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Status:
Possibly Marketed Outside US
Source:
M016
(2012)
Source URL:
First approved in 2007
Source:
M005
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Hydroxytyrosol is an important phenolic compound obtained from olive oil. Hydroxytyrosol possesses anti-inflammatory properties and has the capacity to inhibit cyclooxygenase and lipoxygenase enzymes. Hydroxytyrosol is a powerful antioxidant due to its protective function in cells. Hydroxytyrosol protects the cardiovascular system, avoiding oxidation of LDL cholesterol, maintaining normal blood HDL cholesterol concentrations and thus preventing atherosclerosis. Hydroxytyrosol protects brain cells from lipid peroxidation because it easy penetrates through the blood-brain barrier. Thus, the compound can be used in the disease treatment of Alzheimer or Parkinson. In addition, the compound also helps to prevent osteoporosis because its consumption has positive effects on the formation and growth of bones. Hydroxytyrosol is under investigation phase II clinical trials for breast cancer women to evaluate its effect on mammographic density. The recently published article has shown hydroxytyrosol could prevent obesity and insulin resistance by altering the composition of the intestinal microbiota and improving the integrity of the intestinal wall.
Status:
Possibly Marketed Outside US
Source:
21 CFR 333D
(2012)
Source URL:
First approved in 2000
Source:
21 CFR 352
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Sodium dehydroacetate, a water-soluble antiseptic, is a food and feed additive with antimicrobial effects. Recently published studies have shown that sodium dehydroacetate in patients with leg ulcers could cause allergic contact dermatitis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Tenidap ([Z]-5-chloro-2,3-dihydro-3-[hydroxy-2-thienylmethylene]-2-oxo-1H-indole-1-carboxamide) is an oxindole derivative, a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis. Tenidap shows potent inhibition of cyclooxygenase in vitro, that is of several magnitudes greater than 5-lipoxygenase inhibition. Lipoxygenase inhibition, however, has been difficult to document in vivo because Tenidap is highly protein bound and free drug concentrations are below those necessary for 5-lipoxygenase inhibition. However, several in-vitro activities distinguish Tenidap from conventional cyclooxygenase inhibitors. As shown with stimulated human neutrophils, tenidap inhibits activation of collagenase, lysosomal enzyme secretion, and superoxide generation, as well as aggregation and adhesion to endothelium. Furthermore, unlike Non-steroidal anti-inflammatory drugs (NSAIDs), it lowers circulating C-reactive protein (CRP) concentrations by a magnitude equivalent to hydroxychloroquine and auranofin. This result suggests an effect on the synthesis and/or release of the cytokines known to induce the acute-phase protein response-namely, IL-1, IL-6, and TNF-alpha. Tenidap, like existing second-line drugs, lowers serum IL-6 concentrations, a property not shared by NSAIDs The cytokine inhibitory effect also includes reduced in-vitro concentrations of TNF-alpha and IL-1 from both RA synovium and peripheral blood mononuclear cells. There is no immunosuppressive effect of Tenidap in either animal or clinical studies. In clinical studies. The comparisons between tenidap and other second-line agents show that Tenidap produced a faster reduction in CRP than Auranofin. The rate of withdrawal because of inefficacy was similar (18-20%) in Auranofin and Tenidap groups. The quality of life using the arthritis impact measurement scales has also been assessed Scores were better with tenidap than with NSAID monotherapy, but equivalent to the second line plus NSAID combinations. Tenidap is registered in the United States, Netherlands, and Italy but is not marketed because marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.
Status:
Possibly Marketed Outside US
Source:
Abbott-85761 by Abbott
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Atreleuton is a potent, orally administered, selective 5-Lipoxygenase inhibitor. Atreleuton had been in phase III clinical trials for the treatment of asthma and phase II clinical trials for the treatment of acute coronary syndrome and atherosclerosis. However, this research has been discontinued.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Acetyl-11-keto-beta-boswellic acid (AKBA), a pentacyclic triterpene, is a component of gum resin of Boswellia serrata. It inhibits 5-lipoxygenase in a selective, enzyme directed, non-redox, and noncompetitive manner. In addition, AKBA inhibited topoisomerase I. It induces apoptosis and exerts antineoplastic properties. 5-LOXIN, a dietary supplement ingredient (Boswellia serrata extract enriched with 30% 3-O-acetyl-11-keto-beta-boswellic acid) is effective in reducing pain and improving physical functioning in osteoarthritis patients.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Malotilate (NKK-105) is a drug used in the treatment of liver disease. Malotilate selectively inhibits the 5-lipoxygenase. Malotilate prevented increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver.
Status:
Possibly Marketed Outside US
Source:
Ibudros by Manetti-Roberts [Italy]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Ibuproxam is a prodrug which metabolizes into ibuprofen and is therefore indicated for the treatment of pain and inflammation. Administration of oral ibuproxam resulted in a significantly higher plasma concentration than administration of an equal dose of ibuprofen after 45 minutes. Despite showing some promise as a NSAID ibuproxam does not appear to have been approved or marketed.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. Marketed under the brand name Zubrin, Tepoxalin is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. Tepoxalin has an unique property as an NSAIDs that suppresses both cyclooxygenase and lipoxygenase.
Status:
US Approved Rx
(2019)
Source:
ANDA211858
(2019)
Source URL:
First approved in 1987
Source:
NDA019618
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Mesalamine, also known as Mesalazine or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects. As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism. Although the mechanism of action of mesalazine is not fully understood, it appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon. Mesalazine is used for the treatment of active ulcerative proctitis.
Status:
US Approved Rx
(2019)
Source:
ANDA211858
(2019)
Source URL:
First approved in 1987
Source:
NDA019618
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Mesalamine, also known as Mesalazine or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects. As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism. Although the mechanism of action of mesalazine is not fully understood, it appears to be topical rather than systemic. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with chronic inflammatory bowel disease, and it is possible that mesalazine diminishes inflammation by blocking cyclooxygenase and inhibiting prostaglandin production in the colon. Mesalazine is used for the treatment of active ulcerative proctitis.