Safety
Hazardous Substances Data | 1245916-14-6(Hazardous Substances Data) |
Alirocumab Chemical Properties,Usage,Production
Clinical Use
Human IgG1 monoclonal antibody:Treatment of primary hypercholesterolaemia / mixed dyslipidaemia
Enzyme inhibitor
This humanized anti-PCSK9 monoclonal antibody (MW = 146 kDa; CAS 1245916-14-6), developed as REGN727 (Regeneron Pharmaceuticals) and SAR236553 and Praluent? in cooperation with Sanofi, inhibits atherosclerosis, improves plaque morphology, and enhances statin effects. Its target, Pro-protein Convertase Subtilisin/Kexin type 9 (or PCSK9), is a secreted pro-protein convertase. Inhibition of PCSK9 increases hepatic Low-Density Lipoprotein Receptors (LDLRs), thereby enhancing hepatic LDL clearance. PCSK9 undergoes autocatalytic processing of its pro-domain within the endoplasmic reticulum, and its inhibitory pro-peptide segment remains associated with it following subsequent secretion. PCSK9 phosphorylation at Ser-47 in its pro-peptide and Ser-688 in its C-terminal domain by a Golgi casein kinase-like protein kinase appears to stabilize secreted PCSK9. The level of circulating PCSK9 appears to be inversely related to blood HDL levels, and it is understandable that cholesterol-lowering statins have the effect of increasing PCSK9 gene expression as well as the circulating level of PCSK9. Alirocumab binds to circulating PCSK9, blocking the latter’s action on surface LDLR. Alirocumab dose-dependently decreases plasma lipids and atherosclerosis progression, and it enhances the beneficial effects of atorvastatin in ApoE3-Leiden transgenic mice. (See also Evolocumab)Drug interactions
Potentially hazardous interactions with other drugsLive vaccines: risk of generalised infections - avoid.
Metabolism
As alirocumab is a protein it is expected to degrade to small peptides and individual amino acids. At low concentrations, the elimination is mainly through saturable binding to target (PCSK9), while at higher concentrations the elimination is largely through a nonsaturable proteolytic pathway.Preparation Products And Raw materials
Alirocumab Suppliers
Global(64)Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
+8613288715578 | sales@hbmojin.com | China | 12456 | 58 | |
+8613367258412 | ada@ipurechemical.com | China | 10326 | 58 | |
+86-0371-86658258 15093356674; |
laboratory@coreychem.com | China | 30255 | 58 | |
86 18062405514 18062405514 |
ada@ipurechemical.com | CHINA | 3465 | 58 | |
+8617315815539 | sales@minbiotech.com | CHINA | 129 | 58 | |
0571-85134551 | info@afinechem.com | CHINA | 15377 | 58 | |
+8615604608665 15604608665 |
dominicguo@gk-bio.com | CHINA | 9427 | 58 | |
+8619930503252 | daisy@crovellbio.com | China | 5964 | 58 | |
+8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 | |
+8618339805032 | alfa4@alfachem.cn | China | 12755 | 58 |
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