Ronifibrate, a hypolipidemic agent, is an agonist of peroxisome proliferator-activated receptor.

Acipimox (5-methylpyrazinecarboxylic acid 4-oxide) is a new lipolysis inhibitor that has a distant chemical relationship with nicotinic acid (NA). The anti-lipolytic action of acipimox is mediated through suppression of intracellular cyclic AMP levels, with the subsequent decrease in cyclic AMP-dependent protein kinase activity, leading to the reduced association of hormone-sensitive lipase with triacylglycerol substrate in the lipid droplet of adipocytes. Acipimox has been identified as an agonist at G-protein coupled nicotinic acid HM74A and HM74B receptors. Acipimox (Olbetam) is indicated for the treatment as alternative or adjunct treatment to reduce triglyceride levels in patients who have not responded adequately to other treatments such as statin or fibrate treatment for hypertriglyceridaemia (Fredrickson type IV hyperlipoproteinaemia) and hypercholesterolaemia and hypertriglyceridaemia (Fredrickson type IIb hyperlipoproteinaemia).

Alibendol (2-hydroxy-N-(2-hydroxyethyl)-3-methoxy-5-prop-2-enyl benzamide) is an antispasmodic, choleretic, and cholekinetic compound, used in the treatment of gastrointestinal disorders in Egypt

Theofibrate (Etofylline clofibrate, trade name Duolip) is the clofibric acid ester of theophylline, used for the treatment of hyperlipoproteinaemia with elevated triglycerides and cholesterol. The low dose of Etophylline clofibrate (750mg) has a similar lipid-lowering effect as pure clofibrate (1500mg), probably due to a synergistic hypolipidemic effect with theophylline, which has no lipid-lowering effect per se. Secondly, etophylline clofibrate substantially decreases platelet aggregability and plasma viscosity, properties which may be desirable in the prevention of coronary heart disease (CHD). Finally, etophylline clofibrate is clearly a less potent inducer of peroxisomal proliferation in the rat liver than clofibrate, bezafibrate or fenofibrate. Theofibrate increases lipoprotein lipase activity to promote the conversion of Very low-density lipoprotein (VLDL) to Low-density lipoprotein (LDL), and hence reduce the level of VLDL.

Nicofuranose is a niacin derivative used as a hypolipidemic agent. The Nicofuranose administration leads to inhibition of free fatty acid turnover and consequently a marked reduction in triglyceride turnover. Nicofuranose, unlike clofibrate, did not affect the mechanisms responsible for the clearance of plasma triglycerides.

Glibornuride is sulphonylurea derivative used as an oral hypoglycemic drug in patients with diabetes. The drug was marketed under the name Glutril, however, it is no longer available.

Buformin (1-butylbiguanide) is an oral antidiabetic drug of the biguanide class. AMPK activator. AMPK is a potential therapeutic target in the prevention and the treatment of type 2 diabetes and insulin resistance. Major classes of antidiabetic drugs have been reported to activate AMPK. Buformin exerts its anti-tumorigenic activity via activation of AMPK and inhibition of the mTOR signaling pathways in endometrial cancer cells. Toxicity: guinea pig LD50 subcutaneous 18 mg/kg; mouse LD50 intraperitoneal 140 mg/kg and 300 mg/kg oral. Buformin was withdrawn from the market in many countries due to an elevated risk of causing lactic acidosis.

Ebrotidine is the first of a new generation of H2 receptor antagonists with gastroprotective activity It stimulates epithelial cell proliferative activity and produces beneficial physicochemical changes in the gastric mucus that contribute to its gastro-protective action against ethanol-, aspirin- or stress-induced gastric mucosal damage The antisecretory properties of ebrotidine are similar to those of ranitidine and approximately 10-fold greater than those of cimetidine This drug exhibits anti-Helicobacter pylori activity that is synergistic with a number of antibacterial agents; it inhibits the urease enzyme and the proteolytic and mucolytic activities of H. pylori, and counteracts the inhibitory effects of H. pylori lipopolysaccharide Ebrotidine is as effective as ranitidine for the treatment of patients with gastric or duodenal ulcers or erosive reflux oesophagitis Ebrotidine therapy results in significantly better ulcer healing rates than ranitidine treatment in patients who smoke. Ebrotidine was marketed in Spain in early 1997 and withdrawn in July 1998. Shortly after the drug was approved, several cases of acute liver injury were reported to the Regional Pharmacosurveillante Centers, the manufacturer and to a Registry of Hepatotoxicity in use in Southern Spain since 1994. On the basis of these cases the manufacturer withdrew ebrotidine from the market on 27 July 1998. This drug was also marketed in two other countries: Paraguay and Maurice Island.

Troglitazone (TGZ, brand name: Rezulin and Prelay) is a peroxisome proliferator-activated receptor gamma (PPAR gamma) ligand, which was developed by Daiichi Sankyo and approved for the US market for the treatment of Type II diabetes mellitus. The drug is used alone or in combination with a sulfonylurea, metformin, or insulin as an adjunct to diet and exercise, and was not indicated as initial therapy in patients with type 2 diabetes. This drug was withdrawn from the UK market due to liver toxicity. It was removed from the US market in 2000, only 3 years after its introduction and from Japan, shortly afterward. In addition, was conducted a clinical trial for the treatment of patients with advanced liposarcoma by using troglitazone, but the positive result wasn’t obtained. It was shown, that in case of cancer cells troglitazone acted independently of PPAR gamma, by up-regulation of early growth response-1 (Egr-1). Egr-1 transcription factor has been linked to apoptosis and shown to be activated by extracellular signal-regulated kinase (ERK).