Bisaramil, an antiarrhythmic drug was developed as an inhibitor of calcium transport and as a membrane stabilizer. In addition, the drug showed tonic and frequency-dependent block that is most potent against the heart Na+ channel. However, the phase-II for Arrhythmias in Japan was discontinued.

Mitratapide is a potent inhibitor of the microsomal triglyceride transfer protein used for the treatment of obesity in dogs. The drug was developed by Janssen Pharmaceutica and is chemically related to the antifungal drugs such as itraconazole which were also developed by Janssen. Administration of mitratapide to dogs results in reduced uptake of dietary lipids, dose dependent decreases in serum cholesterol and triglyceride and an increased presence of triglyceride containing droplets in enterocytes. Mitratapide also has a slight appetite decreasing effect that is claimed to be associated with its mode of action. Vomiting, diarrhoea or softened stools may occur during treatment. In most cases, these effects are mild and transient.

Giracodazole (also Girodazole or RP 49532A) is a marine compound has been isolated from the sponge Pseudaxinyssa cantharella. It has shown broad antitumor activity in experimental models and has been studied as a potential antitumor compound that inhibits protein synthesis in cell cultures and in cell free systems. Dose-limiting toxic effects that were observed were delayed hypotension and severe asthenia. Independent of dose level, transient nausea and vomiting were reported during infusion. As a result of this toxicity profile, no phase II clinical trial was conducted for Giracodazole.

Alnespirone [S 20499] is a potent and full agonist at pre- and postsynaptic serotonin 1A receptors. Alnespirone is the (+)-enantiomer, S 20244 is the racemate. In animal models, alnespirone demonstrated both anxiolytic and antidepressant activity and was undergoing phase II trials in these indications with Servier in France. However, development of Alnespirone was discontinued for anxiety disorders and major depressive disorder.

Aloracetam [CAS 493] is a nootropic agent with potential in the treatment of Alzheimer's disease. Aloracetam was undergoing clinical evaluation with Hoechst for the treatment of Alzheimer's disease, but this research was discontinued later.

Astra Hässle (now Hässle Läkemedel, a subsidiary of AstraZeneca) of Sweden was developing an IV formulation of almokalant for use in the treatment of atrial arrhythmias. Almokalant is a selective blocker of the delayed outward K+ current. Almokalant exhibited properties of a selective class III antiarrhythmic agent, devoid of β-blocking activity, in vitro and in vivo, in animals and humans. In humans, prolongation of the refractoriness of the atria and ventricles has been demonstrated, as well as a prolongation of the ventricular repolarization. A moderate antiarrhythmic efficacy has been disclosed in studies in patients with supraventricular reciprocating tachycardias, with atrial fibrillation and with premature ventricular contractions. Almokalant also has proarrhythmic potential and thedevelopment of almokalant was discontinued due to induction of Torsade de Pointes, which occurred in some susceptible patients during the clinical trials.

Nacartocin is synthetic oxytocin analogue patented by Ceskoslovenska Akademie as a specific natriuretic agent. The natriuretic effect is mainly due to the inhibitory action of the peptide on tubular sodium resorption. Nacartocin decreased the blood pressure of anesthetized rats by the decrease of the total peripheral resistance which was greater than that observed after oxytocin administration.

Biclodil was investigated as an antihypertensive vasodilator.

Sarcolysin is the isomeric form of melphalan with alkylating activity. Sarcolysin is a bifunctional alkylating agent. The cytotoxicity of sarcolysin appears to be related to the extent of its interstrand cross-linking with DNA, probably by binding at the N7 position of guanine. Like other bifunctional alkylating agents, it is active against both resting and rapidly dividing tumor cells. The levo-isomer - melphalan (L-sarcolysin) is approved under the brand name ALKERAN for the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. In addition, the drug was approved under the trade name Evomela. Evomela is indicated for use as a high-dose conditioning treatment prior to hematopoietic progenitor (stem) cell transplantation in patients with multiple myeloma. In addition, for the palliative treatment of patients with multiple myeloma for whom oral therapy is not appropriate.

Soquinolol [WE 704] is a β-blocker that was under clinical development for the treatment of heart failure, but this research was discontinued. Soquinolol is a highly potent non-subtype-selective beta-adrenergic receptor blocker, which is devoid of any intrinsic sympathomimetic activity. Its local anaesthetic activity (membrane stabilizing effect) is very weak. It also shows good enteral efficacy and long duration of action. In binding studies with heart (Ki beta 1 = 3.25 nmol/l) and lung membranes (Ki beta 2 = 0.85 nmol/l) its binding profile was found to be similar to that of propranolol.