Difference between revisions of "Nintedanib (Vargatef)"

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=Mechanism of action=
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==Mechanism of action==
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=504524 NCI Drug Dictionary]: An orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3).
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=504524 NCI Drug Dictionary]: An orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3).
  
=Preliminary data=
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==Diseases for which it is used==
==[[Mesothelioma]]==
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*[[Mesothelioma]]
* '''LUME-Meso:''' Grosso F, Steele N, Novello S, Nowak AK, Popat S, Greillier L, John T, Leighl NB, Reck M, Taylor P, Planchard D, Sørensen JB, Socinski MA, von Wangenheim U, Loembé AB, Barrueco J, Morsli N, Scagliotti G. Nintedanib plus pemetrexed/cisplatin in patients with malignant pleural mesothelioma: phase II results from the randomized, placebo-controlled LUME-Meso trial. J Clin Oncol. 2017 Nov 1;35(31):3591-3600. Epub 2017 Sep 11. [https://ascopubs.org/doi/full/10.1200/JCO.2017.72.9012 link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/28892431 PubMed]
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*[[Non-small cell lung cancer]]
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*[[Ovarian cancer]]
  
==[[Non-small cell lung cancer]]==
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==History of changes in FDA indication==
* '''LUME-Lung 1:''' Reck M, Kaiser R, Mellemgaard A, Douillard JY, Orlov S, Krzakowski M, von Pawel J, Gottfried M, Bondarenko I, Liao M, Gann CN, Barrueco J, Gaschler-Markefski B, Novello S; LUME-Lung 1 Study Group. 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, randomised controlled trial. Lancet Oncol. 2014 Feb;15(2):143-55. 2. Epub 2014 Jan 9. [https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(13)70586-2/fulltext link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/24411639 PubMed]
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''Not FDA approved at this time.''
* '''LUME-Lung 2:''' Hanna NH, Kaiser R, Sullivan RN, Aren OR, Ahn MJ, Tiangco B, Voccia I, Pawel JV, Kovcin V, Agulnik J, Gaschler-Markefski B, Barrueco J, Sikken P, Schloss C, Kim JH; LUME-Lung 2 Study group. 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 Dec;102:65-73. Epub 2016 Oct 27. [https://www.lungcancerjournal.info/article/S0169-5002(16)30510-4/fulltext link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/27987591 PubMed]
 
  
==[[Ovarian cancer]]==
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==Also known as==
* '''OTHER:''' du Bois A, Kristensen G, Ray-Coquard I, Reuss A, Pignata S, Colombo N, Denison U, Vergote I, Del Campo JM, Ottevanger P, Heubner M, Minarik T, Sevin E, de Gregorio N, Bidziński M, Pfisterer J, Malander S, Hilpert F, Mirza MR, Scambia G, Meier W, Nicoletto MO, Bjørge L, Lortholary A, Sailer MO, Merger M, Harter P; AGO Study Group led Gynecologic Cancer Intergroup/European Network of Gynaecologic Oncology Trials Groups Intergroup Consortium. Standard first-line chemotherapy with or without nintedanib for advanced ovarian cancer (AGO-OVAR 12): a randomised, double-blind, placebo-controlled phase 3 trial. Lancet Oncol. 2016 Jan;17(1):78-89. Epub 2015 Nov 16. [https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(15)00366-6/fulltext link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/26590673 PubMed]
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*'''Code name:''' BIBF 1120
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*'''Brand names:''' Ofev, Vargatef
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
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[[Category:SRC inhibitors]]
 
[[Category:SRC inhibitors]]
  
[[Category:Investigational drugs]]
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[[Category:Mesothelioma medications]]
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[[Category:Non-small cell lung cancer medications]]
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[[Category:Ovarian cancer medications]]
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[[Category:EMA approved drugs]]

Revision as of 20:27, 6 September 2019

Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3).

Diseases for which it is used

History of changes in FDA indication

Not FDA approved at this time.

Also known as

  • Code name: BIBF 1120
  • Brand names: Ofev, Vargatef