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

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Showing 11 - 20 of 89 results

Status:
Investigational
Source:
INN:fanetizole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fanetizole is a derivative of 2-aminothiazole. It is an anti-inflammatory agent. This drug is reported to have some cyclooxygenase inhibiting activity. Production of superoxide in response to the chemotactic factor formyl-methionyl-leucyl-phenylalanine (f-Met-Leu-Phe) was markedly inhibited by fanetizole. Suppression of neutrophil production of toxic oxygen metabolites may partially explain the antiarthritic effect of fanetizole. Fanetizole was shown to restore depressed E-rosetting activity in adult thymectomized mice, as well as enhance in in vitro proliferation of murine thymic cells to mitogen and synergistically acted with the monokine interleukin-1. It displays anti-arthritic activity in viva in the rat adjuvant arthritis model, inhibiting the development of disease in the non-infected foot. This drug has less side effects than levamisole in animals.
Status:
Investigational
Source:
INN:nicotredole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nicotredole (Tryptamide), similarly to ibuprofen and piroxicam, shows anti-inflammatory and analgesic properties. Tryptamide reversed pyrogen-induced hyperthermia in rats, elicited analgesic effects in rats, but not in mice, prolonged the time of hexobarbital sleep in rats and inhibited locomotor activity in rats and mice. Tryptamide has not elicited side effects on the circulatory system of rats and cats.
Licofelone (ML 3000) is a pyrrolizine derivative originally discovered by Merckle GmbH and developed by EuroAllaince with a unique pharmacological profile, which comprises optimal gastrointestinal tolerability and high analgesic and anti-inflammatory activity. These effects are due to balanced and selective inhibition of both cyclo-oxygenase and 5-lipoxygenase. Inhibition of 5-lipoxygenase may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs, which only inhibit cyclooxygenase. Licofelone also has antipyretic and antiaggregatory properties. Clinical and preclinical trials were also undertaken for osteoarthritis, rheumatoid arthritis, asthma, pain and inflammation. However, development for these indications appear to have been discontinued.
Phillyrin, an active ingredient found in many medicinal plants and certain functional foods, elicits anti-obesity and anti-inflammatory properties in vivo. Phillyrin is one of the main chemical constituents of Forsythia suspensa (Thunb.), which has shown to be an important traditional Chinese medicine. Phillyrin, has being shown to possess various bioactivities, including anti-inflammatory, anti-oxidant, and antiviral activities. It has being reported that Phillyrin attenuates high glucose-induced lipid accumulation in human HepG2 hepatocytes through the activation of LKB1/AMP-activated protein kinase-dependent signalling.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



2-Carboxy-2-Phenylethyl 1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1h-Indole-3-Acetate (Tropesin, VUFB-12018) is indometacin prodrug with potent anti-inflammatory efficacy and advantageous therapeutic properties. In experiments in vivo in rats, after oral administration of a Tropesin dose of 50 mg/kg, esterolysis was observed between 2-3, with a peak level of liberated indometacin between 10-13 h after ingestion. Tropesin was administered orally to rats and dogs in the daily therapeutic dose, triple the dose and ten times the dose for 3 months. After the highest dosage, in isolated cases, some dogs were found to have superficial erosions of the gastric mucosa and dystrophic lesions of renal tubules without biochemical correlations. Indometacin, administered in parallel doses, caused severe lesions of the gastrointestinal tract with melaena and subsequent anemia, as well as severe degenerative changes in renal tubules, in all dosage groups. From the toxicological aspect, Tropesin is substantially more acceptable than indomethacin. The anti-inflammatory and anti-arthritic activities of Tropesin in comparison with indomethacin, were studied in various models of both acute and chronic inflammatory reactions. Both compounds exhibited significant therapeutic activities without substantial quantitative differences.
1-Phenyl-3-pyrazolidinone (phenidone) is a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX). Phenidone inhibits both the LO (lipoxygenase) and Cox (cyclooxygenase) pathways, the synthesis of Fos-related antigen protein, and is described as an anti-inflammatory and anti-oxidant compound. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone was also the best in suppressing LPS induced neurotoxicity, where the more potent neuroprotection by phenidone may be attributable to the synergistic effects of dual COX and LOX inhibition. Therefore, dual inhibitors of COX and LOX, such as phenidone, represent valuable candidates for the development of novel drugs for inflammation-related neurodegenerative disorders including PD.
Status:
US Previously Marketed
Source:
Zomax by McNeil
(1980)
Source URL:
First approved in 1980
Source:
Zomax by McNeil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Zomepirac Sodium (Zomax) is a pyrrole-acetic acid structurally related to tolmetin sodium. Zomepirac is a prostaglandin synthetase inhibitor and is not an opioid, an opioid antagonist, or a salicylate. Zomepirac was approved by the Food and Drug Administration for marketing in the United States as an analgesic. It was indicated for all forms of mild to moderately severe pain, and was being promoted as a "comprehensive, non-addicting analgesic." Later Zomepirac was found to be associated with fatal and near-fatal anaphylactoid reactions. The manufacturer voluntarily removed Zomax tablets from the Canadian, US, and UK markets in March 1983.
Status:
US Previously Marketed
First approved in 1960

Class (Stereo):
CHEMICAL (RACEMIC)



Oxyphenbutazone is a non-steroidal anti-inflammatory drug, cyclooxygenase (prostaglandin synthetase) inhibitors which was marked under brand name tandearil for the treatment rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis. But this drug was withdrawn from markets due to bone marrow suppression.
Status:
US Previously Marketed
First approved in 1952

Class (Stereo):
CHEMICAL (ACHIRAL)



Phenylbutazone is an anti-inflammatory drug, which binds to and inactivates cyclooxygenases and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues. Phenylbutazone was marked under the brand name butazolidin for the treatment rheumatoid arthritis and gout, but then this usage was discontinued. In addition, phenylbutazone is used in UK for the treatment of ankylosing spondylitis, but only in those cases, when other therapies are unsuitable.
Status:
US Previously Marketed
Source:
ALLONAL AMINOPHENAZONE by ROCHE
(1961)
Source URL:
First marketed in 1897
Source:
Pyramidon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aminophenazone is a phenyl-pyrazolone derivative with potent analgesic and antipyretic properties. Aminophenazone has been used as salt or complexes, including topically as the salicylate. It was recommended for the treatment of a fever, neuralgia, myositis, acute rheumatism, arthritis, chorea. In 1999 the FDA suspended aminophenazone. The drug caused agranulocytosis. Some of the cases of agranulocytosis were fatal. Another reason for suspending this drug from the market was its ability to react with nitrite-containing food, thus forming carcinogenic nitrosamines. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests.

Showing 11 - 20 of 89 results