Aflibercept
Clinical data | |
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Trade names | Eylea, Zaltrap |
Other names | ziv-aflibercept |
Biosimilars | Yesafili[1][2] |
AHFS/Drugs.com | Aflibercept Monograph Ziv-aflibercept Monograph |
MedlinePlus | a612004 |
License data |
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Pregnancy category |
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Routes of administration | Intravenous, intravitreal injection |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number | |
DrugBank | |
ChemSpider |
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Chemical and physical data | |
Formula | C4318H6788N1164O1304S32 |
Molar mass | 96898.57 g·mol−1 |
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Aflibercept, sold under the brand names Eylea among others, is a medication used to treat
It is an inhibitor of vascular endothelial growth factor (VEGF).[10][11]
Medical uses
Aflibercept (Eylea) is
Aflibercept (Zaltrap), in combination with
It is used for the treatment of wet macular degeneration and is administered as an
In August 2014, aflibercept (Eylea) was approved for the treatment of people with visual impairment due to diabetic macular edema, according to the updated summary of product characteristics.[12] In May 2019, the US FDA expanded the indication for aflibercept to include all stages of diabetic retinopathy.[13]
In February 2023, the US FDA approved aflibercept (Eylea) as a treatment for retinopathy of prematurity.[14]
Contraindications
Aflibercept (Eylea) is contraindicated in people with infections or active inflammations of or near the eye,[5] while Aflibercept (Zaltrap) has no contraindications.[6]
Adverse effects
Common adverse effects of the eye formulation include conjunctival
Aflibercept (Zaltrap) has adverse effects typical of anti-cancer drugs, such as reduced blood cell count (leukopenia, neutropenia, thrombocytopenia), gastrointestinal disorders like diarrhea and abdominal pain, and fatigue. Another common effect is hypertension (increased blood pressure).[6]
Interactions
No interactions are described for either formulation.[5][6]
Mechanism of action
In wet macular degeneration, abnormal blood vessels grow in the
Aflibercept (Zaltrap) binds to circulating VEGFs and acts like a "VEGF trap".
Composition
Aflibercept is a
History
Regeneron commenced clinical testing of aflibercept in cancer in 2001.
Society and culture
Legal status
In November 2011, the United States Food and Drug Administration (FDA) approved aflibercept for the treatment of wet macular degeneration.[21]
In August 2012, the US FDA approved aflibercept (Zaltrap) for use in combination with
In November 2012, the European Medicines Agency (EMA) approved aflibercept (Eylea) for the treatment of wet macular degeneration.[8][23]
In February 2013, the European Medicines Agency (EMA) approved aflibercept (Zaltrap) for the treatment of adults with metastatic colorectal cancer for whom treatment based on oxaliplatin has not worked or the cancer got worse.[9][24] Aflibercept (Zaltrap) is used with FOLFIRI, which is a treatment combining the medicines irinotecan, 5-fluorouracil, and folinic acid.[9]
Economics
In March 2015, aflibercept was one of a group of drugs delisted from the UK Cancer Drugs Fund.
Research
In March 2011, Regeneron reported that aflibercept failed its primary
In April 2011, Regeneron reported that aflibercept improved its primary endpoint of overall survival in the Velour phase III clinical trial for
Aflibercept was also in a phase III trial for
A 2016 Cochrane Review examined outcomes comparing aflibercept versus ranibizumab injections in over 2400 people with neovascular AMD, from two randomized controlled trials. Both treatment options yielded similar improvements in visual acuity and morphological outcomes, though the authors note that the aflibercept treatment regimen has the potential to reduce treatment burden and risks from frequent injections.[28]
A 2017 review update studying the effects of anti-VEGF drugs on diabetic macular edema found that while all three studied treatments have advantages over laser therapy, there was moderate evidence that aflibercept is significantly favored in all measured efficacy outcomes over ranibizumab and bevacizumab, after one year, longer term advantages were unclear.[29]
References
- ^ "Yesafili: Pending EC decision". European Medicines Agency. 21 July 2023. Archived from the original on 2 October 2023. Retrieved 2 October 2023.
- ^ "Yesafili Product information". Union Register of medicinal products. 19 September 2023. Archived from the original on 2 October 2023. Retrieved 2 October 2023.
- ^ "Ziv-aflibercept (Zaltrap) Use During Pregnancy". Drugs.com. 25 December 2019. Archived from the original on 29 November 2020. Retrieved 12 March 2020.
- ^ "Regulatory Decision Summary for Eylea HD". Drug and Health Products Portal. 2 February 2024. Retrieved 2 April 2024.
- ^ a b c d e f "Eylea- aflibercept injection, solution". DailyMed. 12 August 2019. Archived from the original on 25 March 2021. Retrieved 13 August 2020.
- ^ a b c d e f "Zaltrap- ziv-aflibercept solution, concentrate". DailyMed. 10 June 2020. Archived from the original on 4 August 2020. Retrieved 13 August 2020.
- ^ "Eylea HD- aflibercept injection, solution". DailyMed. 18 August 2023. Archived from the original on 29 August 2023. Retrieved 28 August 2023.
- ^ a b c "Eylea EPAR". European Medicines Agency (EMA). 9 July 2019. Archived from the original on 9 November 2020. Retrieved 12 March 2020.
- ^ a b c d "Zaltrap EPAR". European Medicines Agency (EMA). 12 November 2019. Archived from the original on 11 November 2020. Retrieved 12 March 2020.
- from the original on 8 December 2019. Retrieved 3 July 2008.
- PMID 18388198.
- ^ "New indication for Eylea". The Pharmaceutical Journal. No. 7826. Royal Pharmaceutical Society. 27 August 2014. Archived from the original on 20 June 2015. Retrieved 20 September 2014.
- ^ "FDA Approves Eylea (aflibercept) Injection for Diabetic Retinopathy". Regeneron Pharmaceuticals Inc. (Press release). 13 May 2019. Archived from the original on 14 May 2019. Retrieved 28 June 2023.
- ^ "Eylea (aflibercept) Injection Approved as the First Pharmacologic Treatment for Preterm Infants with Retinopathy of Prematurity (ROP) by the FDA". Regeneron Pharmaceuticals Inc. (Press release). 8 February 2023. Archived from the original on 28 June 2023. Retrieved 28 June 2023.
- ^ "Aflibercept Approved for Colorectal Cancer in Europe". 7 February 2013. Archived from the original on 10 February 2013.
- ^ a b c d "Regeneron and Sanofi-Aventis Report Positive Phase III mCRC Trial Data". 27 April 2011. Archived from the original on 2 February 2012.
- ^ a b "Ziv-Aflibercept". FDA Drug Approvals Database. Food and Drug Administration. 3 August 2012. Archived from the original on 16 October 2013. Retrieved 16 October 2013.
- ^ a b "Our History - A 25 year commitment to repeated innovation". www.regeneron.com. 1988. Archived from the original on 17 May 2017. Retrieved 7 May 2018.
- ^ Candace Hoffmann for First Word Pharma. 8 September 2003 Aventis inks deal with Regeneron for collaboration on cancer therapy Archived 14 April 2014 at the Wayback Machine
- ^ Genetic Engineering and Biotechnology News. 19 October 2006 Bayer HealthCare Signs On to Help Develop Regeneron's VEGF Trap-Eye Archived 14 April 2014 at the Wayback Machine
- ^ Gever J (19 November 2011). "FDA Approves Eylea for Macular Degeneration". MedpageToday.com. Archived from the original on 28 May 2013. Retrieved 16 October 2013.
- ^ BioWorld: GPhA: Common Name is Key to Biosimilar Competition Archived 13 December 2013 at the Wayback Machine
- ^ "Aflibercept Injection Approved for the Treatment of Wet Age-Related Macular Degeneration in Europe". Amd-fruehdiagnose.de. Archived from the original on 25 November 2013. Retrieved 16 October 2013.
- ^ "Zaltrap : EPAR - Summary for the public" (PDF). Archived (PDF) from the original on 16 October 2013. Retrieved 1 July 2013.
- ^ "Cancer: Drugs:Written question - HL3340". UK Parliament. 19 November 2015. Archived from the original on 2 April 2018.
- ^ "Physician/Supplier National Data" (PDF). Centers for Medicare & Medicaid Services. Archived (PDF) from the original on 17 August 2018. Retrieved 11 June 2019.
- ^ "Regeneron and Sanofi-Aventis Cancer Drug Misses Phase III Primary Endpoint but Meets Secondary Targets". 11 March 2011. Archived from the original on 6 April 2012.
- PMID 26857947.
- PMID 38275741.
External links
- "Ziv-aflibercept Injection". MedlinePlus.
- "Ziv-aflibercept". National Cancer Institute. 15 August 2012. Retrieved 10 February 2023.