Anti-Human Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) (Alirocumab) – Fc Muted™

Unknown

This biosimilar antibody is aseptically packaged and formulated in 0.01 M phosphate buffered saline (150 mM NaCl) PBS pH 7.2 - 7.4 with no carrier protein, potassium, calcium or preservatives added. Due to inherent biochemical properties of antibodies, certain products may be prone to precipitation over time. Precipitation may be removed by aseptic centrifugation and/or filtration.

Liquid

Recombinant biosimilar antibodies are manufactured in an animal free facility using only in vitro protein free cell culture techniques and are purified by a multi-step process including the use of protein A or G to assure extremely low levels of endotoxins, leachable protein A or aggregates.

To protect mouse colonies from infection by pathogens and to assure that experimental preclinical data is not affected by such pathogens, all of Leinco’s recombinant biosimilar antibodies are tested and guaranteed to be negative for all pathogens in the IDEXX IMPACT I Mouse Profile.

Functional grade preclinical antibodies may be stored sterile as received at 2-8°C for up to one month. For longer term storage, aseptically aliquot in working volumes without diluting and store at ≤ -70°C. Avoid Repeated Freeze Thaw Cycles.

Research Use Only

2 – 8° C Wet Ice

This non-therapeutic biosimilar antibody uses the same variable region sequence as the therapeutic antibody Alirocumab. Alirocumab activity is directed against secreted proprotein convertase subtilisin/kexin type 9 (PCSK9).

PCSK9 is a negative regulator of liver low-density lipoprotein (LDL)-receptors (LDLR)¹ involved in maintaining lipoprotein homeostasis². PCSK9 binds to LDLRs responsible for LDL-C removal from the bloodstream. PCSK9 binds to LDLRs at the surface of hepatocytes, preventing LDLR recycling, and instead enhancing LDLR degradation³. This results in reduced numbers of LDLRs on liver cells and leads to high levels of circulating LDL-C². Pathogenic variants of LDLR² or PCSK9³ can be found in the autosomal dominant genetic disorder heterozygous familial hypercholesterolemia and can cause dysfunctional LDL-C metabolism and increased risk of premature atherosclerotic cardiovascular disease. Some patients with hypercholesterolemia, regardless of cause, are not able to attain target LDL-C levels with statins or ezetimibe, in which case monoclonal antibodies that inhibit PCSK9 can be used as an additional management tool².

Alirocumab is a PCSK9 inhibitor that limits the levels of circulating LDL-C^1,2. Alirocumab prevents PCSK9-mediated degradation of LDLRs, and thereby increases LDLR availability on the liver surface. This results in increased removal of LDL-C from serum.

Alirocumab has been approved for treatment of hypercholesterolaemia in both adult¹and pediatric (8–17 years)² patients.

PCSK9 is a circulating serine protease secreted from hepatocytes.

Low-density lipoprotein (LDL)-receptors (LDLR)

1 Markham A. Drugs. 75(14):1699-1705. 2015.
2 Kang C. Paediatr Drugs. 26(4):469-474. 2024.
3 Natarajan P, Kathiresan S. Cell. 165(5):1037. 2016.
4 Robinson JG, Farnier M, Krempf M, et al. N Engl J Med. 372(16):1489-1499. 2015.