Foropafant is a platelet-activating factor (PAF) antagonist which was developed by Sanofi. It was in clinical development for the treatment of asthma, thrombosis and ulcerative colitis. The development of the drug was discontinued due to lack of efficacy.

Saracatinib (AZD0530) is an oral, dual inhibitor of c-Src/Abl kinases initially developed by AstraZeneca for the treatment of cancer. The drug was tested for many neoplasms and reached phase III for ovarian cancer (in combination with paclitaxel), however without demonstrating any significant effect. Sarcatinib is also tested in patients with Alzheimer's Disease (Phase II). Its effect on Alzheimer's Disease patients is explained by inhibition of another kinase, Fyn, which is highly expressed in brain.

Mitemcinal (GM-611), an erythromycin-derived prokinetic agent, was developed by Chuga as an agonist of the motilin receptor. Mitemcinal acts by a novel mechanism whereby it stimulates and promotes peristalsis in the stomach and other segments of the gastrointestinal tract. This drug was studied as a potential treatment for gastric motility disorder, as well as reflux esophagitis, non-ulcer dyspepsia, and diabetic gastroparesis. Mitemcinal was involved in phase II clinical trials in Patients with diabetic gastroparesis. Although gastroparetic symptoms improved with both mitemcinal and placebo, the prominent placebo effect was not statistically exceeded by mitemcinal. That is why the development of this drug has stalled. In addition, mitemcinal has been studied in phase II for the treatment of irritable bowel syndrome, but this study was also discontinued.

Aplindore (DAB-452) is a small molecule that displays potent dopamine D2 receptor partial agonist activity in in vitro and in vivo assays and is predicted to have antipsychotic efficacy without motor side effects. Aplindore had been in phase II clinical trials for the treatment of Parkinson's disease and restless legs syndrome. Aplindore was generally well tolerated and there were no withdrawals due to adverse events and no serious adverse events.

Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.

Liarozole is an imidazole-containing compound that inhibits the cytochrome P-450-dependent metabolism of all-trans-retinoic acid (RA). Liarozole, a retinoic acid (RA) metabolism-blocking agent (RAMBA) in clinical development, has been granted orphan drug designation for congenital ichthyosis by the European Commission and the U.S. Food and Drug Administration. Later, based on the mixed results from a phase II/III trial of liarozole for the treatment of ichthyosis, Barrier decided to discontinue the development of liarozole. Liarozole displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.A large phase III international study was completed comparing liarozole 300 mg twice daily with cyproterone acetate (CPA) 100 mg twice daily in a total of 321 patients with metastatic prostate cancer in relapse after first-line endocrine therapy. The results indicate that liarozole might be a possible treatment option for prostate cancer (PCA) following failure of first-line endocrine therapy.

Eplivanserin (SR 46349) is an antagonist of serotonin 2A receptor. Eplivanserin was previously in development by Sanofi-aventis in an effort to educate the public regarding this new mechanism of action for sleep aids. Eplivanserin was reviewed by the FDA as a potential treatment for patients with chronic insomnia, but the FDA requested additional information regarding benefit-risk and development of the drug has been discontinued.

Celivarone is a benzofuran derivative with a multifactorial mode of action including class IV Vaughan Williams’ electrophysiological as well as anti-adrenergic properties. It has no iodine and has a limited tissue accumulation compared with amiodarone. Celivarone exhibits effective anti-arrhythmic properties in several ventricular ischemia- or reperfusioninduced arrhythmia models as well as in in vitro and in vivo atrial fibrillation (AF) models. Its electrophysiological properties are similar to amiodarone (multifactorial mode of action) but with different relative effects on the ion channels. At the ventricular level, celivarone shows anti-arrhythmic activities by suppressing reperfusion-induced arrhythmias (i.v. and oral routes) and reducing the early mortality due to myocardial infarction (oral route) in rats models. At the atrial level, celivarone is effective in atrial fibrillation models with restoration of sinus rhythm or prevention of AF induction and AF recurrence.

Clovoxamine is an antidepressant and anxiolytic drug, acting as a serotonin and norepinephrine reuptake inhibitor. The drug was investigated in the double-blind clinical trials for the treatment of anxiety neurosis, where it was compared with diazepam, and found to have comparable efficacy but higher drop out rate.

Linogliride is a substituted guanidine structurally unrelated to the sulphonylureas but with a similar mechanism of action. Linogliride potentiates insulin release in isolated islets and in the perfused pancreas. In islets, linogliride is reported to stimulate insulin secretion in the presence of glucose but not in its absence. Linogliride and the sulphonylureas act via closely related mechanisms. Possible extrapancreatic effects of the agent have also been suggested. Linogliride produces hypoglycaemic effects in various non-diabetic and diabetic animals. In normal rats and dogs, it improves glucose tolerance and in fasted rats or mice, linogliride lowers blood glucose. Linogliride showed modest effects in the db/db mice but significantly lowered fasting blood glucose in neonatal streptozotocin-treated rats. Clinical studies with non-insulin-dependent diabetes patients have shown linogliride to be effective at lowering fasting and postprandial plasma glucose levels in non-insulin-dependent diabetes patients. linogliride leads to a decrease in the activity of ATP-sensitive K+ channels.