Entinostat (MS-275) is an orally active, highly selective, small-molecule histone deacetylase inhibitor (HDACi) derived from benzamide. Entinostat preferentially inhibited HDAC1 versus HDAC3 and had no inhibitory activity toward HDAC8. The time to maximum plasma concentration (tmax) of entinostat ranged from 0.5 to 60h (median of 2h). Elimination of the drug was bi-exponential, with a terminal half-life of 30-80h. Entinostat is a well-tolerated that demonstrates promising therapeutic potential in both solid and hematologic malignancies. Its efficacy does not appear directly dose-related, and as such, more relevant biomarkers are needed to adequately assess its activity.

Ditekiren is a relatively large renin inhibitor incorporating the hydroxyethylene isostere as well as both the P4 proline and P2’ isoleucine of angiotensinogen. Methylation of the P2-site histidine backbone nitrogen stabilizes the P2-P3 peptide bond towards degradation by chymotrypsin. Even though oral bioavailability was low, serum ditekiren levels were equivalent to 4–8 times the in vitro IC50 for renin inhibition for this peptide throughout the 2.5 h after oral administration that blood levels were monitored. In Na-depleted cynomolgus monkeys, oral dose elicited a hypotensive response that had not returned to baseline by 5 h. Ditekiren had been in phase II clinical trials for the treatment of heart failure and hypertension. However, these studies were discontinued.

Amifloxacin [WIN 49375] is a fluoroquinolone antibacterial with a broad range of activity against aerobic Gram-negative and some aerobic Gram-positive organisms. Amifloxacin is a DNA gyrase inhibitor. The 50% inhibiory concentration for supercoiling activity of E.coli KL16 DNA gyrase of amifloxacin (MIC, 0.10 ug/ml) was 2.47 ug/ml. Amifloxacin was in trials for the treatment of gram-negative infections, septic shock and urinary tract infections. However, development of amifloxacin has been discontinued.

Loxiglumide is a potent, orally active, and selective CCK-A receptor antagonist which stimulates calorie intake and hunger feelings in humans. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying. Intravenous administration of loxiglumide antagonized the CCK-induced reduction of gastric emptying in rats, acceleration of intestinal transport in mice, increase in ileal motility in rabbits, gallbladder contraction in guinea pigs and acceleration of gallbladder emptying in mice.

OSI-7904L is a liposomal formulation of the highly specific, noncompetitive thymidylate synthase inhibitor OSI-7904 (also known as GW1843, BW1843U89, and GS7904). The liposome formulation was developed to enhance the therapeutic index and dose schedule convenience of this potent antifolate compound. This drug was studied in phase II clinical trial in patients to treat head and neck cancer, gastroesophageal adenocarcinoma and advanced biliary cancer, but these studies were discontinued. As an example in case of OSI-7904L, was revealed that its activity was below a level of clinical relevance in advanced biliary tract cancer, providing only a small degree of disease stabilization.

Tampramine (also known as AHR-9377) is a potent and selective, noncompetitive inhibitor of norepinephrine reuptake possesses antidepressant activity. This drug was studied for the treatment of the major depressive disorder; however, this study was discontinued.

Tametraline (also known as CP-24,441) is a norepinephrine-dopamine reuptake inhibitor that was developed as an Antidepressant agent. Information about the current use of this drug is not available.

Octriptyline was used as an antidepressant, however, it has never been marketed.

Xanthocillin is an antibiotic derived from Penicillium notatum. In vitro tests have shown that most of the common Gram-positive and Gram-negative pathogens, including Proteus and Pseudomonas pyocyanea, are sensitive to xanthocillin. Xanthocillin participated in the trial in patients with a variety of eczematous and intertriginous eruptions, in all of which bacterial infection was thought to be playing a part. Xanthocillin cream produced results, which were on par with other treatments. Information about the current use of this agent is not available.