PubMed Health⌕ Search

PubMed · 15500389

Lipid-lowering therapies in development.

Abstract

Lipid lowering is established as a proven intervention to reduce atherosclerosis and its complications. This article summarises novel developments in the lipid-altering therapies under development, including combination therapies, squalene synthase inhibitors, microsomal transfer protein inhibitors, acyl-cholesterol acyl transferase inhibitors, cholesterol ester transfer protein antagonists, peroxisome proliferator-activated receptor agonists, high-density lipoprotein-derived peptides and inflammation inhibitors, which have at least reached trials in animal models. Lipid-altering drugs are likely to to be a fast-developing area for novel treatments as possible synergies exist between new and established compounds for the treatment of atherosclerosis. New agents will have to show significant advantage in tolerability or efficacy over existing agents and have the potential to be used in combination therapy as is well established for bile acid sequestrants, nicotinic acid or fibrates and statins. Any new drugs will also have to be assessed in clinical end-point trials against current compounds with proven outcome benefits.

Explore related subjects

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

Anthony S Wierzbicki. 2004. Lipid-lowering therapies in development.. https://doi.org/10.1517/13543784.13.11.1405

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

Molecular biology of PCSK9: its role in LDL metabolism.

Proprotein convertase subtilisin-like kexin type 9 (PCSK9) is a newly discovered serine protease that destroys low density lipoprotein (LDL) receptors in liver and thereby controls the level of LDL in plasma. Mutations that increase PCSK9 activity cause hypercholesterolemia and coronary heart disease (CHD); mutations that inactivate PCSK9 have the opposite effect, lowering LDL levels and reducing CHD. Although the mechanism of PCSK9 action is not yet clear, the protease provides a new therapeutic target to lower plasma levels of LDL and prevent CHD.

Cholesterol, LDL↗

Monday, Wednesday, and Friday dosing of rosuvastatin in patients previously intolerant to statin therapy.

Statins are normally administered for the treatment of dyslipidemia on a daily basis. This standard dosing regimen is well tolerated by most patients. Occasionally, patients discontinue therapy secondary to side effects, most commonly myalgias. We describe 2 patients who were unable to tolerate daily atorvastatin therapy secondary to myalgias and were subsequently treated with rosuvastatin administered on Mondays, Wednesdays, and Fridays, with resolution of adverse effects. Significant reductions in serum low-density lipoprotein cholesterol levels were observed in the 2 patients despite the alternate-day dosing regimen. Rosuvastatin was chosen because of its long half-life (19 hours) and very high potency.

Cholesterol, LDL↗