Glysobuzole (stabinol) is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glysobuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.

Amelubant, its metabolite BIIL 260 (formed by removal of the ethoxycarbonyl protecting group), and its major metabolite BIIL 315 (formed by removal of the protecting group and glucuronidation) had potent in vitro and in vivo Leukotriene B4 receptor antagonistic properties. Amelubant has been in phase II clinical trials by Boehringer Ingelheim for the treatment of cystic fibrosis, chronic obstructive pulmonay disease, bronchial asthma and rheumatoid arthritis. However, this research has been discontinued. In 2002, orphan drug designation was received in E.U. for the treatment of cystic fibrosis. Serious adverse events of Amelubant were characterized by increased presentation of respiratory signs and/or symptoms associated with pulmonary exacerbation and resulted in admission to a hospital and/or administration of IV antibiotics.

Dexsotalol is an isomer of antiarrhythmic drug d,l-sotalol, but in opposite to drug, it increases the incidence of arrhythmias

Ameltolide (ADD 75073, LY 201116) is a 4-aminobenzamide anticonvulsant patented by Research Corporation Technologies in the USA. Ameltolide is a sodium channel antagonist, it represents a potential therapy for the treatment of epilepsy. Ameltolide had been in phase I clinical trials by Research Corporation Technologies for the treatment of epilepsy. However, this research has been discontinued.

Diclofensine is an antidepressant with equipotent inhibitive effects on the neuronal uptake of norepinephrine (NE), serotonin, and dopamine. It is devoid of monoamine-releasing or monoaminoxidase-inhibiting properties. Diclofensine was found to be an effective antidepressant in human trials, with relatively few side effects, but was ultimately dropped from clinical development.

Lotrafiban (SmithKline Beecham) is a member of the latest generation of orally-active platelet GPIIb/IIIa blockers undergoing Phase III clinical trials to test the relative effectiveness versus other oral platelet inhibitors for ischaemic conditions including unstable angina, restenosis after PCI and stroke. Lotrafiban is converted from an esterified prodrug by plasma and liver esterases to a peptidomimetic of the arginine-glycine-aspartic acid amino acid sequence. This sequence itself mimics the binding site of fibrinogen and von Willebrand Factor to the platelet GPIIb/IIIa receptor. Preliminary results of the clinical trial APLAUD (antiplatelet useful dose) show that lotrafiban is clinically safe and well-tolerated in patients with recent myocardial infarction, unstable angina, transient ischaemic attack (TIA), or stroke when added to aspirin therapy. The Blockade of the IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) trial of SmithKline Beecham's oral GpIIb/IIIa blocker, lotrafiban, has been stopped early because of concerns about both safety and efficacy. The drug was showing a higher mortality rate than placebo, and was also associated with an increased incidence of serious thrombocytopenia and major bleeding. As a result of these findings the company has discontinued development of lotrafiban.

Isamoltan (CGP 361A) is a β-adrenoceptor and serotonin 1B receptor antagonist. Isamoltane has reported activity as an anxiolytic in man. Isamoltan had been in phase III clinical trials for the treatment of anxiety. However, this research has been discontinued.

RU 28318 also known as OXPRENOATE is a mineralocorticoid receptor (MR) antagonist, inhibiting aldosterone production and secretion. RU 28318 has been studied in normal and diabetic rats. It was revealed, that in combination with angiotensin converting enzyme inhibitors, RU 28318 was the most effective at improving -dP/dt (a measure of diastolic function) and attenuated cardiac dysfunction in diabetes.

Etifenin is a diagnostic radiopharmaceutical for the liver function assessment. It is used for hepatobiliary function scintigraphy where there is the following suspicion: Acute cholecystitis; Chronic gall duct changes; Occlusion of ductus choledochus; Congenital aberrances of the gall duct system such as atresia; Provision of evidence of bile leak; For differential diagnosis of intrahepatic growth (suspicion of focal nodular hyperplasia versus suspicion of liver cell cancer). The diagnostic significance in liver cancer is rather marginal compared to other imaging procedures. No information on adverse reactions after intravenous injection of the ready-to-use solution is available.

Methylbenactyzium bromide has been used as a spasmolytic for the treatment of gastrointestinal ulcer and gastrointestinal spasms.