MK-0533 is a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus. In comparison with PPARγ full agonists, MK-0533 displayed diminished maximal activity (partial agonism) in cell-based transcription activation assays and attenuated gene signatures in adipose tissue. MK-0533 exhibited comparable efficacy to rosiglitazone and pioglitazone in vivo. However, with regard to the induction of untoward events, MK-0533 displayed no cardiac hypertrophy, attenuated increases in brown adipose tissue, minimal increases in plasma volume, and no increases in extracellular fluid volume in vivo. MK-0533 was teste in phase II clinical trials but future development was discontinued.

Tecarfarin (also known as ATI-5923), an anticoagulant, is a vitamin K reductase antagonist. Tecarfarin is participating in phase III clinical trials for the treatment of thromboembolism and thrombosis. On March 11, 2019, Espero BioPharma Inc. announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for tecarfarin for the prevention of systemic thromboembolism of cardiac origin. Tecarfarin is metabolized by esterases, escaping metabolism by the cytochrome P450 system and thereby avoiding cytochrome P450-mediated drug-drug or drug-food interactions as well as genetic variations found in the cytochrome P450 system.

Eprotirome (KB2115) is a thyroid hormone mimetic developed at Karo Bio AB (Huddinge, Sweden). Eprotirome has a 22-fold higher affinity for thyroid hormone receptor (TR)β in comparison with TRα. It lowers plasma LDL cholesterol and stimulates bile acid synthesis. Eprotirome can lower LDL cholesterol concentrations in patients with familial hypercholesterolaemia when added to conventional statin treatment with or without ezetimibe, but that it has the potential to induce liver injury. These findings, along with findings of cartilage damage in dogs, raise serious doubts about selective thyroid hormone mimetics as a therapeutic approach to lower LDL cholesterol concentrations. Eprotirome development was discontinued.

Cicloprofen is fluorene derivative patented by American pharmaceutical company E. R. Squibb as anti-inflammatory agents. Cicloprofen is potent cyclooxygenase inhibitor. Cicloprofen undergoes hydroxylation of the fluorene rings and conjugation with glucuronic acid or sulfate and metabolic transformation leading to stereospecific inversion of the ( - )-enantiomer of Cicloprofen to its (+)-antipode

Amfonelic acid (AFA) is a dopamine reuptake inhibitor. Experiments on rats have shown that AFA treatment completely prevented the effects of methamphetamine on the dopaminergic system, both morphologically and biochemically.

Clodanolene is a skeletal muscle contraction antagonist, closely related to dantrolene sodium. The drug has no measurable direct effect on the peripheral or central nervous systems. In a mouse of muscle spasticity (Straub-tail mouse), clodanolene induced skeletal muscle relaxation more effectively than neuromuscular blocking agents, local anesthetics, or centrally-acting muscle relaxants. Indirect evidence indicates clodanolene acts on caffeine-sensitive calcium stores in the muscle cells.

Fenestrel (ORF-3858) is a nonsteroidal antizygotic compound. It antagonizes progesterone. Fenestrel is a post-coital contraceptive.

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.

It is known that the terbucromil possessed uricosuric effects in man. However, information about the current development and use of this compound is not available.

Dazmegrel [UK 38485] is a thromboxane synthetase inhibitor which was undergoing development in the treatment of thrombosis, ischaemic heart disease, arrhythmias and asthma. Pfizer were conducting phase II studies in Denmark and the UK, phase I studies in Germany and Italy, and preclinical studies in France. Later this research was discontinued.