Evolocumab
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | PCSK9 |
| Clinical data | |
| Trade names | Repatha |
| Other names | AMG-145[1] |
| Routes of administration | Subcutaneous injection |
| ATC code | |
| Legal status | |
| Legal status |
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| Identifiers | |
| CAS Number | |
| ChemSpider |
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| UNII | |
| Chemical and physical data | |
| Formula | C6242H9648N1668O1996S56 |
| Molar mass | 141.8 kg/mol g·mol−1 |
Evolocumab[2] (trade name Repatha) is a monoclonal antibody designed for the treatment of hyperlipidemia.
Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation and thereby reduces the liver's ability to remove LDL-C, or "bad" cholesterol, from the blood.[3]
In 2015 it cost about $14,300 USD per year which makes it not cost effective.[4] It is made by Amgen.[5]
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.
Approval status
Amgen submitted a biologics license application (BLA) for evolocumab to the FDA in August 2014.[6] 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.[7] European Commission approved it in July 2015.[8] Evolocumab received approval from Health Canada on September 10, 2015.[9] Amgen reported approval by Health Canada in a press release on September 15, 2015.[10]
References
- ^ Sheridan, C (2013). "Phase 3 data for PCSK9 inhibitor wows". Nature Biotechnology. 31 (12): 1057–8. doi:10.1038/nbt1213-1057. PMID 24316621.
- ^ World Health Organization (2012). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 108" (PDF). WHO Drug Information. 26 (4).
- ^ Weinreich, M; Frishman, W (2014). "Antihyperlipidemic therapies targeting PCSK9". Cardiology in Review. 3 (22): 140–6. doi:10.1097/CRD.0000000000000014. PMID 24407047.
- ^ Kazi, Dhruv S.; Moran, Andrew E.; Coxson, Pamela G.; Penko, Joanne; Ollendorf, Daniel A.; Pearson, Steven D.; Tice, Jeffrey A.; Guzman, David; Bibbins-Domingo, Kirsten (16 August 2016). "Cost-effectiveness of PCSK9 Inhibitor Therapy in Patients With Heterozygous Familial Hypercholesterolemia or Atherosclerotic Cardiovascular Disease". JAMA. 316 (7): 743. doi:10.1001/jama.2016.11004.
- ^ Statement On A Nonproprietary Name Adopted By The USAN Council - Evolocumab
- ^ Amgen Submits Biologics License Application For Novel Investigational LDL Cholesterol-Lowering Medication Evolocumab To The FDA
- ^ FDA News Release (August 27, 2015). "FDA approves Repatha to treat certain patients with high cholesterol". U.S. Food and Drug Administration. Retrieved 30 August 2015.
- ^ 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
- ^ "Regulatory Decision Summary (SBD): REPATHA - 2015 - Health Canada". www.hc-sc.gc.ca. Retrieved 2015-10-06.
- ^ "Amgen - Media - In The News". www.amgen.ca. Retrieved 2015-09-17.