Atropine-N-oxide hydrochloride is an alkaloid of the belladonna plants. It is the major metabolite of atropine. It is a competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.

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.

FETOXYLATE, a phenoxyethyl ester of diphenoxylate, is an opioid receptor agonist. It is used as antidiarrheal.

Zabofloxacin (also known as DW-224a), a fluoroquinolone antibiotic agent, is a dual inhibitor of both DNA gyrase and topoisomerase IV of Streptococcus pneumonia. Zabofloxacin successfully has completed phase III clinical trial in patients with acute bacterial exacerbation of the chronic obstructive pulmonary disease. In addition, in May 2012, IASO terminated phase II trial of oral zabofloxacin capsules in patients with moderate-to-severe community-acquired pneumonia due to financial considerations.

Piridoxilate is a conjugation product of pyridoxine and glyoxylic acid in which pyridoxine is supposed to facilitate in vivo transformation of glyoxylic acid to glycine rather than to oxalic acid. The protective action of piridoxilate against hypoxia and metabolic inhibition of the myocardium was confirmed in the experiments on the canine heart-lung preparation using the redox potential of the myocardium and the pyridine nucleotide fluorescence of the heart as indices of cellular energy metabolism. The protective action of piridoxilate against hypoxia which may be attributable to rearrangement of the myocardial metabolism. Piridoxilate did not induce any significant changes in objective and subjective sleep variables. Long-term treatment with piridoxilate may result in overproduction of oxalic acid and in calcium oxalate nephrolithiasis. Piridoxilate should be added to the list of chemicals responsible for chronic oxalate nephropathy.

Peliglitazar (also known as BMS 426707-01), a dual α/γ peroxisome proliferator-activated receptor agonist, has been studied in phase I/II clinical trial in patients with type 2 diabetes mellitus. However, this study was discontinued.

Brequinar is a synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. Brequinar had been in phase II clinical trials by Bristol-Myers Squibb for the treatment of cancer and transplant rejection. However, this research has been discontinued. Brequinar had been also in preclinical studys for the treatment of cytomegalovirus infections. However, this research has been discontinued.

Dersalazine is a locally-acting compound. It is a potent platelet activating factor (PAF)-antagonist. Dersalazine inhibited IL-1beta or TNF-alpha production in THP-1 or U937 cells, respectively. Dersalazine sodium reduced colonic proinflammatory cytokines IL-1b, IL-6, and IL-17 in dextran sodium sulphate (DSS)–induced colitis. After oral administration, dersalazine sodium is mostly unabsorbed until it reaches the large bowel where the azo bond is reduced by bacteria releasing the active compound. Dersalazine had been in phase I clinical trial for the treatment of ulcerative colitis. No serious adverse reactions were detected in clinical trial. However, no recent development has been reported.