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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 }}
Alirocumab works by inhibiting the ]. PCSK9 binds to 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 }}
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Revision as of 20:24, 25 July 2015
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Alirocumab (trade name Praluent) is a human monoclonal antibodyPCSK9 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.
Alirocumab works by inhibiting the PCSK9. PCSK9 binds to 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.
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^ Alirocumab label Label revised, July 2015. Page accessed July 25, 2015
