGFR) are a family of transmembrane receptor tyrosine kinases involved in regulating cellular processes. FGFR mutations are implicated in oncogenesis, representing therapeutic potential in the form of FGFR inhibitors. This phase I, first-in-human study in Japan evaluated safety and tolerability of E7090, a potent selective FGFR1-3 inhibitor, in patients with advanced solid tumors. Dose escalation (daily oral dose of 1-180 mg) was carried out to assess dose-limiting toxicity (DLT), maximum tolerated dose, and pharmacokinetics. Pharmacodynamic markers (serum phosphate, fibroblast growth factor 23, and 1,25-(OH)
Identifiants
pubmed: 31797489
doi: 10.1111/cas.14265
pmc: PMC7004556
doi:
Substances chimiques
Antineoplastic Agents
0
Protein Kinase Inhibitors
0
Receptors, Fibroblast Growth Factor
0
Types de publication
Clinical Trial, Phase I
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
571-579Subventions
Organisme : Eisai Co., Ltd
Informations de copyright
© 2019 The Authors. Cancer Science published by John Wiley & Sons Australia, Ltd on behalf of Japanese Cancer Association.
Références
Ann Oncol. 2017 Jun 1;28(6):1316-1324
pubmed: 29177434
J Clin Oncol. 2013 May 10;31(14):1785-91
pubmed: 23569307
Clin Cancer Res. 2017 Sep 15;23(18):5366-5373
pubmed: 28615371
CA Cancer J Clin. 2013 Jul-Aug;63(4):249-79
pubmed: 23716430
Trends Cell Biol. 2015 Apr;25(4):221-33
pubmed: 25467007
Nat Genet. 2000 Nov;26(3):345-8
pubmed: 11062477
Target Oncol. 2017 Aug;12(4):463-474
pubmed: 28589492
Proc Natl Acad Sci U S A. 2001 May 22;98(11):6500-5
pubmed: 11344269
Crit Rev Oncol Hematol. 2017 May;113:256-267
pubmed: 28427515
Mol Cancer Ther. 2016 Nov;15(11):2630-2639
pubmed: 27535969
Oncotarget. 2017 Feb 28;8(9):16052-16074
pubmed: 28030802
Invest New Drugs. 2018 Jun;36(3):424-434
pubmed: 28965185
Eur J Cancer. 2009 Jan;45(2):228-47
pubmed: 19097774
Invest New Drugs. 2017 Aug;35(4):451-462
pubmed: 28070720
J Bone Miner Res. 2011 Oct;26(10):2486-97
pubmed: 21812026
Semin Oncol. 2015 Dec;42(6):801-19
pubmed: 26615127
Cancer Sci. 2020 Feb;111(2):571-579
pubmed: 31797489
Kidney Int. 2001 Dec;60(6):2079-86
pubmed: 11737582
Nat Rev Cancer. 2017 May;17(5):318-332
pubmed: 28303906
J Clin Oncol. 2017 Jan 10;35(2):157-165
pubmed: 27870574
Clin Cancer Res. 2012 Apr 1;18(7):1855-62
pubmed: 22388515
J Clin Oncol. 2015 Oct 20;33(30):3401-8
pubmed: 26324363
Br J Cancer. 2017 Nov 21;117(11):1592-1599
pubmed: 28972963