Aflibercept
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| Trade names | Eylea |
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| Routes of administration | Injection |
| ATC code | |
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| Legal status |
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| Identifiers | |
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| Chemical and physical data | |
| Formula | C4318H6788N1164O1304S32 |
| Molar mass | 96.90 kDa g·mol−1 |
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Aflibercept is a fusion protein approved in the United States for the treatment of wet macular degeneration and metastatic colorectal cancer.
It is an inhibitor of vascular endothelial growth factor.[1][2] It is designed to bind to VEGF-A, VEGF-B, and placental growth factor (a.k.a PIGF, gene symbol PGF).[3]
Aflibercept is being co-developed by Sanofi-Aventis and Regeneron Pharmaceuticals.
Approvals and indications
In November 2011 the United States Food and Drug Administration approved aflibercept for the treatment of wet macular degeneration.[4]
On August 3, 2012 the United States Food and Drug Administration approved Zaltrap (ziv-aflibercept) for use in combination with 5-fluorouracil, leucovorin and irinotecan to treat adults with metastatic colorectal cancer that is resistant to or has progressed following an oxaliplatin‑containing regimen.[5]
In November 2012 the European Medicines Agency (EMA) approved aflibercept for the treatment of wet macular degeneration.[6]
Clinical trials
In March 2011 Regeneron reported that aflibercept failed its primary endpoint of overall survival in the Vital phase III trial for second-line treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC), although it improved the secondary endpoint of progression-free survival.[3][7]
In April 2011 Regeneron reported that aflibercept improved its primary endpoint of overall survival in the Velour phase III clinical trial for second-line treatment for metastatic colorectal cancer (mCRC).[3]
Aflibercept is also in a phase III trial for hormone-refractory metastatic prostate cancer.[3]
References
- ^ Fraser HM, Wilson H, Silvestri A, Morris KD, Wiegand SJ (2008). "The Role of Vascular Endothelial Growth Factor and Estradiol in the Regulation of Endometrial Angiogenesis and Cell Proliferation in the Marmoset". Endocrinology. 149 (9): 4413–20. doi:10.1210/en.2008-0325. PMID 18499749.
{{cite journal}}: Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ Duncan WC, van den Driesche S, Fraser HM (2008). "Inhibition of Vascular Endothelial Growth Factor in the Primate Ovary Up-Regulates Hypoxia-Inducible Factor-1{alpha} in the Follicle and Corpus Luteum". Endocrinology. 149 (7): 3313–20. doi:10.1210/en.2007-1649. PMID 18388198.
{{cite journal}}: Unknown parameter|month=ignored (help)CS1 maint: multiple names: authors list (link) - ^ a b c d "Regeneron and Sanofi-Aventis Report Positive Phase III mCRC Trial Data". 27 Apr 2011.
- ^ FDA Approves Eylea for Macular Degeneration
- ^ FDA Drug Approvals Database
- ^ Aflibercept Injection Approved for the Treatment of Wet Age-Related Macular Degeneration in Europe
- ^ "Regeneron and Sanofi-Aventis Cancer Drug Misses Phase III Primary Endpoint but Meets Secondary Targets". 11 Mar 2011.
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