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

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Showing 21 - 30 of 32 results

Clofibrate is a fibric acid derivative used to lower cholesterol and triglyceride (fat-like substances) levels in the blood. This may help prevent medical problems caused by such substances clogging the blood vessels. However, this treatment was discontinued in 2002 due to adverse effects. Clofibrate is an agonist of the PPAR-α receptor in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, and increased lipoprotein lipase activity. Clofibrate increased the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis, inhibited the synthesis, and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. In addition, clofibrate was investigated as a novel therapy agent in multiple myeloma and it shown the promising results.
Status:
US Previously Marketed
Source:
HYDROXYSTILBAMIDINE ISETHIONATE by SANOFI AVENTIS US
(1953)
Source URL:
First approved in 1953
Source:
HYDROXYSTILBAMIDINE ISETHIONATE by SANOFI AVENTIS US
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Hydroxystilbamidine is an organic antimonal derivative with antiprotazoal, antifungal and anticancer activity. It was used in the treatment of blastomicosis and leishmaniasis. Moreover, hydroxystilbamidine (FluoroGold) is used as a tracer for neurons.
Zinc Pidolate (Zinc PCA) is a topical skin product with purifying, astingent, anti-inflammatory, antiseptic activity. It has long been used as a cosmetic ingredient, because of its astringent and anti-microbial properties. Zinc Pidolate has also being shown to be effective against halitosis. Zinc PCA prevents the UV-induced MMP-1 production in vitro by suppressing the activation of AP-1. Zinc PCA was also able to enhance type I collagen synthesis in NHDFs, by increasing the expression of the mRNA encoding the ascorbic acid transporter SVCT2 in non-UV irradiated NHDFs, which suggests its promising effect against not only photoaged skin but also for the simple atrophic change of intrinsic skin ageing. Zinc PCA is able to suppress sebum secretion by inhibiting 5-α reductase in hyperseborrhea, to suppress body odor by forming zinc salts with short-chain fatty acids, to suppress wrinkles by inhibiting AP-1 to and inhibit bacterial growth including acne related Propionibacterium acnes.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Pyridofylline was studied in dyspnea, hyperlipemia, and certain hepatobiliary diseases.
Status:
Possibly Marketed Outside US
Source:
NCT02161653: Phase 4 Interventional Completed Severe Alcoholic Hepatitis
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Metadoxine is an ion pair salt of pyridoxine and pyrrolidon carboxilate (PCA). Metadoxine is predominantly used in developing nations for acute alcohol intoxication. The positive effect of metadoxine on ethanol metabolism can be explained by the maintenance of normal levels of alcohol dehydrogenase during chronic ethanol intake. Metadoxine was investigated against ADHD, but FDA put hold on phase III clinical trials. Metadoxine is also investigated as a treatment for fragile X synsdome.
structurally diverse
Status:
US Approved Allergenic Extract (1972)

Class:
STRUCTURALLY DIVERSE

Pyridoxine is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Vitamin B6 (pyridoxine) is a water-soluble vitamin used in the prophylaxis and treatment of vitamin B6 deficiency and peripheral neuropathy in those receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been found to lower systolic and diastolic blood pressure in a small group of subjects with essential hypertension. Hypertension is another risk factor for atherosclerosis and coronary heart disease. Another study showed pyridoxine hydrochloride to inhibit ADP- or epinephrine-induced platelet aggregation and to lower total cholesterol levels and increase HDL-cholesterol levels, again in a small group of subjects. Vitamin B6, in the form of pyridoxal 5'-phosphate, was found to protect vascular endothelial cells in culture from injury by activated platelets. Endothelial injury and dysfunction are critical initiating events in the pathogenesis of atherosclerosis. Human studies have demonstrated that vitamin B6 deficiency affects cellular and humoral responses of the immune system. Vitamin B6 deficiency results in altered lymphocyte differentiation and maturation, reduced delayed-type hypersensitivity (DTH) responses, impaired antibody production, decreased lymphocyte proliferation and decreased interleukin (IL)-2 production, among other immunologic activities. Used for the treatment of vitamin B6 deficiency and for the prophylaxis of isoniazid-induced peripheral neuropathy.
Pyridoxine is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Vitamin B6 (pyridoxine) is a water-soluble vitamin used in the prophylaxis and treatment of vitamin B6 deficiency and peripheral neuropathy in those receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been found to lower systolic and diastolic blood pressure in a small group of subjects with essential hypertension. Hypertension is another risk factor for atherosclerosis and coronary heart disease. Another study showed pyridoxine hydrochloride to inhibit ADP- or epinephrine-induced platelet aggregation and to lower total cholesterol levels and increase HDL-cholesterol levels, again in a small group of subjects. Vitamin B6, in the form of pyridoxal 5'-phosphate, was found to protect vascular endothelial cells in culture from injury by activated platelets. Endothelial injury and dysfunction are critical initiating events in the pathogenesis of atherosclerosis. Human studies have demonstrated that vitamin B6 deficiency affects cellular and humoral responses of the immune system. Vitamin B6 deficiency results in altered lymphocyte differentiation and maturation, reduced delayed-type hypersensitivity (DTH) responses, impaired antibody production, decreased lymphocyte proliferation and decreased interleukin (IL)-2 production, among other immunologic activities. Used for the treatment of vitamin B6 deficiency and for the prophylaxis of isoniazid-induced peripheral neuropathy.
Status:
US Approved OTC
Source:
21 CFR 333.110(a) first aid antibiotic:ointment bacitracin
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ACHIRAL)



Bacitracin is a polypeptide antibiotic produced by Bacillus subtilis and Bacillus licheniformis. Bacitracin in combination with neomycin and polymyxin B is indicated for the treatment of many bacterial diseases. The antibacterial properties of bacitracin are mediated by its binding to C55-isoprenyl pyrophosphate, resulting in inhibition of cell wall biosynthesis.

Showing 21 - 30 of 32 results