Evacetrapib (LY2484595) is a novel benzazepine-based CETP inhibitor that has been developed at Lilly Research Laboratories. Evacetrapib inhibits CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3. On 01 Sep 2016 Eli Lilly terminates the phase III ACCENTUATE trial in Hyperlipidaemia (Adjunctive treatment) in USA and Puerto Rico (PO) due to insufficient efficacy (NCT02227784).

Khelloside is a component of Ammi visnaga L. fruits extract, a medicine which is used in Egypt as remedy for the treatment of kidney stones. Khelloside itself exhibits a wide variety of biological activities including anti-anginal, antiatherosclerotic, lipid altering, antipyretic and spasmolytic. It was clinically tested for asthma, angina pectoris and skin disease, however its develoment seems to be discontinued.

Hyodeoxycholic acid, also known as HDCA, is a secondary bile acid. Natural 6alpha-hydroxylated bile acids are receptor-specific activators of nuclear liver X receptor alpha (LXRalpha), a nuclear receptor regulating the expression of the cholesterol 7alpha-hydroxylase gene. AHRO-001 (Hyodeoxycholic acid) is in phase I clinical trials for the treatment of atherosclerosis. Through a complex signaling processes utilizing LXR receptors, the compound is designed to increase the efficiency of cholesterol efflux using the HDL cells, which act on all cholesterol in the arterial circulation as well as in the lipid core of plaque deposits in the artery walls. Use of AHRO-001 has shown no adverse effects on morbidity, mortality or toxicity and has been well tolerated at high doses.

Desacetoxymatricarin is a sesquiterpene lactone found in the genus Artemisia and in the form of 8-hydroxy and acetoxy derivatives in the genus Achillea. The formation of desacetoxymatricarin from (+)-costunolide probably involves more than one enzyme, including a cytochrome P450 enzyme. It is a potent 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitor. Desacetoxymatricarin showed the highest anti-hypercholesterolemic potential. Oligvon, a preparation containing desacetoxymatricarin, is used to prevent and treat artherosclerosis.

(R)-Bambuterol is a selective β2-adrenoceptor agonist. R-Bambuterol Hydrochloride Tablets ("Laevo-Bambuterol") is categorized as a Class 1 new drug. Its preclinical studies show that it is more effective and have lower toxicity than Bambuterol, a popular asthma drug currenTLy on the market. Laevo-Bambuterol was approved by the China Food and Drug Administration for the treatment of asthma.

Riboflavin 5'-acetate (aka riboflavin acetate) is a derivative of riboflavin which has a single acetylation on the ribityl moiety. There is a patent which describes the use of 'riboflavin acetate' in combination with pravastatin to reduce the serum cholesterol of beagles. However, it should be noted that riboflavin tetraacetate is sometimes colloquially referred to as riboflavin acetate.

Asarinin, an urofuran lignan, is the epimer of sesamin. Asarinin is listed in Chinese Pharmacopoeia and used as a quality control (QC) index of crude herbs by the State Food and Drug Administration of China. Asarinin exhibits several biological activities such as decreasing cholesterol levels, exhibiting antihypertensive and antiangiogenic properties and providing immunosuppressive and hepatoprotective activities. Asarinin can also inhibit myocardial injury in metabolic syndrome of rats and decrease the possibility of acute heart transplant rejection. Sesamin was first isolated from sesame seed oil, while asarinin was first isolated from prickly ash bark. Both sesamin and asarinin have been shown to act as insecticidal synergists with pyrethrins.

Jatrorrhizine is an active component of the traditional Chinese herb Coptis chinensis, which has been used to prevent and treat metabolic disorders. It is also found plants such as Enantia chlorantha, Thalictrum lucidumm, Thalictrum revolutum. Jatrorrhizine possesses antifungal, antibacterial activity. It has low toxicity and was studied in mouse models of obesity and hypercholesterolemia. The mechanism of action of Jatrorrhizine is not fully elucidated. The compound blocks alpha-1 and alpha-2 adrenoreceptors, monoamine oxidase A and B.

Apocholic acid is a product of mild dehydration of cholic acid. Apocholic acid is powerful complexing and enolizing agent, giving stable addition-compounds (“choleric acids”) with numerous organic molecules. It was shown, that apocholic acid is able to produce tumors in situ. Apocholic acid was found to have a decreasing effect on the cholesterol level of both the plasma and the liver of rats.

Delta-tocotrienol is a member of vitamin E family. Tocotrienols are natural compounds found in a number of vegetable oils, wheat germ, barley, and certain types of nuts and grains. Tocotrienol-rich products such as DeltaGold® are gerally recognized as safe and are commecrially available as a dietary supplements. Tocotrienols possess powerful neuroprotective, antioxidant, anti-cancer and cholesterol lowering properties. The mechanism involved in anti-cancer activity of tocotrienols are still unclear, and include activation of caspases, downregulation of Bcl-2 and cyclin D, inhibition of angiogenesis, inhibition of cell proliferation though cell cycle arrest, downregulation of Raf/Erk pathway.