Ligand id: 7343

Name: evolocumab

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 II 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.