Evolocumab mechanism to reduce LDL cholesterol (WP3408)

Homo sapiens

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Evolocumab (Repatha) is an injectable monoclonal antibody that reduces LDL cholesterol levels. A limited quantity of LDL cholesterol is extracted from circulative blood when PCSK9-bound LDLR is degraded upon internalization in liver cells. Evolocumab competitively binds PCSK9 away from LDLR complexes, which allows LDLR to be recycled, returning to the surface and clearing additional molecules of LDL cholesterol.

Authors

Alex Pico , Egon Willighagen , Susan Coort , Denise Slenter , Eric Weitz , Marvin Martens , Martina Summer-Kutmon , and Lars Willighagen

Activity

last edited

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Organisms

Homo sapiens

Communities

Diseases

Annotations

Pathway Ontology

drug pathway altered cholesterol biosynthetic pathway altered cholesterol transport pathway

Cell Type Ontology

hepatocyte

Participants
Query Drugst.One

Label Type Compact URI Comment
LDL-C Metabolite chebi:47774
Evolocumab Metabolite wikidata:Q15623825
PCSK9 GeneProduct ensembl:ENSG00000169174
LDLR GeneProduct ensembl:ENSG00000130164

References

  1. PCSK9 inhibitors: the next cholesterol-lowering blockbusters? The Pharmaceutical Journal [Internet]. 2015; Available from: http://dx.doi.org/10.1211/PJ.2015.20068181 DOI Scholia