Related Experiment Video
Updated: Mar 25, 2026
08:14
A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
8.7K
JCL roundtable: PCSK9 inhibitors in clinical practice
W Virgil Brown1, Patrick M Moriarty2, James M McKenney3
1Emory University School of Medicine, Atlanta, GA, USA.
Journal of Clinical Lipidology
|February 20, 2016
Summary
Two new FDA-approved drugs, alirocumab and evolucumab, offer advanced treatment options for lowering low-density lipoprotein cholesterol (LDL-C) in patients with familial hypercholesterolemia and atherosclerotic cardiovascular disease.
Area of Science:
- Cardiology
- Pharmacology
- Genetics
Background:
- Elevated low-density lipoprotein cholesterol (LDL-C) is a major risk factor for cardiovascular disease.
- Familial hypercholesterolemia (FH) is a genetic disorder characterized by very high LDL-C levels.
- Existing therapies, including statins, may not be sufficient for all patients.
Purpose of the Study:
- To discuss the clinical implications of newly FDA-approved PCSK9 inhibitors.
- To provide insights for practicing physicians regarding the use of alirocumab and evolucumab.
- To review the evidence supporting the safety and efficacy of these novel lipid-lowering agents.
Main Methods:
- Discussion-based roundtable format.
- Expert review of clinical trial data.
- Focus on Food and Drug Administration (FDA) approved indications.
Main Results:
- Alirocumab approved for adults with heterozygous FH or atherosclerotic cardiovascular disease requiring additional LDL-C lowering.
- Evolucumab approved for similar indications plus homozygous FH.
- Both drugs represent a new class of lipid-lowering therapy: PCSK9 inhibitors.
Conclusions:
- PCSK9 inhibitors offer new therapeutic avenues for managing hypercholesterolemia.
- Physicians need to understand the specific indications and clinical utility of these agents.
- These drugs have the potential to significantly impact cardiovascular risk reduction.
Related Concept Videos
01:29Pharmacogenomics: Identification of New Drug Targets
76
Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
76
01:15Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions
65
PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure...
65
01:20Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
1.5K
Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
1.5K
01:23Dipeptidyl Peptidase 4 Inhibitors
1.0K
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
1.0K
01:20Lipid-Lowering Drugs: Statins and Miscellaneous Agents
1.8K
Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
1.8K
01:30Inhibitors of Viral Protein Synthesis
16
Protein synthesis is indispensable for viral replication, as viruses lack the cellular machinery required for this process and must hijack the host's translational apparatus. In response, host cells deploy a critical innate immune defense involving interferons, specialized cytokines that play a central role in inhibiting viral propagation.Upon viral detection, infected cells release interferons that bind to receptors on adjacent uninfected cells, activating the JAK-STAT signaling pathway and...
16