Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.

Eprodisate (1,3-propanedisulfonate) is a negatively charged, sulfonated molecule of low molecular weight that has structural similarities to heparin sulfate; it is a glycosaminoglycan mimetic that binds to the glycosaminoglycan (GAG) binding site on serum A amyloid (AA) to prevent its interaction with glycosaminoglycan and arrest amyloidosis, or inhibit amyloid deposition. In nonclinical toxicity studies in two animal species (i.e., rat and dog), eprodisate was administered orally at doses of up to 2000 mg/kg/day for 39 weeks: eprodisate showed low toxicity potential at doses several fold higher than the anticipated clinical dose, was well tolerated upon chronic exposure and was found to be nonmutagenic and nonclastogenic. Furthermore, a series of safety pharmacology studies showed that eprodisate does not have any clinically significant effect on major organ function.

Vestipitant, also known as GW597599, is a neurokinin1 receptor antagonist that was being developed by GlaxoSmithKline for the treatment of postoperative nausea and vomiting. Vestipitant is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It was under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus and insomnia. Vestipitant was shown to improve sleep maintenance in patients with primary insomnia, with no associated next-day cognitive impairment. The effects on wake after sleep onset and total sleep time were maintained following repeated dosing. Vestipitant has anxiolytic properties and a good safety profile. Vestipitant was investigated for potential effect against chronic tinnitus as a stand-alone treatment and in conjunction with a selective serotonin reuptake inhibitor, paroxetine. Although well-tolerated vestipitant, alone or in combination with paroxetine, was not effective in ameliorating tinnitus in this patient group.

Etonitazene is a potent and selective mu-opioid agonist. It was developed in CIBA. Administration of etonitazene may induce respiratory depression, and therefor etonitazene is not used in humans. Etonitazene is explicitly listed as an illegal drug under UN convention and is illegal throughout the world.

Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.

Iotranic Acid is triiodobenzoic acid derivative with potential application as new cholangiographic contrast media for liver imaging

Ioxotrizoic acid is acylated 3,5-diaminopolyhalobenzoic acid derivative patented by Sterling Drug Inc. as X-ray contrast agent for liver and spleen.

Begacestat (GSI-953 or PF-5212362), a gamma-secretase inhibitor (GSI) that selectively inhibits cleavage of APP over Notch, was discovered for the treatment of Alzheimer's disease. The drug has shown promise results in phase I clinical trials, however further studies were discontinued.

Folitixorin, a thymidylate synthase inhibitor is a substrate used by the enzyme methylenetetrahydrofolate reductase (MTHFR) to generate 5-methyltetrahydrofolate. Folitixorin was studied in clinical trials for the treatment of breast cancer, metastatic colorectal cancer and for the treatment of advanced pancreatic cancer. Folitixorin had been granted orphan drug status for the treatment of pancreatic cancer in both the U.S. and EU. However, further development of this drug was discontinued.

Ditiocarb, the sodium salt of diethyldithiocarbamate, is a drug with strong antioxidant capacity and chelating activities. It improves the depressed immune responses of newborn and aged mice and mice that are treated with chemotherapy or irradiation. Ditiocarb prevents cisplatin nephrotoxicity in animals without reducing the drug's antitumor activity. Ditiocarb has therapeutic activity in the LP-BM5 murine retrovirus-induced immunodeficiency disease. In that AIDS model, it reduces lymphadenopathy and hypergammaglobulinemia, restores immunocompetence, and prolongs survival. Ditiocarb was safe and reduced the incidence of opportunistic infections in patients with symptomatic HIV infection but ditiocarb had no positive effect on HIV patients. The administration of ditiocarb did not induce any major adverse clinical or biological reactions. Sixty-four patients with nonmetastatic high-risk breast cancer were randomized in a double-blind trial of adjuvant immunotherapy with sodium ditiocarb (DDC) versus placebo. At 6 years, overall survival was 81% in DDC group versus 55%.