Binedaline is a drug that was investigated as an antidepressant in the 1980s. It`s development for the treatment of major depressive disorder was discontinued. It acts as a selective norepinephrine reuptake inhibitor (Ki = 25 nM), with relatively insignificant influence on the serotonin (Ki = 847 nM) and dopamine (Ki >= 2 µM) transporters.

Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine is an H1 receptor inverse agonist. Bilastine also exerts anti-inflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-α from human mast cells and granulocytes. Common side effects are headache and drowsiness.

Fenclofenac (Flenac) is a non-steroidal anti-inflammatory drug previously used in rheumatism. Fenclofenac was shown to possess anti-inflammatory, antinociceptive and antipyretic properties. Flenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Flenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis. It has mild immunosuppressive effects and may displace thyroid hormone from its binding protein. The antiinflammatory effects of Flenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of Flenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation. Fenclofenac, despite passing animal toxicity tests in 10 animal species (mice, rats, guinea pigs, ferrets, rabbits, cats, dogs, pigs, horses, and monkeys), produced severe liver toxicity in humans. Due to its side effects it was withdrawn from the UK in 1984.

Chromomycin A3 is an anticancer antibiotic, inhibits DNA synthesis by inhibiting DNA gyrase. The antibiotic has potential reactive centers that could interact with GSH, the most abundant non-protein thiol in eukaryotic cells and a putative cofactor involved in the activation of many antibiotics in vivo. It was found, that chromomycin A3 may be potential drug leads for tumor necrosis factor (TNF)-related apoptosis-inducing ligand, TRAIL-resistant and Wnt signal-related diseases and will be useful chemical tools for use in investigating TRAIL and the Wnt signaling pathway.

Prosultiamine (Alinamin®), a well-known thiamine derivative, was first developed by Takeda Pharmaceutical Company in Japan in the 1950s. The drug is a homolog of allithiamine produced by thiol-type vitamin B1 and allicin. Prosultiamine is converted to vitamin B1 after absorption from the gut. The drug thus enables a long-lasting high blood concentration of vitamin B1, resulting in efficient access of vitamin B1 to nervous tissue. Prosultiamine has cured many patients with vitamin B1 deficiency resulting in beriberi neuropathy and Wernicke’s encephalopathy. Prosultiamine is also a potential treatment for HTLV, since it has been shown to reduce viral load and symptoms.

Pranlukast is an antagonist of cysteinyl leukotriene receptor-1 antagonist. It is marketed in Japan by Ono Pharmaceuticals under trademark ONON for the treatment of bronchial asthma and allergic rhinitis as capsules and dry syrup for pediatric use.

Tenatoprazole, also known as TU-199 and STU-Na, is a proton pump inhibitor drug candidate that was undergoing clinical testing. The compound was invented by Mitsubishi Tanabe Pharma and was licensed to Negma Laboratories (part of Wockhardt as of 2007). Mitsubishi reported that tenatoprazole was still in Phase I clinical trials in 2007 and again in 2012. STU-Na will be used for treatment of acid related diseases (gastroduodenal ulcers, erosive or ulcerative esophagitis due to gastroesophageal reflux disease). Tenatoprazole has an imidazopyridine ring in place of the benzimidazole moiety found in other proton pump inhibitors; the binding sites of tenatoprazole were in the TM5/6 region at Cys813 and Cys822 as shown by tryptic and thermolysin digestion of the ATPase labeled by tenatoprazole. It has a half-life about seven times longer than other PPIs.

GW-501516 is a peroxisome proliferator-activator receptor-delta agonist for the potential treatment of dyslipidemia, hyperlipidemia, metabolic diseases and cardiovascular diseases. GW501516 treatment is associated with significant improvements in multiple lipid profile components (TG, LDL-C, HDL-C, free fatty acids and apoB, apoA-I and apoA-II) and a shift in LDL particle size from small dense to larger, less dense particles. Despite these promising early results, the further investigation and development of GW501516 was discontinued after observations in animal studies of its association with the rapid induction of cancers in several organs (liver, stomach, tongue, skin, bladder, ovaries, womb and testes).