Low density lipoprotein future or investigational therapies
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1] Associate Editor(s)-in-Chief:
Overview
The Unmet Need Driving Research Into Lowering LDL
Investigational Therapies
Inhibition of Apolipoprotein B production
Apolipoprotein B (apo B) is a large protein that is present in all atherogenic lipoproteins i.e., VLDL, LDL, IDL. There is a single copy of apo B-100 in all these lipoproteins, therefore plasma levels of apo B-100 is proportionate to the concentration of circulating atherogenic lipoproteins and a predictor of cardiovascular risk.[1] From the apoB gene, the liver synthesizes apo B-100; and the intestine synthesizes apo B-48. The apo B-100 serves two functions - provides structural stability to the circulating lipoproteins as well as acts as a ligand for LDL receptors. The removal of LDL from the plasma involves the binding of apo B to LDL, thus the resulting complex gets internalized into the liver.
PCSK9 Inhibition
Monoclonal Antibodies
Antisense Oligonucleotides (ASO)
Small Interfering RNAs (SiRNAs)
Microsomal Triglyceride Transfer Protein (MTP) Inhibition
Thyromimetics
Squalene Synthase Inhibition
Table
| Class | Drug Company | Agent Name | Mechanism of Action | Efficacy on Lowering LDL-C | Route of Administration | Adverse Effects | Published Clinical Trials |
|---|---|---|---|---|---|---|---|
| Inhibition of Apo B | |||||||
| PCSK9 Inhibition | |||||||
| MTP Inhibition | |||||||
| Thyromimetics | |||||||
| Squalene Synthase Inhibitors | |||||||
References
- ↑ van der Steeg, WA.; Boekholdt, SM.; Stein, EA.; El-Harchaoui, K.; Stroes, ES.; Sandhu, MS.; Wareham, NJ.; Jukema, JW.; Luben, R. (2007). "Role of the apolipoprotein B-apolipoprotein A-I ratio in cardiovascular risk assessment: a case-control analysis in EPIC-Norfolk". Ann Intern Med. 146 (9): 640–8. PMID 17470832. Unknown parameter
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