Synonyms: AMG-145 | AMG145 | Repatha®
evolocumab is an approved drug (EMA & FDA (2015))
Compound class:
Antibody
Comment: Evolocumab is a clinically approved anti-PCSK9 (proprotein convertase subtilisin/kexin type 9) monoclonal antibody. Peptide sequences for this antibody are available from its IMGT/mAb-DB link. The development and discovery of this antibody is described in patent US8030457, where SEQ IDs 23 and 49 comprising clone 21B12 light and heavy chain variable regions respectively, match the peptide sequences in the INN record for evolocumab.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
No information available. |
Summary of Clinical Use ![]() |
In July 2015, the EMA approved evolocumab as a treatment for patients with uncontrolled cholesterol who require additional intensive low-density lipoprotein cholesterol (LDL-C) reduction. Patient groups include those with primary hypercholesterolemia of both heterozygous familial and non-familial (HeFH) and homozygous familial hypercholesterolemia (HoFH) origin. Evolocumab therapy represents an efficacious alternative treatment for hyperlipidemia [5]. Sabatine et al (2015) had reported positive safety and efficacy results from Phase 2 and III clinical trials comparing treatment with evolocumab plus standard therapy vs. standard therapy alone [4]. Click on this link to view ClinicalTrials.gov's list of currently registered trials assessing evolocumab. In August 2015, the FDA approved evolucumab injection for patients unable to control their LDL-C levels with existing treatment options. |
Mechanism Of Action and Pharmacodynamic Effects ![]() |
Evolocumab is designed to target proprotein convertase subtilisin/kexin type 9 (PCSK9), a protein involved in cholesterol homeostasis. Normally, PCSK9 binds to LDL receptors (LDLR) and induces their degradation. Mutated forms of PCSK9 can cause familial hypercholesterolemia [1-2]. LDLR are involved in the hepatic removal of LDL-cholesterol from the blood. Evolocumab effectively suppresses PCSK9 activity, meaning more LDLR are available for removal of LDL-cholesterol from the blood. |
External links ![]() |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |