Cevoglitazar is a dual agonist for the peroxisome proliferator-activated receptor (PPAR)-alpha and -gamma subtypes. Cevoglitazar was as effective as pioglitazone at improving glucose tolerance, normalizes intramyocellular lipids and reduces body weight gain and adiposity, independent of food intake. Metabolic profiling showed that in the muscle cevoglitazar improves the lipid profile via both PPARα‐ and PPARγ‐mediated mechanisms. Cevoglitazar only induced small changes to the lipid composition of visceral fat. In subcutaneous fat, however, cevoglitazar induced changes similar to those observed with fenofibrate suggesting export of fatty acids from this depot.

An oxazole compound, tioxaprofen, exerted a strong anti-mycotic activity against Trichophyton mentagrophytes and T. rubrum, which were major dermatophytes from patients. It was found that tioxaprofen was a potent uncoupling agent of mitochondrial respiration. Tioxaprofen inhibits the electron transport between cytochromes b and c1 in the mitochondrial respiratory chain. Tioxaprofen blocks the formation of thromboxane most probably by inhibition of cyclo-oxygenase.

Myfadol is a phenacylpiperidine derivative patented by Tanabe Seiyaku Co., Ltd as low molecular weight non-peptide analgesic. Myfadol produces hot-plate analgesia in rodents with minimal side-effects, and when given parenterally in humans produces analgesia to experimentally-produced and postoperative pain.

Remiprostol (also known as SC-46275) is a potent, long-acting gastric antisecretory agent that is not readily available systemically after oral administration. This prostaglandin analog is a very potent and highly selective EP3 receptor agonist with antisecretory and cytoprotective actions. Remiprostol was suggested to be potentially useful in the therapeutic treatment of inflammatory diseases such as peptic ulcer disease (painful sores or ulcers in the stomach or small intestine), ulcerative colitis, Crohn's disease, and autoimmune inflammatory diseases of the central nervous system.

Hexaprofen, a potent anti-inflammatory agent, is an inhibitor of platelet aggregation. Experiments on mice have shown that hexaprofen could reduce the quantity and size of Lewis lung carcinoma (LLC) tumor nodules.

Acevaltrate is an iridoid found in variable amounts in Valerianaceae and might be among the bioactive compounds which confer anxiolytic properties to the Valeriana species. Acevaltrate inhibited total H⁺/K⁺-ATPase activity (60.7 ± 7.3 %) from rat gastric epithelium. Acevaltrate inhibited Na⁺/K⁺-ATPase with IC₅₀ value of 22.8 uM. Na⁺/K⁺-ATPase might be one of their molecular targets of Acevaltrate in vivo.

Oxarbazole was developed as an antiasthmatic agent that inhibited the only bronchoconstriction induced by immune complexes. This drug has never been marketed.

Sobetirome (3,5-dimethyl-4[(4'-hydroxy-3'-isopropylbenzyl)-phenoxy] acetic acid, also known as GC-1 and QRX-431, is a member of a class of compounds known as selective thyromimetics. It was firstly developed by Thomas Scanlan’s group at the University of California-San Francisco (UCSF) in 1995. Sobetirome binds selectively to the main hepatic form of thyroid hormone (TH) receptor, TRβ1, compared to TRα1, which is principally responsible for thyrotoxic effects on heart, muscle and bone. Sobetirome also preferentially accumulates in liver. It was originally envisaged that sobetirome could be used to stimulate hepatic pathways that lower cholesterol without harmful side effects and might be used in conjunction with statins. Indeed, sobetirome progressed through preclinical animal studies and Phase I human clinical trials with excellent results and without obvious harmful side effects. Sobetirome had been in phase I clinical trials for the treatment of lipid metabolism disorders and obesity. However, this research has been discontinued.