Teloxantrone (also known as DuP 937) was developed as an anthrapyrazole intercalator that inhibits DNA synthesis. Teloxantrone interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis. The drug participated in phase II clinical trials in colorectal carcinoma, in non-small cell lung cancer, in metastatic malignant melanoma. However, these studied apparently were discontinued.

Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.

Wilex developed WX-UK1 as a specific inhibitor of human trypsin-2, human trypsin-3 and urokinase-plasminogen activator. WX-UK1 participated in phase I clinical trial in combination with capecitabine in advanced malignancies to determine the safety, tolerability, maximum tolerated dose, pharmacokinetics, and pharmacodynamics. However, in April 2014, the clinical development of this drug was discontinued, as part of a company restructure.

Bentiamine (also known as dibenzoyl thiamine), a derivative of thiamine, is rapidly absorbed and converted to thiamine. Experiments on rodent have shown that this compound had low toxicity and absence of carcinogenicity.

Hydroxyprocaine was invented as a local anesthetic drug that possessed the antibacterial properties. Information about the current use of this drug is not available.

Midamaline was used as a local anesthetic. Information about the current use of this compound is not available.

Piprocurarium is a curarimimetic. It is antagonized by neostigmine. Piprocurarium is strongly vagolytic, producing tachicardia. Its duration of action is shorter than that of d-tubocurare and longer than that of succinylcholine. Piprocurarium is not hypotensive, is only slightly histaminogenic, is nonirritating to the veins, and can be mixed with all the anesthetic drugs. Piprocurarium has been offered for clinical trial as a brief-acting, nondepolarizing neuromuscular blocking drug. The drug appears to be anything but short acting. A persistent tachycardia and elevation in systolic and diastolic pressure invariably follows its intravenous injection. Alarming electrocardiographic changes occur, characterized by AV dissociation, depression of the ST segment, supraventricular tachycardia and, at times, inversion of the T waves. In view of these circulatory effects, it is doubtful that the drug will be useful clinically.

Dexpemedolac is long-acting non-narcotic analgesic. Dexpemedolac exhibited potent analgesic effects against chemically induced pain in rats and mice and against inflammatory pain in rats. Dexpemedolac differed from standard nonsteroidal anti-inflammatory drugs (NSAIDs) in that the doses, which produced analgesia were much lower than those required for either anti-inflammatory or gastric irritant effects. The common to the NCAIDs class actions are antipyresis and inhibitory effects on platelet aggregation. In yeast-induced hyperthermic rats, dexpemedolac exhibited antipyretic actions, whereas the drug did not affect body temperature in normothermic animals. Aggregation of human platelets was inhibited by high concentrations of dexpemedolac.

Sibrafiban (G-7453) is the orally administered, nonpeptide, double-prodrug of Ro 44-3888 which is a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban is a double prodrug that undergoes bioconversion to the inactive prodrug Ro 48-3656 and to the active IIb/IIIa antagonist, Ro 44-3888, after oral administration. Sibrafiban was undergoing clinical trials for secondary prevention of cardiac events in patients stabilised after acute coronary syndromes. Sibrafiban has been shown to have comparable efficacy to aspirin in preventing recurrent ischemic events in patients suffering from acute coronary syndromes. Sibrafiban was under development by Genentech and Hoffmann-La Roche, and in phase III trials as an antithrombotic. The development of sibrafiban was discontinued in 1999 following unfavorable Phase III efficacy data.