U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 81 - 90 of 201 results

Status:
Possibly Marketed Outside US
Source:
Onsior by Novartis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Robenacoxib (trade name Onsior) is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the relief of pain and inflammation in cats and dogs. In an inflammation model in cats, Robenacoxib had analgesic, anti-inflammatory and antipyretic actions with a rapid onset of action (0.5 h). In an in vitro whole blood assay in cats, Robenacoxib demonstrated selective COX-2 inhibition. After oral administration of robenacoxib tablets at 1 mg/kg without food, peak blood concentrations are attained rapidly with a median Tmax of 0.5 h, a mean Cmax of 1159 ng/ml and a mean AUC of 1337 ng*h/ml. Robenacoxib persists longer in the inflammatory exudate of a tissue cage model than in blood. The median Robenacoxib elimination half-life in exudate was about 27 hours versus 2.5 hours for blood. Robenacoxib is extensively metabolized by the liver in cats. The systemic exposure of lactam metabolite is about 25% of Robenacoxib exposure following oral administration to fed cats. Further, the systemic exposure to lactam appears to be two-fold greater in fed cats than fasted cats. Apart from one lactam metabolite, the identity of other metabolites is not known in cats.
Cianidanol is an antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms. One of the polyphenols present in green tea, (+)-catechin (Cianidanol), has been studied for its effects on animal models of hepatitis, as well as in human clinical studies. Pure (+)-catechin (also known as (+)- cyanidanol-3 – trade name Catergen) has been used to treat hepatitis since 1976. This compound has been shown to be an efficient immune stimulator, promoting activation of macrophages, cytotoxic-T-lymphocytes, and natural killer cells in mice. Several clinical studies demonstrate the effectiveness of (+)-catechin in the treatment of viral hepatitis. Pure (+)-catechin has been found to cause hemolysis in some patients, possibly by the promotion of antibody formation against (+)-catechin, which might cross-react with red blood cells. However, there are no reports in the literature of green tea, green tea extracts, or green tea polyphenols causing this side-effect.
Status:
Possibly Marketed Outside US
Source:
PREVICOX by Merck
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Firocoxib is a selective COX-2 inhibitor which was approved by FDA and EMEA for the treatment of osteoarthritis and postoperative pain in dogs (Previcox trade name) and horses (Equioxx trade name). The drug is not for human use.
Glyceryl 1-oleate (1-O-Oleyl-rac-glycerol, Glyceryl oleate, Monoolein), is a surfactant that releases free glycerol and oleic acid upon hydrolysis. Monoolein has been used in liquid crystal studies and research shows that in the presence of monoolein, the penetration of the drug cisplatin (sc-200896) is doubled. Monoolein (1-Oleoyl-rac-glycerol) is used in the development of monoolein-based nanoparticulate liquid dispersions as possible vehicles for drug delivery. Glyceryl oleate is the monoester of glycerin and oleic acid. It's part of the hair lipids and skin lipids and has re-fating properties. Used as emulsifier and nonionic co-surfactant in various skin and hair care products. Creates water-in-oil emulsions (HLB value 3.5) but can also be used as a co-emulsifier and thickener for oil-in-water formulations. Add to oil/emulsifier phase of formulas. Typical use level: 0.5-3%. If used in surfactant systems, typical use level is 0.5-1% which should still keep shampoos clear and transparent.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Etofenamate is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain.
Status:
Possibly Marketed Outside US
Source:
Japan:Alclofenac
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alclofenac (Preservex) is a non-steroidal anti-inflammatory agent advocated for use in rheumatoid arthritis, degenerative joint disease and ankylosing spondylitis. Aceclofenac has little pharmacological activity itself; its main mode of action is through its metabolites which include diclofenac and 4’-hydroxy diclofenac. Skin rash is the most frequent side-effect, which in a small proportion of affected patients may be associated with systemic effects. A cutaneous reaction appears to be more likely in patients with a history of previous allergy to penicillin and other drugs. In June 2013 was told about the new contraindications and warnings for diclofenac. This was after a review by European regulators concluded that the risk of arterial thrombotic events (myocardial infarction; stroke) with diclofenac is greater than with other non-selective NSAIDs and similar to the COX-2 inhibitors.
Status:
Possibly Marketed Outside US
Source:
NCT00419796: Phase 4 Interventional Completed Osteoarthritis With Controlled Hypertension
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lumiracoxib is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug. On August 11, 2007, Australia's Therapeutic Goods Administration (TGA, the Australian equivalent of the FDA) cancelled the registration of lumiracoxib in Australia due to concerns that it may cause liver failure. New Zealand and Canada have also followed suit in recalling the drug. It has never been approved for use in the United States. Lumiracoxib has a different structure from the standard COX-2 inhibitors (e.g. celecoxib). It more closely resembles the structure of diclofenac (one chlorine substituted by fluorine, the phenylacetic acid has another methyl group in meta position), making it a member of the arylalkanoic acid family of NSAIDs. It binds to a different site on the COX-2 receptor than the standard COX-2 inhibitors. It displays extremely high COX-2 selectivity. The mechanism of action of lumiracoxib is due to inhibition of prostaglandin synthesis via inhibition of cyclooygenase-2 (COX-2). Lumiracoxib does not inhibit COX-1 at therapeutic concentrations. Lumiracoxib is used for the acute and chronic treatment of the signs and symptoms of osteoarthritis of the knee in adults.
Status:
Possibly Marketed Outside US
Source:
Unknown by Asahina, Y.|Kashiwaki, K.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs, first isolated by Asahina and Kashiwaki. Among the active components of evodia are quinolone and indoloquinazoline alkaloids, such as evodiamine and rutaecarpine. A significant portion of the analgesic effects of evodia is attributed to these alkaloids. Rutaecarpine has also been shown to have anti-inflammatory action that is related to inhibition of COX-2, as well as other mechanisms. Evodia rutaecarpa ('Wu-Chu-Yu') remains the most popular and multi-purpose herb traditionally used in China for treatment of headache, abdominal pain, postpartum hemorrhage, dysentery and amenorrhea. Rutaecarpine is one of the main active component isolated from 'Wu-Chu-Yu'. Rutaecarpine has been shown to have cardiovascular biological effects such as inotropic and chronotropic, vasorelaxant, anti-platelet aggregation and anti-inflammatory effects. Furthermore, rutaecarpine has the potential for use as an anti-atherosclerosis agent with a novel mechanism. Rutaecarpine prevents hypoxia-reoxygenation-induced myocardial cell apoptosis via inhibition of NADPH oxidases. Also was shown, that rutaecarpine could be effective in preventing the growth of a variety of cancer cells, including downregulating the estrogen receptor of breast cancer.
Status:
Possibly Marketed Outside US
Source:
Afloxan by Fresenius
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Proglumetacin (usually as the maleate salt, trade names Afloxan, Protaxon and Proxil) is a non-steroidal anti-inflammatory drug. Proglumetacin is indicated for the pain and inflammation associated with musculoskeletal and joint disorders. The action of proglumetacin maleate is qualitatively the same as that of indomethacin in vivo; that is, it inhibits cyclo-oxygenase in inflammatory sites.
Status:
Possibly Marketed Outside US
Source:
NCT02229747: Phase 4 Interventional Completed Pharyngitis
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the second line treatment of acute pain and primary dysmenorrhoea. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.