evolocumab

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evolocumab

GtoPdb Ligand ID: 7343

Synonyms: AMG-145 | AMG145 | Repatha®

evolocumab is an approved drug (EMA & FDA (2015))

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.

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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.

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.

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.