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.

Tecastemizole (aka Norastemizole) is an H1 receptor antagonist that showed great promise as potential next-generation antihistamine allergy medication. Sepracor developed Norastemizole through phase III clinical trials; however, the FDA rejected the application for approval on the grounds of an unacceptable profile of adverse side-effects including phospholipidosis and cardiomyopathies in animals exposed to the drug.

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

Mequidox is an antibacterial agent.

Meclorisone is a synthetic corticosteroid exerting anti-inflammatory activity.

Prednival is prednisolone derivative patented by Francesco Vismara, Societa per Azioni as anti-inflammatory and progestational agent.

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.

Nifurimide, a 5-nitrofuran derivative, is an antibacterial agent. It was used for controlling Salmonella choleraesuis in swine. The mode of action of 5-nitrofuran analogues is based on red-ox biotransformation.