GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.

Pargeverine (also known as a propinox) is an antispasmodic drug that was studied for the treatment of disorders of the gastrointestinal tract, the uterus, and the gallbladder. Pargeverine showed a dual mechanism of action, it binds to muscarinic and calcium receptors that can be related to its antispasmodic activity. The clinical trial has shown that pargeverine was an effective drug in the treatment of moderate to severe colic pain of biliary origin. In addition, its efficacy and tolerability were determined in patients with moderate-to-severe acute intestinal colic pain. As a result, no differences in blood pressure or heart rate were found among treatments. The incidence of mouth dryness was significantly more frequent with the 20 mg and 30 mg doses of propinox than with the placebo or the 10 mg dose. Information about the current development of this drug is not available.

Quinacillin is semisynthetic penicillase-resistant penicillin patented by Boots Pure Drug Co. Ltd. For the treatment of bacterial infection. Quinacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. In clinical trials Staph. aureus was eradicated from all but two patients during treatment but recurred in 4 after withdrawal. The antibiotic was especially useful in the treatment of staphylococcal respiratory infections, as it has little effect on the normal bacterial flora of the chest.

Pentiapine is a dopamine release inhibitor. It is a tranquiliser. Pentiapine produces a dose-dependent decrease in spontaneous motor activity and blocks the morphineinduced hyperactivity. Moreover, this drug in itself has no effect on place conditioning but blocks the acquisition of morphine-induced conditioned place preference.

Lubazodone (YM 992) or (S)-2-[[(7-fluoro-4-indanyl)oxy]methyl]morpholine monohydrochloride, exhibited the biochemical profile of a selective serotonin (5-HT) reuptake inhibitor (SSRI) with 5-HT2A receptor antagonistic activity. It has been studied in the treatment of depression.

Denagliptin is a dipeptidyl peptidase IV (DPP-IV) and and tripeptidyl-peptidase inhibitor, which entered phase III clinical trials in 2006 for the treatment of type 2 diabetes mellitus at GlaxoSmithKline. Development of this compound was put on hold due to unfavorable preliminary data from preclinical long-term toxicity trials. Stress testing or forced degradation studies of denagliptin revealed that drug was stable in the solid-state, but degraded in solution, in blends with all excipients, and in capsules predominantly by cyclization to (3S,7S,8aS) amidine, which epimerized to (3S,7S,8aR) amidine.

Diclofurime is a powerful coronary vasodilator, which lowers the resistance of large coronary arteries and decreases the O2 consumption of the myocardium. The activity of diclofurime is similar to digitalis: increase of cardiac flow, bradycardia, redistribution of the blood to peripheral area. These properties demonstrated in dogs have been confirmed in patients with cardiac diseases. Diclofurime is the antianginal agent. It might be effective in the control of cardiac arrhythmias since it exhibited both local anesthetic-like and calcium antagonistic properties. Diclofurime appears to be one of the most active and best tolerated drugs for long-term oral treatment of arterial hypertension.

Dazoxiben is a selective inhibitor of thromboxane synthetase (IC50 3 nM), an enzyme that converts the endo-peroxide PGH2 into thromboxane A2, which is a potent vasoconstrictor and platelet aggregating agent. Dazoxiben has demonstrated efficacy in some clinical trial for the treatment of Raynaud's syndrome, an ischaemic condition manifested by the pallor of affected digits. In subsequent studies, however, no significant effect of dazoxiben was found. Dazoxiben was also evaluated in patients with sepsis, adult respiratory distress syndrome, stable angina, and other conditions.

Propipocaine (also known as falicaine) is an aromatic ketone derivative with potent local anaesthetic activity. The toxicity of Propipocaine has been worked out in mice. Given intravenously it is 4 times, and subcutaneously 10 times as toxic as procaine. Falicaine is suitable for surface anaesthesia in a concentration of 0.5 to 1 %. Higher concentrations cause irritation or even necrosis.

Propetamide (also known as FC 379) is a propionamide derivative patented by All-Union Scientific Research Chemical-Pharmaceutical Institute as an analgesic compound. In mice, Propetamide produced both a depression of spontaneous motility and relaxation of muscular tone. However, Propetamide was less active than meprobamate. Propetamide at 400 mg/kg reduced muscular relaxation in 70% of the animals, while the same effect was obtained in 100% of the animals with meprobamate at 200 mg/kg.