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

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Showing 21 - 30 of 71 results

Status:
Investigational
Source:
INN:cortodoxone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



11-Deoxycortisol (also known as cortodoxone) is the predominant deoxycorticosteroid and is the immediate precursor of cortisol, which is formed by the enzymatic action of 11beta-hydrozylase (P450). Deficiency of this enzyme causes congenital adrenal hyperplasia, which is characterized by hypertension. 11-deoxycortisol is measured as part of the Metyrapone Test. Metyrapone blocks the formation of cortisol, resulting in increased secretion of Adrenocorticotropic hormone (ACTH) and 11-deoxycortisol in normal individuals.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(23)(i) internal analgesic salsalate
Source URL:
First approved in 1995
Source:
Salsalate by Caraco Pharmaceutical Laboratories, Ltd.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Salsalate is a dimer of salicylic acid. Upon administration, it is metabolically hydrolyzed to salicylic acid. Salsalate is is a nonsteroidal anti-inflammatory agent for oral administration for treatment of rheumatoid arthritis, osteoarthritis and related rheumatoid disorders. In addition, salsalate is investigated for treatment of type 2 diabetes.
Status:
US Previously Marketed
First approved in 1987

Class (Stereo):
CHEMICAL (RACEMIC)



Carprofen is an anti-inflammatory drug developed in Japan by Nippon Roche Research Center. Carprofen, as many NSAIDs, selectively inhibits COX-2 and was shown to suppress inflammation in vitro, using osteoarthritis models. The drug was approved by FDA for human use under the name Ridamyl, however, now it is sold only for veterinary purposes and prescribed for the treatment of postoperative pain and the relief of pain and inflammation associated with osteoarthritis in dogs.
Status:
Possibly Marketed Outside US
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Felbinac, an active metabolite of fenbufen, is two times more potent than the parent drug. Felbinac is used topically to alleviate pain in the joints and muscles caused by injury or inflammation (Trixam 3% gel or foam). The drug is believed to exert its action by inhibiting COX-2 protein.
Flunixin meglumine is a potent, non-narcotic, non-steroidal, analgesic agent with anti-inflammatory and anti-pyretic activity was approved to use in horses, cattle and pigs. In horses it is recommended for the alleviation of inflammation and pain associated with musculoskeletal disorders. It is also recommended for the alleviation of visceral pain associated with colic. In the cattle: it is indicated for the control of pyrexia associated with bovine respiratory disease, endotoxemia and acute bovine mastitis. It is also indicated for the control of inflammation in endotoxemia. Flunixin persists in inflammatory tissues and is associated with anti-inflammatory properties which extend well beyond the period associated with detectable plasma drug concentration. Flunixin meglumine is classified as a carboxylic acid. Its mechanism of action is believed to be primarily via the inhibition of cyclooxygenase (COX) enzymes. This inhibition results in decreased formation of cyclooxygenase-derived eicosanoids involved in the pathophysiology of inflammation, such as thromboxanes and prostaglandins.
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.
Azapropazone is a non-steroidal anti-inflammatory drug. It is indicated for use in the treatment of rheumatoid arthritis, osteo-arthritis and gout. Gastro-intestinal disturbances, allergic skin rashes and photosensitivity, headache, vertigo, oedema and kidney impairment may occur. Gastro-intestinal bleeding and angioedema have been reported. Pre-treatment with this drug failed to modify plasma concentrations of phenobarbitone. Brain levels of imipramine or desmethyl imipramine were unaffected 60 minutes after oral administration of imipramine.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Isoxicam is a nonsteroidal anti-inflammatory drug with long half-life. The major oxidative excretion product of isoxicam is the hydroxymethlyisoxazole metabolite, minor metabolites are open-ring sulfonamide and N-methylsaccharin. Isoxicam Is effective and well tolerated in all the major rheumatic diseases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluocortin butyl, a corticosteroid, is available in Germany for nasal application to improve symptoms and signs of perennial rhinitis. This drug is also used in Italy under the brand name Vaspit for the treatment of skin diseases such as dermatitis, eczema, erythema, first-degree burns, and insect bites. Once the cellular environment is reached, the fluocortin butyl induces the expression of protein lipocortin 1, an inhibitor of the enzyme phospholipase A2, an initiator of a cascade of molecular events that leads to the formation of inflammatory mediators such as prostaglandins, and prostacyclins.
Status:
Possibly Marketed Outside US
Source:
NCT01564680: Phase 4 Interventional Completed Postoperative Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



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.