- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: evinacumab-dgnb | Evkeeza® | REGN1500
evinacumab is an approved drug (FDA (2021))
Compound class: Antibody
Comment: Evinacumab is a fully human monoclonal antibody targeting angiopoietin-like 3 (ANGPTL3). Due to its role in lipid metabolism, ANGPTL3 is being investigated as a potential molecular target for the treatment of hypertriglyceridemia.
Peptide sequence and structural information for this antibody are available from its IMGT/mAb-db record.
A BLAST search of patented peptide sequences reveals that the heavy chain variable domain of evinacumab is identical to SEQ ID: NO 66 from patent US9018356 B2 , and the light chain variable region is identical to SEQ ID: NO 74 from the same patent (this heavy/light chain combination corresponds to antibody identifier H4H1276S).
Evinacumab utilises a different molecular mechanism compared to Regeneron's already approved anti-hyperlipidemic drug alirocumab (targets proprotein convertase subtilisin/kexin type 9).
|No information available.|
|Summary of Clinical Use|
|Evinacumab was advanced to clinical trial for its potential to treat homozygous familial hypercholesterolemia (HoFH), which is an ultra-rare genetic disease. HoFH is a difficult to treat disease, with patients struggling to control their cholesterol levels. The FDA granted evicanumab priority review in August 2020, as an adjunct to other lipid-lowering therapies in patients with HoFH. FDA's decision to approve evinacumab for this indication was announced in February 2021.|
|Mechanism Of Action and Pharmacodynamic Effects|
|ANGPTL3 inhibits lipoprotein lipase (LPL) activity leading to increased level of lipids , and subsequently regulates very low density lipoprotein (VLDL) triglyceride levels . The N-terminal coiled-coil region of ANGPTL3 inhibits LPL when expressed without the C-terminal fibrinogen region and therefore appears to confer its inhibitory function. The H4H1276S antibody clone in patent US9018356 B2, presumed to be evinacumab, inhibits the ANGPTL3-induced decrease in LPL activity in vitro , but does not block ANGPTL4-induced decrease in LPL activity. H4H1276S shows cross-species activity, inhibiting mouse and monkey ANGPTL3 at comparable levels to the human protein .|