NMS-P937 is a selective PLK1 inhibitor. It was developed by Nerviano Medical Sciences and tested in phase I clinical trials.

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.

Mefenidil has been reported to be a selective cerebral vasodilator. It significantly increased cerebral blood flow (without stimulation of O2 uptake) and lowered cerebral vascular resistance without having significant effects in other circulatory regions. Increase in cerebral blood flow is not mediated via the beta-adrenergic receptor as the effect was not blocked by propranolol. However, the clinical usefulness of mefenidil as a cerebral vasodilator may be limited by the accompanying arterial hypotension due to systemic vasodilation, which was most prominent in heart and gut.

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.

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.

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.

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.

Tampramine (also known as AHR-9377) is a potent and selective, noncompetitive inhibitor of norepinephrine reuptake possesses antidepressant activity. This drug was studied for the treatment of the major depressive disorder; however, this study was discontinued.

Dazopride is an antagonist of the 5-HT3 receptor and agonist of the 5-HT4 receptor, structurally related to metoclopramide. Dazopride was developed by A. H. Robins Company as an antiemetic and gastroprokinetic drug. Dazoptide demonstrated an antiemetic effect in the clinic after i.v. infusion to patients, receiving anticancer therapy.