Vadimezan (5,6-dimethyl(xanthenone-4-acetic acid), ASA404, DMXAA) is a fused tricyclic analogue of flavone acetic acid with potential antineoplastic activity. In pre-clinical mouse tumour models it was demonstrated that administration of Vadimezan rapidly leads to disruption of the existing vasculature in the tumour and consequent haemorrhagic necrosis of the tumour. This was consistent with the finding that a single dose of Vadimezan induced a prolonged reduction in the growth of xenografted tumours in animal models. The ability to disrupt the vasculature in these pre-clinical models has been attributed to a rapid induction of cytokines, particularly TNFα (tumour necrosis factor α), serotonin and nitric oxide, resulting in hemorrhagic necrosis and a decrease in angiogenesis. Despite the fact that the molecular targets for the drug remained unknown, the promising pre-clinical results led to Vadimezan being selected for clinical development. Results of Phase I trials showed some restriction of tumour blood flow within 24 h of treatment, although this was not as dramatic as seen in pre-clinical models. Unlike the animal models, there was also very little evidence for the rapid death of blood vessels or for increases in TNFα levels in human tumors. No difference in antitumour activity, cytokine induction or toxicity was observed between two parallel Phase I trials, one dosed weekly and the other dosed every 3 weeks. Therefore the drug proceeded to Phase II clinical trials, dosed every 21 days in combination with chemotherapeutic agents. These trials indicated the drug had small benefits in the treatment of non-small-cell lung cancer and prostate cancer. However, a subsequent Phase III clinical trial was not able to reproduce this response and clinical development was halted.

Pirdonium is an antihistamine agent. It is the hydrophilic Histamine H1 receptor antagonist.

Prifuroline is a benzofuran derivative patented by French pharmaceutical company Laboratoires Jacques Logeais S. A. As an antiarrhythmic agent. After intravenous administration to pentobarbital-anesthetized dogs, Prifuroline produced a significant dose-related decrease in heart rate and in sinus node recovery time. Prifuroline dose-dependently antagonizes the arrhythmogenic action of aconitine in rats when administered either intravenously or intraduodenally. Prifuroline also diminishes ventricular susceptibility to electrical stimulation in open-chest rats; its effect is comparable to that of disopyramide and amiodarone at the same dose levels. Prifuroline was also able to restore sinus rhythm in guinea-pigs after intracardiac conduction blockade with acetylcholine, although being devoid of anticholinergic activity.

Emakalim (EMD 56431) is ATP-sensitive potassium channel opener. It exerts vasorelaxant and cardioprotective effects. Emakalim was being developed for the treatment of hypertension and ischaemic heart disorders.

Methaphenilene, an antihistaminic agent, was studied as a peroxisome proliferator. Information about the current use of this compound is not available.

Enazadrem (CP-70490-09) is an antipsoriatic agent inhibiting arachidonate 5-lipoxygenase.

Bromofos is an organic thiophosphate used as pesticide and insecticide for apple-pest control. Bromophos possesses remarkable stability in alkaline media and extremely low mammalian toxicity. The oral toxicity for small rodents is 3.75 to 13.4 mg/kg. body wt. Bromofos acts as contact and stomach poison. Very good efficacy is obtained against flies and their larvae, especially against parasitic species on sheep. Bromopros in sheep dip soln. is as effective as diazinon. It is effective in stables for fly control, depending on the surface, for up to 14 weeks.

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.

Volpristin is an antibiotic. Information about the current use of this agent is not available.