Niacin, also known as vitamin B3 or nicotinic acid, is an organic compound with the formula C5H4NCO2H. This colourless, water-soluble solid is a derivative of pyridine, with a carboxyl group (COOH) at the 3-position. Other forms of vitamin B3 include the corresponding amide, nicotinamide ("niacinamide"), where the carboxyl group has been replaced by a carboxamide group (CONH2), as well as more complex amides and a variety of esters.
The bile acid sequestrants are a group of medications used to bind certain components of bile in the gastrointestinal tract. They disrupt the enterohepatic circulation of bile acids by sequestering them and preventing their reabsorption from the gut. They are generally classified as hypolipidemic agents, although they may be used for purposes other than lowering cholesterol.
Ezetimibe is an anti-hyperlipidemic medication that is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. It may be used alone, marketed as Zetia,when other cholesterol-lowering medications are not tolerated, or together with statins when cholesterol levels are unable to be controlled on statins alone. Ezetimibe was originally discovered by a team of four Schering-Plough research chemists: Drs. Stuart B. Rosenblum, Duane A. Burnett, John W.
Cholestyramine or colestyramine (Questran, Questran Light, Cholybar) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. The resin is a strong anion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix.
Phytosterols (also called plant sterols) are a group of steroid alcohols, phytochemicals naturally occurring in plants. Phytosterols occur naturally in small quantities in vegetable oils, especially sea buckthorn oil (1640 mg/100g oil), corn oil (968 mg/100g), and soybean oil (327 mg/100g oil). One such phytosterol complex, isolated from vegetable oil, is cholestatin, composed of campesterol, stigmasterol, and brassicasterol, and is marketed as a dietary supplement.
Torcetrapib was a drug being developed to treat hypercholesterolemia and prevent cardiovascular disease. Its development was halted in 2006 when phase III studies showed excessive all cause mortality in the treatment group receiving a combination of atorvastatin and the study drug.
ApoA-1 Milano is a naturally occurring mutated variant of the apolipoprotein A1 protein found in human HDL, the lipoprotein particle that carries cholesterol from tissues to the liver and is associated with protection against cardiovascular disease. ApoA1 Milano was first identified by Dr Cesare Sirtori in Milan, who also demonstrated that its presence significantly reduced cardiovascular disease, even though it caused a reduction in HDL levels and an increase in triglyceride levels.
Anti-cholesterol is a naturally occurring antibody to cholesterol produced by mammals. It is believed that this antibody serves a ‘housekeeping’ or protective role for the host animal, helping to protect the animal from harmful forms of cholesterol such as LDL and VLDL.
Cholesterol absorption inhibitors are a class of compounds that prevents the uptake of cholesterol from the small intestine into the circulatory system. An example is ezetimibe, previously known as "Sch-58235". Another example is Sch-48461. The "Sch" is for Schering-Plough, where this class was developed.
Colesevelam is a bile acid sequestrant administered orally. It is developed by Genzyme and marketed in the US by Daiichi Sankyo under the brand name WelChol and elsewhere by Genzyme under the tradename Cholestagel.
Acipimox is a niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects,although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid . These drug inhibit hepatic triglyceride production and VLDL secretions,which leads indirectly to a modest reduction in LDL and increase in HDL. Longterm administration is associated with reduced mortality, but unwanted effects limit it's clinical use.
Benfluorex is an anorectic and hypolipidemic agent. Clinical studies have shown it may improve glycemic control and decrease insulin resistance in people with poorly controlled type 2 diabetes; it is marketed in France as an adjuvant antidiabetic.
Lapaquistat (TAK-475) is a cholesterol-lowering drug. Unlike statins, which inhibit HMG-CoA reductase, lapaquistat metabolites inhibit squalene synthase, which is further downstream in the synthesis of cholesterol. It is hoped that side effects can be reduced by not disturbing the mevalonate pathway, which is important for other biochemical molecules besides cholesterol.
AEGR-773 (previously BMS-201038) is an investigational drug for the treatment of familial hypercholesterolemia, developed by Aegerion Pharmaceuticals. It has been tested in several Phase II clinical trials as single treatment and in combinations with atorvastatin, ezetimibe and fenofibrate. As of February 2009, a Phase III trial is recruiting participants.