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

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Showing 11 - 20 of 33 results

Deoxycholic acid is a a bile acid which emulsifies and solubilizes dietary fats in the intestine, and when injected subcutaneously, it disrupts cell membranes in adipocytes and destroys fat cells in that tissue. In April 2015, deoxycholic acid was approved by the FDA for the treatment submental fat to improve aesthetic appearance and reduce facial fullness or convexity. It is marketed under the brand name Kybella by Kythera Biopharma and is the first pharmacological agent available for submental fat reduction, allowing for a safer and less invasive alternative than surgical procedures. As a bile acid, deoxycholic acid emulsifies fat in the gut. Synthetically derived deoxycholic acid, when injected, stimulates a targeted breakdown of adipose cells by disrupting the cell membrane and causing adipocytolysis. This results in an inflammatory reaction and clearing of the adipose tissue remnants by macrophages. Deoxycholic acid's actions are reduced by albumin and tissue-associated proteins, therefore its effect is limited to protein-poor subcutaneous fat tissue. Protein-rich tissues like muscle and skin are unaffected by deoxycholic acid, contributing to its safety profile. Deoxycholic acid is a cytolytic agent. The physiologic effect of deoxycholic acid is by means of decreased cell membrane integrity. Deoxycholic acid inhibits miR-21 expression in primary rat hepatocytes in a dose-dependent manner, and increases miR-21 pro-apoptotic target programmed cell death 4 (PDCD4) and apoptosis. Deoxycholic acid decreases NF-κB activity, shown to represent an upstream mechanism leading to modulation of the miR-21/PDCD4 pathway.
Status:
US Approved OTC
Source:
21 CFR 344.1 otic:earwax removal aid carbamide peroxide 6.5% (in anhydrous glycerin)
Source URL:
First marketed in 1921
Source:
Hydrogen Peroxide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydrogen peroxide has been used in medicine for more than 100 years. It is known in surgery as a highly useful irrigation solution by virtue of both its hemostatic and its antimicrobial effects. Hydrogen peroxide is a mild antiseptic used on the skin to prevent infection of minor cuts, scrapes, and burns. It may also be used as a mouth rinse to help remove mucus or to relieve minor mouth irritation (e.g., due to canker/cold sores, gingivitis). This product works by releasing oxygen when it is applied to the affected area. The release of oxygen causes foaming, which helps to remove dead skin and clean the area. Hydrogen peroxide is a strong oxidizing agent used in aqueous solution as a ripening agent, bleach, and topical anti-infective. It is relatively unstable and solutions deteriorate over time unless stabilized by the addition of acetanilide or similar organic materials.
Status:
US Previously Marketed
First approved in 1999

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Mequinol (mequinol is 4-hydroxyanisole) is an active ingredient in topical drugs used for skin depigmentation. The mechanism of action of mequinol is unknown. Although mequinol is a substrate for the enzyme tyrosinase and acts as a competitive inhibitor of the formation of melanin precursors, the clinical significance of these findings is unknown.
Status:
US Previously Marketed
First approved in 1960
Source:
Dianabol by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Metandienone is an orally active synthetic anabolic-androgenic steroid. In 1970, the FDA accepted that Metandienone (Dianabol) was “Probably Effective” in treating post-menopausal osteoporosis and pituitary-deficient dwarfism. Methandrostenolone is still produced today, but typically in nations with loose prescription drug regulations and by companies that still prefer to cater to an underground athletic market. Androgenic side effects are still common with this substance. This may include bouts of oily skin, acne, and body/facial hair growth. Anabolic/androgenic steroids may also aggravate male pattern hair loss.
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:
Possibly Marketed Outside US
Source:
Canada:CADMIUM METALLICUM
Source URL:
First approved in 2018
Source:
EBV/CFS Plus by Deseret Biologicals, Inc.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Cadmium is a chemical element with symbol Cd and atomic number 48. Its most common oxidation state is +2. Cadmium has no known biological function in higher organisms, but a cadmium-dependent carbonic anhydrase has been found in marine diatoms. In humans, the highest concentration of cadmium is absorbed by the kidneys and up to 30 mg of cadmium is commonly inhaled during childhood and adolescence. Cadmium is under preliminary research for its toxicity in humans, potentially contributing to risks of cancer, cardiovascular disease, and osteoporosis. The most risk of cadmium toxicity is from industrial exposure to inhalation of dust and fumes, or ingestion of soluble cadmium compounds.
Status:
Possibly Marketed Outside US
Source:
NCT00329680: Phase 4 Interventional Completed Sepsis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gamolenic acid also known as gamma-linolenic acid is a natural component of Oenothera biennis L. (Evening Primrose). Gamolenic acid was used for the treatment of breast painand atopic dermatitis in Europe, although now the drug is withdrawn from the market (there is no safety issue associated with the withdrawal of the licences). The mechanism of action of gamolenic acid is connected with its interaction with prostanoid pathway.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxaceprol, a structural analog of hydroxyproline, has been used for several years for the treatment of osteoarthritis and rheumatoid arthritis, showing good gastrointestinal safety, particularly in comparison with NSAIDs. It was shown that oxaceprol does not inhibit the synthesis of prostaglandins in vitro, but acts predominantly by inhibiting leukocyte adhesion and migration, thus inhibiting inflammation at an early stage and helps in pain relief.
Status:
Possibly Marketed Outside US
Source:
Canada:SELENIUM
Source URL:
First approved in 1996
Source:
Strovite Forte Caplet by Everett Laboratories, Inc.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Selenium (Se) is mineral that is found in soil and occurs naturally in certain foods (such as whole grains, Brazil nuts, sunflower seeds, and seafood). Selenium, which is nutritionally essential for humans, is a constituent of more than two dozen selenoproteins that play critical roles in reproduction, thyroid hormone metabolism, DNA synthesis, and protection from oxidative damage and infection. Selenium is used to treat or prevent selenium deficiency. Selenium deficiency produces biochemical changes that might predispose people who experience additional stresses to develop certain illnesses. For example, selenium deficiency in combination with a second stress (possibly a viral infection) leads to Keshan disease, a cardiomyopathy that occurred in parts of China prior to a government-sponsored selenium supplementation program that began in the 1970s. Before the Chinese government supplementation program, adults in the Keshan disease areas had average selenium intakes of no more than 11 mcg/day; intakes of at least 20 mcg/day protect adults from Keshan disease. Selenium has been used in alternative medicine as an aid to treat Hashimoto's thyroiditis, and to treat high cholesterol. Selenium is an important enzyme in the prevention of cellular damage by free radicals and reactive oxygen species. Selenium is first metabolized to selenophosphate and selenocysteine. Selenium incorporation is genetically encoded through the RNA sequence UGA. This sequence is recognized by RNA ste loop structures called selenocysteine inserting sequences (SECIS). These structures require the binding of SECIS binding proteins (SBP-2) to recognize selenocystiene. The specialized tRNA is first bound to a serine residue which is then enzymatically processed to a selylcysteyl-tRNA by selenocystiene sythase using selenophosphate as a selenium donor. Other unidentified proteins are required as part of the binding of this tRNA to the ribosome. Numerous studies in animal models and more recent studies in humans have demonstrated cancer chemopreventive effects with Se. There is extensive evidence that monomethylated forms of Se are critical metabolites for chemopreventive effects of Se. Induction of apoptosis in transformed cells is an important chemopreventive mechanism. Apoptosis can be triggered by micromolar levels of monomethylated forms of Se independent of DNA damage and in cells having a null p53 phenotype. Cell cycle protein kinase cdk2 and protein kinase C are strongly inhibited by various forms of Se. Inhibitory mechanisms involving modification of cysteine residues in proteins by Se have been proposed that involve formation of Se adducts of the selenotrisulfide (S-Se-S) or selenenylsulfide (S-Se) type or catalysis of disulfide formation. Selenium may facilitate reactions of protein cysteine residues by the transient formation of more reactive S-Se intermediates. A novel chemopreventive mechanism is proposed involving Se catalysis of reversible cysteine/disulfide transformations that occur in a number of redox-regulated proteins, including transcription factors. A time-limited activation mechanism for such proteins, with deactivation facilitated by Se, would allow normalization of critical cellular processes in the early stages of transformation. Randomized controlled trials of selenium supplementation for cancer prevention have yielded conflicting results. In 2003, the FDA allowed a qualified health claim on foods and dietary supplements containing selenium to state that while “some scientific evidence suggests that consumption of selenium may reduce the risk of certain forms of cancer… FDA has determined that this evidence is limited and not conclusive”. Selenium is available in multivitamin/multimineral supplements and as a stand-alone supplement, often in the forms of selenomethionine or of selenium-enriched yeast (grown in a high-selenium medium) or as sodium selenite or sodium selenate.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Biphenamine is a local anesthetic with antibacterial and antifungal properties. It has been used in the treatment of seborrheic scalp disorders.

Showing 11 - 20 of 33 results