Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.

Moxadolen is tricyclo-[5.2.1.0.2.6endo]decenone derivative. Moxadolen pharmacokinetics were investigated after oral application in male Wistar rats. The compound is extensively absorbed and mainly renally eliminated. Within 60 h, 63% of the activity is recovered in urine and feces. After 12 h 27% of the activity is eliminated (application in polyethylene glycol). The highest total concentration of the activity in the plasma is found after 2 h, the highest of the unchanged drug is found after 1 h. The half-life is 2.9 h.

Miroprofen, an imidazopyridine derivative, possesses anti-inflammatory properties. It was shown that this compound could be effective in suppressing pain responses and acute inflammation accompanied by increased vascular permeability. Analgesic effect of this compound was studied in post-extraction pain. However, information about the current study of this agent is not available.

Micinicate, a vasodilator was developed as a spasmolytic agent. Information about the current use of this compound is not available.

Brecanavir (previously known as VX-385), a HIV aspartyl protease inhibitor was developed for the treatment of HIV. The inhibition of HIV viral proteinase enzyme prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Brecanavir reached Phase II development. However, GlaxoSmithKline announced to discontinue development brecanavir. Because of the inability to develop a viable oral dosage formulation capable of delivering the desired brecanavir levels in patients with multi-drug resistant HIV.

Naxaprostene (CG 4305) is a prostacyclin analogue, which causes concentration dependent inhibition of thrombocyte function. Naxaprostene is more selective for IP receptors and tends towards partial agonism. Naxaprostene prevented thrombotic arterial occlusion in rabbits.

Deprostil is prostaglandin E analog. The drug exhibits a prolonged inhibition of basal gastric acid secretion. Deprostil is the orally active anti-ulcer agent. It is a racemate with four possible optical isomers. Like deprostil the (nat)- and (epi)-isomers appear to be potentially useful therapeutic agents for the treatment of hypergastrlc acid secretion and peptic ulcers.

Dicirenone is an aldosterone antagonist. It is used as a hypotensive agent. Dicirenone inhibited the effects of aldosterone on urinary K(+):Na(+) ratios and the binding of [(3)H]aldosterone to renal cytoplasmic and nuclear receptors. Dicirenone blocked the action of aldosterone on Na-K ATPase. Cytoplasmic binding of [(3)H]aldosterone and dicirenone was similar in magnitude and involved the same set of sites. It had no effect on adrenal steroidogenesis.

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.