Declopramide is an apoptosis inducer. Also, it inhibits NFkappaB activation by inhibition of IkappaBbeta breakdown. In preclinical research, Declopramide demonstrated strong antitumor properties. It had been in phase II clinical trials for the treatment of colorectal cancer. However, this research has been discontinued.

Faropenem medoxomil is an ester prodrug derivative of the beta-lactam antibiotic faropenem. The prodrug form of faropenem offers dramatically improved oral bioavailability and leads to higher systemic concentrations of the drug. Faropenem medoxomil is a broad-spectrum antibiotic that is highly resistant to beta-lactamase degradation. It was under development for the treatment of acute bacterial sinusitis, community-acquired pneumonia, acute exacerbation of chronic bronchitis, and uncomplicated skin and skin structure infections.

Dolastatin 10 is an unusual peptide of marine origin which binds to tubulin, inhibits microtubule assembly, resulting in the formation of tubulin aggregates and inhibition of mitosis. Dolastatin 10 has been used in trials phase II studying the treatment of Sarcoma, Leukemia, Lymphoma, Liver Cancer, among others. In case of hormone-refractory prostate cancer, it lacks significant clinical activity as a single agent and also dolastatin-10 is inactive against hepatobiliary and pancreatic carcinomas.

Metiamide is an antagonist of histamine H2-receptors synthesized at Smith Kline & French Laboratories. It potently inhibited gastric acid secretion. Metiamide demonstrated promising clinical effects in patients with duodenal ulcers but questionable safety.

Rebeccamycin analog (RA, Becatecarin/ BMS 181176, rebeccamycin derivative, NSC 655649) is an antitumor antibiotic with inhibitory activity against both topoisomerase I and II, and DNA-intercalating properties. The mechanism of action of becatecarin is not exactly known, but it is thought that by inhibiting (blocking) the function of topoisomerase enzymes, it will destroy cancer cells and slow down the growth of the tumour. On 25 July 2006, orphan designation (EU/3/06/388) was granted by the European Commission to Helsinn Birex Pharmaceuticals Ltd, Ireland, for becatecarin for the treatment of cancers of the biliary tree.

Pimonidazole (developed as RO 038799) is a derivative of 2-nitroimidazole, which forms adducts (binds to thiol-containing proteins) only at low oxygen tension. Pimonidazole is a novel nontoxic hypoxia marker for the complementary study of tumor hypoxia and cell proliferation in different types of cancer. The drawback of pimonidazole as a hypoxic marker is that it detects only severe hypoxia.

Eperezolid is an antibiotic agent developed for the treatment of a wide range of bacterial infections. The drug exerts its action by binding to 50 S ribosome subunit causing the inhibition of protein synthesis in bacterias. Eperezolid was tested in preclinical in vivo models of different becterial diseases in which it was shown to be active.

Eptapirone is a potent, selective and efficacious 5-HT1A receptor agonist. In rats, it is readily bioavailable after oral administration. Likely, because of its high efficacy at 5-HT1A receptors, Eptapirone exerted powerful antidepressant- and anxiolytic-like activity in animal models. Eptapirone given in the evening suppresses REM (rapid eye movement) sleep more than buspirone and implies a greater central effect on serotonin receptors, which is consistent with the preclinical data that indicate it has greater efficacy than buspirone. It has little effect on other sleep stages. Eptapirone has been in phase I clinical trials for the treatment of anxiety and major depressive disorder. However, this research has been discontinued.

Kynurenic acid is a product of the normal metabolism of amino acid L-tryptophan which has been shown to have a neuroactive profile. It exhibits activity against NMDA receptors and Neuronal acetylcholine receptor subunit alpha-7. It has been investigated as a potential therapeutic compound and as a biomarker in a number of neurological disorders. Although Kenyruic acid exhibits a poor penetration of the blood-brain barrier, it remains to be of particular interest to those researching Schizophrenia.

Fluprazine (previously known as DU27716), a psychoactive drug was studied as a behaviorally selective, anti-aggressive agent. Experiments on rodents have shown that fluprazine didn’t appreciably affect defensive attack or other defensive behaviors even though it strongly inhibited offensive attack. This agent is used to test both differences and similarities in neurochemical substrates and adaptive significance of different forms of intraspecific aggression.