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

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Status:
US Previously Marketed
Source:
Quilene by Warner /Chilcott
(1969)
Source URL:
First approved in 1969
Source:
Quilene by Warner /Chilcott
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Conditions:

PENTAPIPERIUM is a synthetic quaternary ammonium anticholinergic and the antisecretory agent used especially in the treatment of peptic ulcer.
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.
Cortisone is a hormone that is FDA approved for the treatment of primary and secondary adrenocortical deficiency, rheumatic disorders, psoriasis, exfoliative dermatitis, bronchial asthma, allergic conjunctivitis, hemolytic anemia, enteritis, tuberculosis, trichnosis. Cortisone acetate binds to the cytosolic glucocorticoid receptor. After binding the receptor, the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. Common adverse reactions include convulsions, increased intracranial pressure with papilledema, vertigo, headache, psychic disturbances, hirsuitism, glaucoma, exophthalmos. Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression. Co-administration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports. Cortisone is a natural steroid hormone. Its sulfate analog has been detected in in umbilical vein blood fetus plasma between 19 and 32 weeks of gestation with a significant increase at 29-30 weeks and in amniotic fluid. Base on the experiments with rats it was suggested that cortisone sulfate in mammals could be hydrolyzed enzymatically liberating sulfate ions from cortisone. Cortisone sulfate has been proposed for use as one of the glycosaminoglycan compound materials in a cartilage prosthesis and biological nasal bridge implant manufacture as well as auxiliary agent in powder aerosol composition for use in baby powder, dry shampoo, water-eczema remedy and antiperspirant.
Status:
US Previously Marketed
Source:
Zinc Valerate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Zinc Valerate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Valeric acid is a colorless, oily liquid with an unpleasant odor. It is highly corrosive and must be handled with care. Valeric acid is mainly used as a chemical intermediate to manufacture flavors and perfumes, synthetic lubricants, agricultural chemicals, and pharmaceuticals. It is also used as a flavoring aid in foods. Valeric acid is considered safe as a food additive by the World Health Organization.
Status:
US Previously Marketed
Source:
Zinc Valerate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Zinc Valerate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Valeric acid is a colorless, oily liquid with an unpleasant odor. It is highly corrosive and must be handled with care. Valeric acid is mainly used as a chemical intermediate to manufacture flavors and perfumes, synthetic lubricants, agricultural chemicals, and pharmaceuticals. It is also used as a flavoring aid in foods. Valeric acid is considered safe as a food additive by the World Health Organization.
Status:
US Previously Marketed
Source:
Zinc Valerate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Zinc Valerate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Valeric acid is a colorless, oily liquid with an unpleasant odor. It is highly corrosive and must be handled with care. Valeric acid is mainly used as a chemical intermediate to manufacture flavors and perfumes, synthetic lubricants, agricultural chemicals, and pharmaceuticals. It is also used as a flavoring aid in foods. Valeric acid is considered safe as a food additive by the World Health Organization.
Status:
US Previously Marketed
Source:
Zinc Valerate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Zinc Valerate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Valeric acid is a colorless, oily liquid with an unpleasant odor. It is highly corrosive and must be handled with care. Valeric acid is mainly used as a chemical intermediate to manufacture flavors and perfumes, synthetic lubricants, agricultural chemicals, and pharmaceuticals. It is also used as a flavoring aid in foods. Valeric acid is considered safe as a food additive by the World Health Organization.
Status:
Possibly Marketed Outside US
Source:
Canada:LIPOIC ACID, ALPHA
Source URL:
First approved in 2001
Source:
Strovite OneCaplets by Exeltis USA, Inc.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Thioctic acid also known as alpha-lipoic acid is a dietary supplement, which is a common ingredient in OTC (over-the-counter) multivitamin formulas and anti-aging supplements. Thioctic acid exists in both R- and S-enantiomeric forms, however, only R-form is essential as a cofactor in biological systems (the acid is coupled via an amide linkage to a lysine of several multienzyme complexes, such as the pyruvate dehydrogenase complex, the alpha-ketoglutarate dehydrogenase complex, the glycine cleavage system and the branched-chain oxo acid dehydrogenase complex). Most commercially available thioctic acid supplements are a mixture of both R and S enantiomers or R-form alone. Several studies have shown that the acid has beneficial effect on diabetes complications, cancer, glaucome, liver disease, etc. The mechanisms of thioctic acid is related to its antioxidant properties, metal chelator properties, however, those mechanisms need futher confirmation.
Status:
Possibly Marketed Outside US
Source:
Japan:Anecortave Acetate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Anecortave is a novel angiogenesis inhibitor used in the treatment of the exudative (wet) form of age-related macular degeneration. It will be marketed by Alcon as anecortave acetate (AA) for depot suspension under the trade name Retaane. In 2007 they received their letter of approval for Retaane’s indication to treat wet age-related macular degeneration (AMD), but final approval would require the completion of an additional clinical study. As a result, the Anecortave Acetate Risk-Reduction Trial (AART) was continued to be supported by Alcon. This study looked at the efficacy of Retaane to reduce the progression of the dry from of AMD to the wet-form. In 2008, Alcon Inc. announced they were terminating the development of anecortave acetate for the prevention of developing sight-threatening choroidal neovascularization secondary to age-related macular degeneration. In 2009, Alcon Inc. announced they would terminate the development of the drug for the reducing intraocular pressure associated with glaucoma. Currently, anecortave acetate is not on the market or being made for therapeutic use by Alcon Inc.[7] This could be due to the lack of efficacy of clinical trials with anecortave acetate or because of newer more efficacious products that are currently on the market. Anecortave acetate functions as an antiangiogenic agent, inhibiting blood vessel growth by decreasing extracellular protease expression and inhibiting endothelial cell migration. Its angiostatic activity does not seem to be mediated through any of the commonly known pharmacological receptors. RETAANE blocks signals from multiple growth factors because it acts downstream and independent of the initiating angiogenic stimuli and inhibits angiogenesis subsequent to the angiogenic stimulation. Recently was discovered, that phosphodiesterase 6-delta (PDE6D) was a molecular binding partner of AA and this provided insight into the role of this drug candidate in treating glaucoma.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Diflucortolone (used in the form of valerate prodrug) is a corticosteroid developed for the treatment of inflammatory skin diseases. It is supposed that Diflucortolone acts by inducing Annexin A1, a phospholipase A2 inhibitory protein, and thus controls the biosynthesis of prostagladins and leukotrienes. The drug is marketed as a cream under the tradename Nerisone.