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| ==Side effects== | ==Side effects== | ||
| Side effects that occurred in more than 2% of people treated with in clinical trials and that occurred more frequently than with placebo, included nose and throat irritation, injection site reactions and bruising, flu, urinary tract infection, diarrhea, bronchitis and cough, and muscle pain, soreness, and spasms.<ref name=Label/> | Side effects that occurred in more than 2% of people treated with in clinical trials and that occurred more frequently than with placebo, included nose and throat irritation, injection site reactions and bruising, flu, urinary tract infection, diarrhea, bronchitis and cough, and muscle pain, soreness, and spasms.<ref name=Label/> | ||
| ==Pharmacology== | |||
| {{main|PCSK9}} | |||
| Alirocumab works by inhibiting the ]. PCSK9 binds to the ] (EGF-A) domain of the ], which leads to the receptor being degraded, and thus less ] being removed from circulation. Inhibiting PCSK9 prevents the LDLR from being degraded, and thus promotes removal of LDL cholesterol from circulation.<ref name=uendo>*{{cite web | url = http://www.uendocrine.com/resources/presentations/item/36-the-evolving-role-of-pcsk9-modulation-in-the-regulation-of-ldl-cholesterol | title = The Evolving Role of PCSK9 Modulation in the Regulation of LDL-Cholesterol | accessdate = 13 May 2015 }} | |||
| </ref> | |||
| ==Physical and chemical properties== | |||
| ==History== | ==History== | ||
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| Monoclonal antibody | |
|---|---|
| Type | ? |
| Source | Human |
| Target | Proprotein convertase subtilisin/kexin type 9 (PCSK9) |
| Clinical data | |
| Trade names | Praluent |
| Routes of administration | Subcutaneous injection |
| ATC code |
|
| Legal status | |
| Legal status |
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| Identifiers | |
| CAS Number | |
| ChemSpider | |
| Chemical and physical data | |
| Formula | C6472H9996N1736O2032S42 |
| Molar mass | 146.0 kDa g·mol |
Alirocumab (trade name Praluent) is a human monoclonal antibody PCSK9 inhibitor biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment of hypercholesterolemia for adults whose cholesterol is not controlled by diet and statin treatment. It is also known as REGN727 and SAR236553.
Medical uses
Alirocumab is used as a second line treatment to lower LDL cholesterol for people who have hereditary high cholesterol and people with atherosclerosis who require additional lowering of LDL cholesterol when diet and statin treatment have not worked. It is administered by injection.
Side effects
Side effects that occurred in more than 2% of people treated with in clinical trials and that occurred more frequently than with placebo, included nose and throat irritation, injection site reactions and bruising, flu, urinary tract infection, diarrhea, bronchitis and cough, and muscle pain, soreness, and spasms.
Pharmacology
Main article: PCSK9Alirocumab works by inhibiting the PCSK9. PCSK9 binds to the epidermal growth factor-like repeat A (EGF-A) domain of the low-density lipoprotein receptor (LDLR), which leads to the receptor being degraded, and thus less LDL cholesterol being removed from circulation. Inhibiting PCSK9 prevents the LDLR from being degraded, and thus promotes removal of LDL cholesterol from circulation.
Physical and chemical properties
History
It was discovered by Regeneron Pharmaceuticals and is being co-developed with Sanofi. A main competitor in the race to worldwide health authority approval is evolocumab in development by Amgen.
In July 2015, the FDA approved alirocumab as a second line treatment to lower LDL cholesterol for people who have hereditary high cholesterol and people with atherosclerosis who require additional lowering of LDL cholesterol when diet and statin treatment have not worked. This was the first approval of a PCSK9 inhibitor.
References
- International Nonproprietary Names for Pharmaceutical Substances (INN), World Health Organization
- Attention: This template ({{cite pmid}}) is deprecated. To cite the publication identified by PMID 24316621, please use {{cite journal}} with
|pmid=24316621instead. - ^ Alirocumab label Label revised, July 2015. Page accessed July 25, 2015
- *"The Evolving Role of PCSK9 Modulation in the Regulation of LDL-Cholesterol". Retrieved 13 May 2015.
- ^ FDA. July 24, 2015 FDA Press release: FDA approves Praluent to treat certain patients with high cholesterol
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