Terbufibrol, an antihyperlipoproteinemic agent that blocks the hepatic cholesterol synthesis in a step between acetate and HMG-CoA (3-hydroxy-3-methylglutaryl-CoA). Information about the current use of this compound is not available.

Terbuprol was developed as a choleretic agent that has never been marketed. Information about the current use of this drug is not available.

Indeglitazar is orally available peroxisome proliferator-activated receptor (PPAR) pan-agonist for all three PPAR subtypes alpha (α), delta (δ) and gamma patented by Plexxikon, Inc for metabolic disorders treatment. Indeglitazar is a full agonist of PPAR alpha but only a partial agonist of PPAR gamma and delta; this may provide a better side effect profile than full activators. The molecule shows impressive pharmaceutical properties (high oral bioavailability, the long half-life, etc.) as well as promising activity in mouse and rat models of diabetes (lower blood glucose, insulin, total cholesterol, triglycerides, free fatty acids, etc.). In contrast to other PPAR agonists, which sometimes cause weight gain, Indeglitazar also caused weight loss in rodent and primate models. Although Indeglitazar was advanced to phase 2 trials in collaboration with Wyeth, increasing concerns over the potential side effects of PPAR agonists have caused Wyeth to discontinue development of this compound

Treloxinate is a potent hypolipidemic agent. Treloxinate and its acid are structurally related to clofibrate. The activities of treloxinate and its acid form have been found to be identical. In rats treloxinate is 8 times as potent as clofibrate in reducing plasma cholesterol levels and 30 times as potent in lowering plasma triglyceride concentration.

Lozilurea (N' -3-chlorobenzyl-N'-ethylurea, ITA 312) has shown marked anti-ulcer activity. It has shown itself to be active against chemically and neurogenically induced gastric and duodenal lesions in various experimental animal models. It has no major anti-secretory action. The experimental data obtained suggest that the mechanism of action of lozilurea consists in increasing the protective function of the mucus barrier. It increased gastric levels of hexosamines and mucoproteins. In the screening trials carried out in order to detect the side effects of lozilurea, it has shown sedative, antipyretic and vasodilatory actions.

Thiohexamide is a first-generation, cyclohexyl-containing sulfonylurea with antihyperglycemic activity. The hypoglycemogenic activity of thiohexamide was detected in fasting, stable diabetic subjects.

Netoglitazone (also called MCC-555) is a hypoglycemic agent belonging to the thiazolidinedione group that exerts both peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist activity. It was developed by Mitsubishi-Tokyo (formerly Mitsubishi Chemical) as a potential treatment for type 2 diabetes due to the enhancement of insulin sensitivity. This drug was in clinical trial phase II but then was discontinued. In addition, was also investigated the behaviour of MCC-555 on colorectal cancer (CRC) cells and was revealed, that the drug had an effect on the early events of colon carcinogenesis and could be a potential preventive compound for CRC.

Tiqueside is the synthetic spirostane-based steroid glycoside. It precipitates cholesterol from micellar solution in vitro and reduces plasma cholesterol absorption in rats through a mechanism that is currently thought to be independent of either association of the saponin with the intestinal mucosal surface or absorption of the saponin molecule. As a consequence of this inhibition, tiqueside has been shown to reduce plasma cholesterol concentrations in cynomolgus monkeys. Inhibition of cholesterol absorption by tiqueside produces profound effects on cholesterol metabolism without affecting bile acid metabolism, and these changes lead to reductions primarily in plasma non-HDL cholesterol concentrations. Tiqueside produced a dose-dependent reduction in plasma LDL cholesterol levels in the hypercholesterolemic patients. In the mechanistic study, it decreased fractional cholesterol absorption rates and increased fecal neutral sterol excretion rates, changes associated with trends toward lower LDL cholesterol levels. Other lipoprotein levels were unaffected, as were fecal fat and bile acid excretion and fat-soluble vitamin absorption. Thus tiquesidedose-dependently inhibits cholesterol absorption in humans, resulting in a reduction in serum LDL cholesterol levels.

Aronixil was developed as an anti-atherosclerotic drug.

Ecabapide (DQ 2511) is a compound with antiulcer and gastroprokinetic activity. Evidence from basic studies in animal models suggests that the drug acts on peripheral mechanisms of neural control. In the stomach, ecabapide acts to suppress firing in vagal afferent nerves and thereby reduce the flow of sensory information into the dorsal vagal complex. The mechanism of action of ecabapide in suppressing discharge in vagal afferent terminals appears to mimic that of nitric oxide by stimulating formation of cGMP and activation of an inhibitory transduction cascade in the sensory fibres. In this respect the mechanism of its pro-kinetic action differs from other promoter agents. Ecabapide development has been discontinued.