Tilmacoxib [JTE 522] is an orally active, potent and highly selective cyclo-oxygenase-2 (COX-2) inhibitor. It entered phase II clinical trials for the treatment of Familial adenomatous polyposis, rheumatoid arthritis, osteoarthritis, and acute pain in Japan, but was discontinued in 2003.

Mavacoxib (trade name Trocoxil) is a veterinary drug used to treat pain and inflammation in dogs with the degenerative joint disease. Mavacoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Mavacoxib acts by preferential inhibition of COX-2-mediated prostaglandin synthesis. It, therefore, possesses analgesic and anti-inflammatory properties. The products of COX-2 metabolism are also involved in ovulation, implantation, and closure of the ductus arteriosus. Mavacoxib is well absorbed after oral administration; bioavailability was 87% in fed dogs and 46 % in fasted conditions and the recommended dose is based on administration with food. Therapeutic concentrations in fed dogs are reached rapidly and peak concentrations are obtained in less than 24 hours after administering a dose. Mavacoxib is approximately 98% bound to plasma proteins. It is extensively distributed throughout the body and almost all the mavacoxib-related residues in plasma comprise parent drug. The rate of body clearance of mavacoxib is slow and the major route of elimination is by biliary excretion of the parent drug. Adverse reactions of the digestive tract such as vomiting and diarrhea were commonly reported, loss of appetite, hemorrhagic diarrhea, and melaena have been reported in uncommon cases. Gastrointestinal ulceration was reported in rare cases. Apathy, degradation of renal biochemistry parameters and impaired renal function have been reported in uncommon cases. In rare cases, these adverse reactions may be fatal.

Dexibuprofen, S(+)-ibuprofen, is a non-steroidal anti-inflammatory drug and active dextrorotatory enantiomer of ibuprofen. Pharmacotherapeutic effects of dexibuprofen are more potent with lesser side effects than that of the racemic mixture of both isomers. In the acute and chronic treatment of osteoarthritis, it exhibits equivalent efficacy and tolerability as that of celecoxib. Dexibuprofen is a non-selective inhibitor of cyclooxygenase (COX), which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway. Dexibuprofen is a non-selective cyclooxygenase inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of Dexibuprofen including GI ulceration. The major disadvantage of dexibuprofen is its low bioavailability, the account of its low solubility in physiological media.

Guacetisal (Broncaspin) is a bronchomucotropic synthesized by the Bayer Italia S.p.A. Research Laboratories. It is obtained from the esterification of acetylsalicylic acid with guaiacol. Guacetisal was used for the treatment of chronic bronchitis and other inflammatory diseases of the respiratory tract. Guacetisal, used rectally, proved to be a valuable instrument for anti-inflammatory and anti-cough treatment in acute diseases of the airways in infancy.

Alminoprofen is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. It has anti-inflammatory properties different from the classical NSAID. Alminoprofen possesses both antiphospholipase A2 (PLA2) activity and anti-cycloxygenase (COX) activity.

Lornoxicam (Xefo®) is a nonsteroidal anti-inflammatory drug of the oxicam class with analgesic, anti-inflammatory and antipyretic properties. It differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. The inhibition of the cyclooxygenase enzymes (COX-1 and COX-2) by lornoxicam (Xefo®) leads to desensitisation of peripheral nociceptors and consequently inhibition of inflammation. A central effect on nociception which seems to be independent of anti-inflammatory effects has also been suggested.

Nitroxoline (8-hydroxy-5-nitroquinoline) has been used since 1962 in the treatment of urinary tract infections especially those due to gram negative bacilli (E. coli). Nitroxoline is active against most Gram-negative and –positive uropathogenic bacteria, against mycoplasmas (M. hominis, Ureaplasma urealyticum) and human pathogenic Candida spp. The mode of antibacterial and antifungal action is based on the ability of nitroxoline to chelate with various metallic bivalent cations. Nitroxoline is a fluorquinolone that is active against bacterial gyrases. This drug may also have antitumor activity by inhibition of type 2 methionine aminopeptidase (MetAP2) protein which is involved in angiogenesis. Nitroxoline induces apoptosis and inhibits glioma growth in vivo and in vitro. Due to the excellent anticancer activity and its well-known safety profile and pharmacokinetic properties, nitroxoline has been approved to enter into a phase II clinical trial in China for non-muscle invasive bladder cancer treatment

Clonixin is a nonsteroidal agent. It is an anilino-nicotinic acid derivative. It is a drug of anti-inflammatory antipyretic and analgesic activity that produces minor digestive side-effects. At high concentrations, clonixin inhibited PGE2 formed by COX-2 and partly by COX-1 activity. The drug is indicated for the relief of headaches, muscle aches, joint, dental, ear, dysmenorrhea, post-traumatic, post-surgical, gynecological. Adverse effects are occasionally nausea, dizziness, and somnolence, were mild and transient. On rare occasions, and administering high doses, it is possible the appearance of dry mouth or constipation. Concomitant use of anticholinergic drugs to be avoided by the possibility that they enhance their effects atropine.

Flosulide, a selective cyclooxygenase-2 (COX-2) inhibitor, was studied for the treatment for inflammatory diseases. It was shown, that selective inhibition of COX-2 could alter renal function and could be useful in the therapy of esophageal cancer. Experiments on rodent have revealed that therapeutic use of flosulide in proteinuria could be a benefit.

Gamma-oryzanol is a naturally occurring component in rice bran and rice germ, which consists of a mixture of ferulic acid esters of sterols and triterpene alcohols. The mechanism of action of gamma-oryzanol is believed to be involved in the metabolism of catecholamine in the hypothalamus. The antioxidant effect of gamma-oryzanol was well documented and excellent in inhibiting lipid peroxidation. Isolation, extraction, and purification of gamma oryzanol were first reported in the mid-1950s. It has been sold in Japan as a medicine since 1962, first to treat anxiety and later in menopause. Gamma oryzanol and rice bran oil therapy have been used to manage elevated cholesterol and triglyceride levels since the late 1980s. No human clinical studies reported adverse effects of rice bran or its fiber fraction.