Tolpadol is an analgesic agent. It is a prostaglandin synthesis inhibitor.

Denibulin is a novel antineoplastic agent. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation. Denibulin hydrochloride had been in phase I clinical trials for the treatment of solid tumours. It was generally well tolerated and showed decrease in tumor vascular parameters. However, no recent development has been reported.

Benzotript, a cholecystokinin antagonist is an anti-gastrinic.

Ethylmethylthiambutene is a potent analgesic compatible with morphine. It possesses addiction liability similar to that of morphine.

Nitecapone (3-(3,4-dihydroxy-5-nitrobenzylidine)-2,4- pentanedione, OR-462) is a selective, short-acting catechol-O-methyltransferase (COMT) inhibitor, whose main site of action is in the gastrointestinal tract. Nitecapone displays in vivo activity in peripheral tissues but does not penetrate the blood-brain barrier. The compound increases mechanical and thermal nociception and reduces neuropathic pain in diabetic rats and in a spinal nerve ligation model. Nitecapone has been shown to have a protective effect against ischemia-reperfusion injury in experimental heart transplantation and in Langendorff preparations. Nitecapone added to cardioplegia solution reduces cardiac neutrophil accumulation and transcoronary neutrophil activation during clinical cardiopulmonary bypass. Reflected by better left ventricular stroke volume, nitecapone treatment may be an additional way of reducing the deleterious effects of neutrophil activation during cardiopulmonary bypass. Nitecapone was patented as an antiparkinsonian agent but was never marketed.

Mespiperone C-11 (3-N-[11C] methylspiperone) is a radiolabeled 3-N-methylspiperone. 3-N-methylspiperone is high-affinity D2/3 dopamine and 5-HT2A serotonin receptor antagonist. It has been studied as a positron emission tomography (PET) tracer for imaging D2/3 and 5HT2A receptor densities.

Milveterol (also known as GSK159797) was developed as a longer-acting beta2 adrenoceptor agonist for the treatment of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). Milveterol completed phase II clinical trials for asthmatic subjects. However further development of the drug was discontinued.

Mebiquine is an antidiarrheal and antihelmintic compound.

Elopiprazole [DU 29894 or 1-(7-benzofuranyl)-4-[[5-(4-fluorophenyl)-1-H-pyrrol-2yl]methyl]piperazine) is an antagonist at dopamine D2 and D3 receptors and an agonist at serotonin1A receptors. Elopiprazole development for the treatment of psychotic disorders has been discontinued.