Darglitazone is a member of the thiazolidinedione class of drugs and an agonist of peroxisome proliferator-activated receptor-γ (PPAR-γ), an orphan member of the nuclear receptor superfamily of transcription factors. It has a variety of insulin-sensitizing effects, such as improving glycemic and lipidemic control, and is used in the treatment of metabolic disorders such as type II diabetes. Darglitazone sodium had been in phase I clinical trials by Pfizer for the treatment of type 2 diabetes. However, this study has been discontinued.

D-glucitol hexanicotinate (sorbinicate, SN) is a derivative of nicotinic acid. In rabbits kept on a diet containing 1 g/day cholesterol for 12 weeks, sorbinicate displayed greater hypolipemic and antiatherogenic activity than an equidose of plain nicotinic acid at much lower and more constant plasma nicotinic acid levels. By modulating the bioavailability of nicotinic acid, sorbinicate maintains and in some cases enhances the pharmacological activity of the acid, avoiding at least some of its major side effects. Sorbinicate has effective lipid-lowering activity; the combination of hypolipidemic and anti-aggregating properties may prove important in primary and secondary prevention of atherosclerotic disease. It is suggested that the antilipolytic activity of sorbinicate is at least partly mediated by an inhibition of glucagon secretion (and/or synthesis).

Tiquinamide (Wy 24081) is a potent inhibitor of gastric secretion and gives good protection in animals against gastric and duodenal erosions induced by stress and chemical stimuli. It reduces basal as well as stimulated acid secretion but has no anticholinergic activity and is only a weak histamine H2 antagonist, since it is substantially more potent in inhibiting basal acid-secretion than the established H2-receptor antagonists, metiamide and burimamide. Since no other pharmacological effect of tiquinamide has been detected in isolated tissues, it seems unlikely that the gastric antisecretory effect of the compound results from a direct action on the peripheral autonomic nervous system. The report from Dr. Szabo on the protective effect of dopamine agonists against duodenal ulceration suggests a possible mechanism of action for tiquinamide.

Timoprazole is a substituted benzimidazole patented by Aktiebolag Hassle as an antisecretory agent that inhibits gastric acid secretion by interference with (H+-K+)-ATPase. Timoprazole given orally was found to be cytoprotective for the stomach when given 30 min prior to a challenge to boiling water, ethanol, or HCl. Timoprazole also prevented necrosis of the mucosa and acute ulcerations induced by alcohol in the rat fundus, as evaluated by histopathology.

Irsogladine, a mucosal protective drug, was developed in Japan for the treatment of peptic ulcer disease and acute gastritis. Irsogladine increases intracellular cyclic adenosine 3',5'-monophosphate content via non-selective inhibition of phosphodiesterase isozymes and exhibits gastric cytoprotection partly mediated by endogenous nitric oxide. These effects may account for a variety of actions of irsogladine in the gastrointestinal tract, including facilitation of gap junctional intercellular communication, inhibition of the reduced gastric mucosal blood flow response, suppression of reactive oxygen generation and so on.

Lucartamide is an antisecretory and antiulcer agent.

Biclofibrate was investigated as an antilipidemic agent.

Vanitiolide is a choleretic agent.

Timefurone is a benzopyranone derivative patented by pharmaceutical company Upjohn Co. for the treatment of atherosclerosis. Timefurone mediates the hypolipidemic effect via the reduction of the intracellular synthesis of cholesterol. In preclinical studies, Timefurone significantly lowered low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and total cholesterol in cholesterol-fed male rats and monkeys. Timefurone caused small but significant changes in several clinical chemistry parameters including creatinine, total bilirubin, albumin, glucose, serum glutamic-oxalacetic transaminase, and serum glutamic-pyruvic transaminase in cynomolgus monkeys

Imiglitazar (also known as TAK-559) is a dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist patented by Japanese pharmaceutical company Takeda Chemical Industries for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance, and impaired glucose tolerance. Imiglitazar shows potent hypoglycemic and hypolipidemic activity and has been studied in clinical trials in treating subjects receiving a stable dose of insulin to control type 2 diabetes mellitus. Unfortunately, Imiglitazar shows hepatotoxicity and has never been marketed.