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

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Showing 1381 - 1390 of 3321 results

Status:
US Previously Marketed
Source:
Fugillin by Upjohn
(1953)
Source URL:
First approved in 1953
Source:
Fugillin by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Fumagillin, an antimicrobial compound first isolated in 1949 from the fungus Aspergillus fumigatusa, naturally occurring water-insoluble antibacterial agent developed by sanofi-aventis, is approved in France for the treatment of microsporidiosis. Fumagillin (Flisint, Sanofi-Aventis, Paris, France) has been approved in France since 2002 for the treatment of intestinal microsporidiosis due to E. bieneusi in patients with AIDS, and is also available through an expanded access program for patients without AIDS. It has not been approved, however, by the US Food and Drug Administration. The discovery of fumagillin, a MetAP-2 inhibitor, with potent antiangiogenic and antiproliferative activities promoted the development of fumagillin analogues as a novel class of anticancer agents. It has been the subject of research in cancer treatments by employing its angiogenesis inhibitory properties.
Status:
US Previously Marketed
Source:
Neodrol by Pfizer
(1953)
Source URL:
First approved in 1953
Source:
Neodrol by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


STANOLONE, also known as dihydrotestosterone, is a potent androgenic metabolite of testosterone and anabolic agent for systemic use. It may be used as a replacement of male sex steroids in men who have androgen deficiency, for example as a result of the loss of both testes, and also the treatment of certain rare forms of aplastic anemia which are or may be responsive to anabolic androgens.
Status:
US Previously Marketed
First approved in 1952

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Monobenzone is a topical drug used for medical depigmentation. The mechanism of action of monobenzone is not fully understood. Monobenzone is oxidized by tyrosinase from melanocytes to a toxic quinones which induce non-apoptotic melanocyte cell death.
Status:
US Previously Marketed
Source:
Inositol by Commercial Solvents
(1949)
Source URL:
First approved in 1949
Source:
Inositol by Commercial Solvents
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Inositol is a vitamin-like substance. It is found in many plants and animals. It is produced by the human body from glucose, it is not an essential nutrient. Inositol and some of its mono- and polyphosphates function as the basis for a number of signaling and secondary messenger molecules. Inositol is used for diabetic nerve pain, panic disorder, high cholesterol, insomnia, cancer, depression, schizophrenia, Alzheimer’s disease, attention deficit-hyperactivity disorder (ADHD), autism, promoting hair growth, a skin disorder called psoriasis, and treating side effects of medical treatment with lithium. Inositol is also used by mouth for treating conditions associated with polycystic ovary syndrome, including failure to ovulate; high blood pressure; high triglycerides; and high levels of testosterone. Inositol is possibly safe for most adults. It can cause nausea, tiredness, headache, and dizziness.
SODIUM GLYCOLATE, a sodium salt of carboxymethyl ether, is used as a pharmaceutical grade dissolution excipient for solid dosage forms. It absorbs water rapidly, resulting in swelling which leads to the rapid disintegration of tablets and capsules. Without a disintegrant, these may not dissolve appropriately and may effect the amount of active ingredient absorbed, thereby decreasing effectiveness.
Status:
US Previously Marketed
First approved in 1945
Source:
Methionine by Various Mfrs.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Methionine is an non-polar, aliphatic, essential α-amino acid that is used in the biosynthesis of proteins. High levels of methionine can be found in eggs, sesame seeds, Brazil nuts, fish, meats and some other plant seeds; methionine is also found in cereal grains. Most fruits and vegetables contain very little of it. Most legumes are also low in methionine. However, it is the combination of methionine and cystine which is considered for completeness of a protein. There is scientific evidence that restricting methionine consumption can increase lifespans in some animals. However, since methionine is an essential amino acid, it cannot be entirely removed from animals' diets without disease or death occurring over time. For example, rats fed a diet without methionine developed steatohepatitis (fatty liver), anemia and lost two thirds of their body weight over 5 weeks. Administration of methionine ameliorated the pathological consequences of methionine deprivation.
Glutamic acid is a non-essential aminoacid used in biosynthesis of proteins. Besides being a building block of proteins, glutamic acid plays a principal role in neural activation. Glutamate is also responsible for the umami (savory) flavor of certain foods. In medicine, glutamate is used as a metabolic supplemnet in patients undergoing coronary surgery.
Sulfapyridine is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. It was used to treat of infections in humans in particular, dermatitis herpetiformis (Duhring's disease), a skin problem, but that usage was discontinued by manufacturer. It is also known, that sulfapyridine is one of the two primary metabolite of the anti-inflammatory drug salicylazosulfapyridine.
Quinacrine was initially developed as an anti-malarial drug marketed under the name Atabrine. Also it was approved for the teratment of ascites, however it was wothdrawn for both indication in 1995 and 2003, respectively. The drug is also used for the treatment of giardiasis, lupus, rheumatoid arthritis, refractory pulmonary effusion and pneumothorax, induce female sterilization etc. Proposed mechanisms of action include DNA intercalation interference with RNA transcription and translation, inhibition of succinate oxidation interference with electron transport, inhibition of cholinesterase, and inhibitor of phospholipase.
Status:
US Previously Marketed
Source:
Dinitrophenol
(1933)
Source URL:
First marketed in 1933

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

2,4-dinitrophenol (DNP) is a FDA-banned weight-loss agent and EPA-regulated environmental toxicant, traditionally used in research labs as an uncoupler of OXPHOS. Although not licensed for human consumption, DNP and DNP crystal form are used by bodybuilders and extreme dieters for their fat burning properties through inhibiting efficient energy (ATP) production in cells. Through uncoupling mitochondrial oxidative phosphorylation by facilitating proton transport across the mitochondrial membrane, DNP leads to rapid consumption of energy without generating ATP and consequently, to increased fat metabolism. However, the weight-loss effect comes with serious, and in some cases potentially fatal, adverse side effects, namely hyperthermia (the leading cause of fatality with acute DNP toxicity) and cardiac arrest, but also diaphoresis, tachycardia, tachypnea, skin toxicity, Fourier’s gangrene and cataracts with low dose chronic exposure. The proposed mechanism of DNP induced toxicity suggests the activation of ATP-sensitive K channels.

Showing 1381 - 1390 of 3321 results