Evolocumab

Evolocumab
Monoclonal antibody
TypeWhole antibody
SourceHuman
TargetPCSK9
Names
Trade namesRepatha
Other namesAMG-145[1]
Clinical data
Drug classPCSK9 inhibitor[2]
Main usesAbnormal lipids, prevent heart disease[3]
Side effectsRunny nose, upper respiratory tract infection, back pain, pain site of injection[2]
Pregnancy
category
  • AU: B1
  • US: N (Not classified yet)
    Routes of
    use    		Subcutaneous
    Typical dose140 mg q 2 wk[4]
    External links
    AHFS/Drugs.comMonograph
    Legal
    License data
    Legal status
    • US: [5]
    • In general: ℞ (Prescription only)
    Chemical and physical data
    FormulaC6242H9648N1668O1996S56
    Molar mass141790.89 g·mol−1

    Evolocumab, sold under the brand name Repatha, is a medication used to treat abnormal lipids and prevent heart disease.[3] It is less preferred to statins.[3] It is given by injection under the skin every 2 weeks or once a month.[3]

    Common side effects include runny nose, upper respiratory tract infection, back pain, and pain at the site of injection.[2] Other side effects may include allergic reactions.[3] Safety in pregnancy is unclear.[3] It is a monoclonal antibody that attaches to and blocks proprotein convertase subtilisin/kexin type 9 (PCSK9).[2]

    Evolocumab was approved for medical use in the United States and Europe in 2015.[3][2] In the United Kingdom it costs the NHS about £340 every 4 weeks as of 2021.[4] This amount in the United States is about 470 USD.[6]

    Medical uses

    Dosage

    It is used at a dose of 140 mg every two weeks or 420 mg once a month.[2]

    Mechanism

    Evolocumab is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface. In the absence of PCSK9, there are more LDL receptors on the surface of liver cells to remove LDL-C from the blood.[7]

    PCSK9 is a protein that targets LDL receptors for degradation and its inhibition thereby enhances the liver's ability to remove LDL-C, or "bad" cholesterol, from the blood.[8]

    History

    Amgen submitted a biologics license application (BLA) for evolocumab to the FDA in August 2014.[9] The FDA approved evolocumab injection on 27 August 2015, for some patients who are unable to get their LDL cholesterol under control with current treatment options.[10] The European Commission approved it in July 2015.[11] Evolocumab received approval from Health Canada on September 10, 2015.[12] Amgen reported approval by Health Canada in a press release on September 15, 2015.[13]

    Regeneron Pharmaceuticals and Amgen had each filed for patent protection on their monoclonal antibodies against PCSK9 and the companies ended up in patent litigation in the U.S. In March 2016 a district court found that Regeneron's drug alirocumab infringed Amgen's patents; Amgen then requested an injunction barring Regeneron and Sanofi from marketing alirocumab, which was granted in January 2017. The judge gave Regeneron and Sanofi 30 days to appeal before the injunction went into effect.[14]

    Results of the FOURIER trial were published in March 2017.[15]

    Society and culture

    Economics

    In 2015 it cost about US$14,100 per year. One article calculated this to be about $400,000 to $500,000 per quality-adjusted life year (QALY), which did not meet "generally accepted" cost-benefit thresholds. The authors calculated that an annual cost of $4,500 would meet an acceptable $100,000 per QALY standard.[16] It is made by Amgen. On October 26, 2018 Amgen announced a 60% cut in price and the drug now costs $5,850 per year.[17]

    References

    1. ↑ Sheridan C (December 2013). "Phase 3 data for PCSK9 inhibitor wows". Nature Biotechnology. 31 (12): 1057–8. doi:10.1038/nbt1213-1057. PMID 24316621. S2CID 34214247.
    2. 1 2 3 4 5 6 "Repatha". Archived from the original on 19 October 2021. Retrieved 17 December 2021.
    3. 1 2 3 4 5 6 7 "Evolocumab Monograph for Professionals". Drugs.com. Archived from the original on 27 October 2020. Retrieved 17 December 2021.
    4. 1 2 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 222. ISBN 978-0857114105.
    5. ↑ "Repatha- evolocumab injection, solution Repatha- evolocumab kit". DailyMed. 6 May 2020. Archived from the original on 22 October 2020. Retrieved 20 October 2020.
    6. ↑ "Evolocumab Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 7 May 2016. Retrieved 17 December 2021.
    7. ↑ "PCSK9 инхибитори – нов клас медикаменти за лечение на дислипидемия | Списание МД". spisaniemd.bg. Archived from the original on 2018-10-28. Retrieved 2018-10-28.
    8. ↑ Weinreich M, Frishman WH (2014). "Antihyperlipidemic therapies targeting PCSK9". Cardiology in Review. 22 (3): 140–6. doi:10.1097/CRD.0000000000000014. PMID 24407047. S2CID 2201087.
    9. ↑ Amgen Submits Biologics License Application For Novel Investigational LDL Cholesterol-Lowering Medication Evolocumab To The FDA
    10. ↑ FDA News Release (August 27, 2015). "FDA approves Repatha to treat certain patients with high cholesterol". U.S. Food and Drug Administration. Archived from the original on 30 August 2015. Retrieved 30 August 2015.
    11. ↑ European Commission Approves Amgen's New Cholesterol-Lowering Medication Repatha™ (evolocumab), The First PCSK9 Inhibitor To Be Approved In The World, For Treatment Of High Cholesterol
    12. ↑ "Regulatory Decision Summary (SBD): REPATHA - 2015 - Health Canada". www.hc-sc.gc.ca. Archived from the original on 2015-10-07. Retrieved 2015-10-06.
    13. ↑ "Amgen - Media - In The News". www.amgen.ca. Archived from the original on 2016-03-04. Retrieved 2015-09-17.
    14. ↑ Feeley J, Bloomfield D, Decker S (5 January 2017). "Amgen Wins Ban on Sanofi's Praluent Cholesterol Drug Sales". Bloomberg News. Archived from the original on 2020-10-06. Retrieved 2021-08-30.
    15. ↑ Sabatine MS, Giugliano RP, Keech AC, Honarpour N, Wiviott SD, Murphy SA, et al. (May 2017). "Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease" (PDF). The New England Journal of Medicine. 376 (18): 1713–1722. doi:10.1056/nejmoa1615664. PMID 28304224. S2CID 1972937. Archived (PDF) from the original on 2018-07-19. Retrieved 2021-08-30.
    16. ↑ Kazi DS, Moran AE, Coxson PG, Penko J, Ollendorf DA, Pearson SD, et al. (August 2016). "Cost-effectiveness of PCSK9 Inhibitor Therapy in Patients With Heterozygous Familial Hypercholesterolemia or Atherosclerotic Cardiovascular Disease". JAMA. 316 (7): 743–53. doi:10.1001/jama.2016.11004. PMID 27533159.
    17. ↑ Goldman, Dana. "The bigger message behind Amgen's decision to slash cost of its Repatha cholesterol drug". MarketWatch. Archived from the original on 2018-11-28. Retrieved 2018-10-28.
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