Trimoprostil is a synthetic prostaglandin E2 derivative and prostanoid receptor agonist, with potential gastric secretion inhibitor and antiulcerogenic activity. It has been shown to reduce hydrogen ion secretion, to enhance gastric bicarbonate secretion and to reduce aspirin-induced gastric mucosal injury. In contrast to many E prostaglandins, it does not lower the tone of the lower oesophageal sphincter. Trimoprostil was well tolerated and more effective than placebo in the treatment of mild to moderate symptomatic reflux oesophagitis. It may be protective to human squamous oesophageal mucosa. Trimoprostil was not as effective as cimetidine in the treatment of duodenal ulcer.

Halofenate (MK-185) was invented as a hypolipidemic and hypouricemic agent. It was shown that halofenate lower serum triglycerides and uric acid in patients with a variety of hyperlipidemias. Treatment of dyslipidemic type 2 diabetic patients also showed triglyceride lowering and, surprisingly, significant reductions in plasma glucose and insulin. Halofenate is a selective PPAR-γ modulator (SPPARγM). SPPARγMs are believed to bind in distinct manners to the ligand-binding pocket of PPAR-γ, leading to altered receptor conformational stability and resulting in distinct patterns of gene expression. Thus, was suggested that halofenate hold promising therapeutic potential in the treatment of type 2 diabetes, without the side effects. However, information about the current use of this compound is not available.

Colestolone (5 alpha-cholest-8(14)-en-3 beta-ol-15-one) is an inhibitor of sterol biosynthesis. The compound reduces the level of 3-hydroxy-3-methylglutaryl coenzyme A reductive activity in cultured mammalian cells. In nonhuman primates, the compound decreases the levels of total serum cholesterol and low-density lipoprotein and increases the percentage of total cholesterol associated with high-density lipoprotein.

Tolimidone, Lyn protein-tyrosine kinase stimulant, is in phase II clinical by Melior Discovery and Bukwang for the treatment of type 2 diabetes. It is also in phase II clinical by Pfizer for the treatment of ulcer. However, this research has been discontinued.

Tiformin (also known as γ-Guanidinobutyramide) is a butyramide derivate with antidiabetic activity. Tiformin was isolated for the first time from a medium containing arginine which had been transformed by washed cells of Streptomyces griseus. In preclinical models, oral administration of Tiformin depresses blood glucose in rats and rabbits. Tiformin given i.v. produced hyperglycemia and sometimes death of experimental animals. Tiformin is not significantly metabolized in the rat or dog.

Lifibrate is the antihyperlipidemic agent. It is a potent hepatic peroxisome proliferator. Administration of lifibrate at a dietary concentration of 0.15% for 3 weeks, increased the activity of catalase in both liver and kidney of male wild type (Cs-a strain) mice. The hypolipidemic activity of lifibrate is eight to nine times greater than that of chlorphenoxy isobutyric acid ethyl ester in the male Wistar rat.

Thyropropic Acid (also known as Triopron) is a hydrocinnamic acid derivative and naturally occurring thyroid analog with antigoitrogenic and anticholesteremic activity. Thyropropic Acid acts as potent antagonist of thyroid hormone receptors and may be useful in the therapy of resistance to thyroid hormone and corticosteroid-induced skin atrophy. In preclinical models, Thyropropic Acid reduced serum cholesterol 27% and liver incorporation of acetate into cholesterol 37% but did not affect liver cholesterol levels.

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.

Toquizine is an anticholinergic agent. It was used as an antiulcer agent.

Glidazamide is an antidiabetic drug. It is a hypoglycemic agent that is part of the second-generation sulfonamide urea derivatives.