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

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Showing 311 - 320 of 713 results

Status:
Possibly Marketed Outside US
Source:
NCT02644707: Phase 4 Interventional Completed Autoimmune Thyroiditis
(2014)
Source URL:
First approved in 2000

Class (Stereo):
CHEMICAL (ABSOLUTE)



L-isomer of selenomethionine (Se-met) is a major natural food-form of selenium, synthetic L-Se-met or enriched food sources thereof such as selenium yeast are appropriate supplemental forms of Se for humans; for animals, DL-Se-met is acceptable. Ingested Se-met is either metabolized directly to reactive forms of selenium or stored in place of methionine in body proteins. Se-met metabolism is closely linked to protein turnover. 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.
Status:
Possibly Marketed Outside US
Source:
NCT00894153: Phase 4 Interventional Unknown status Neoplasms
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Tetrofosmin is a phosphor-organic compound, belonging to the group of diphosphines. Tetrofosmin is used as a component of a Technetium (99mTc) tetrofosmin complex. Due to the relatively short half-life of Tc99m (6 hours), just before the administration, the solution of tetrofosmin should be reconstituted with Tc99m pertechnetate to form a complex of Tc99m Tetrofosmin. When administered intravenously, Tc99m Tetrofosmin shows rapid myocardial uptake and its distribution follows a linear relationship with coronary blood flow. It is taken up by the mitochondria of myocardial cells by passive diffusion and appears to accumulate in viable myocardial tissue. Tc99m Tetrofosmin is used as a diagnostic agent used to assess areas of reversible myocardial ischemia in the presence or absence of infracted myocardium and is also used to assess ventricular function.
Palmitic acid is a saturated fatty acid, the principal constituent of refined palm oil, present in the diet and synthesized endogenously. Palmitic acid is able to activate the orphan G protein-coupled receptor GPR40. Palmitic acid was also a weak ligand of peroxisome proliferator-activated receptor gamma. Palmitic acid is a ligand of lipid chaperones - the fatty acid-binding proteins (FABPs). Dietary palm oil and palmitic acid may play a role in the development of obesity, type 2 diabetes mellitus, cardiovascular diseases and cancer.
Status:
Possibly Marketed Outside US
Source:
Surfaxin by Thannhauser, S.J.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Dipalmitoylphosphatidylcholine (DPPC) is the main lipid component of surfactant, it reduces surface tension, preventing collapse of the alveoli. It is used in the treatment of neonatal respiratory distress. It is an important constituent of the number of surfactant, such as Curosurf®, Lucinactant, Exosurf. Porcine-derived lung surfactant Curosurf® (poractant alfa) intratracheal suspension is indicated for the rescue treatment of respiratory distress syndrome (RDS) in premature infants. Each milliliter of suspension contains 80 mg of poractant alfa that includes 76 mg of phospholipids and 1 mg of protein of which 0.45 mg is SP-B and 0.59 mg is SP-C. The amount of phospholipids is calculated from the content of phosphorus and contains 55 mg of phosphatidylcholine of which 30 mg is dipalmitoylphosphatidylcholine. Curosurf reduces mortality and pneumothoraces associated with RDS. Lucinactant is a new synthetic peptide-containing surfactant for intratracheal use. It contains sinapultide, phospholipids (dipalmitoylphosphatidylcholine, DPPC and palmitoyloleoyl phosphatidylglycerol, POPG) and a fatty acid (palmitic acid). Intended for the prevention of RDS in premature infants at high risk for RDS. FDA approved on March 6, 2012. Exosurf, approved by FDA in 1990, is a protein-free surfactant composed of 85% dipalmitoylphosphatidylcholine, 9% hexadecanol, and 6% tyloxapol by weight.
Status:
Possibly Marketed Outside US
Source:
NCT04704518: Phase 4 Interventional Completed Photorefractive Keratectomy
(2022)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Trehalose, a naturally occurring disaccharide of glucose that appears to function in an anhydrobiotic capacity in many organisms. Bioblast Pharma study trehalose in Phase 2 for treating patients with Oculopharyngeal Muscular Dystrophy (OPMD) and spinocerebellar ataxia, type 3. In OPMD trehalose prevents the aggregation of the pathological protein (PABPN1) in muscle cells, the hallmark of the disease, by stabilizing the protein, reducing the formation of protein aggregations, and promoting their clearance from cells through autophagy, thus preventing muscle cell death. Trehalose induces autophagy via mTOR independent pathway. It activates TFEB, a master controller of lysosomal biogenesis and autophagy, by inhibiting AKT which is a negative regulator of TFEB that acts by direct phosphorylation (and inhibition) of TFEB. In addition, trehalose protects cells from hypoxic and anoxic injury and suppresses protein aggregation. In vivo studies with trehalose show cellular and behavioral beneficial effects in animal models of neurodegenerative diseases. Trehalose was in phase III clinical trial to study if it was possible to use the drug as add-on therapy in Bipolar Depression. Also in combination with hyaluronate, it can be used to treat dry eye syndrome. Trehalose protects the epithelial cells on the ocular surface, improving their resistance to the daily stresses of dry environments and tear film changes in a dry eye.
Status:
Possibly Marketed Outside US
Source:
WHO-ESSENTIAL MEDICINES LIST:6.5.5.1
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Melarsoprol is an organoarsenic compound that was used for the treatment of sleeping sickness (African trypanosomiasis) since 1949. Melarsoprol is used for the treatment of second-stage infection (involving the central nervous system). It is the only available therapy for second-stage Trypanosoma brucei rhodesiense (East African) infection. Melarsoprol is a prodrug, upon administration it is metabolized to the active form melarsen oxide, which acts by interacting with protein sulfhydryl groups and subsequently inactivating enzymes. A small but adequate amount of the drug penetrates the cerebrospinal fluid, where it is taken up and concentrated by trypanosomes. Due to the high toxicity of the drug, it is administered only in the most dangerous cases. Melarsoprol is not commercially available in the USA, but it is available as treatment IND from CDC.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Formestane (trade name Lentaron) is a type I, steroidal, selective aromatase inhibitor used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. Formestane has poor oral bioavailability and thus must be administered fortnightly (bi-weekly) by intramuscular injection. Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Estrogen-sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone-sensitive breast cancers. Common side effects associated with the use of an aromatase inhibitor include hot flashes, joint pain, weakness, fatigue, mood changes, depression, high blood pressure, swelling of the arms/legs, and headache. Aromatase inhibitors may also decrease bone mineral density, which may lead to osteoporosis and an increase in fractures in susceptible patients. Formestane was the first selective aromatase inhibitor to be developed as a prescription drug, first appearing in Europe during the mid-1990s under the Lentaron Depot brand name. With the emergence of newer and more effective aromatase inhibitors, however, formestane soon lost market presence at a rapid rate. Most of the initial Lentaron preparations have since been discontinued. Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance with the regulations of the World Anti-Doping Agency. The drug remains available today, but only in a small number of nations. This includes Austria, Brazil, Czech Republic, Hong Kong, and Turkey.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Brivudine (trade names Zostex, Mevir, Brivir, among others) is an antiviral drug used in the treatment of herpes zoster ("shingles"). Brivudine is an analog of the nucleoside thymidine. The active compound is brivudine 5'-triphosphate, which is formed in subsequent phosphorylations by viral (but not human) thymidine kinase and presumably by the nucleoside-diphosphate kinase. Brivudine 5'-triphosphate works because it is incorporated into the viral DNA, but then blocks the action of DNA polymerases, thus inhibiting viral replication. Brivudine is used for the treatment of herpes zoster in adult patients. It is taken orally once daily, in contrast to aciclovir, valaciclovir, and other antivirals. A study has found that it is more effective than aciclovir, but this has been disputed because of a possible conflict of interest on part of the study authors. The drug is contraindicated in patients undergoing immunosuppression (for example because of an organ transplant) or cancer therapy, especially with fluorouracil (5-FU) and chemically related (pro)drugs such as capecitabine and tegafur, as well as the antimycotic drug flucytosine, which is also related to 5-FU. It has not been proven to be safe for children and pregnant or breastfeeding women. The drug is generally well tolerated. The only common side effect is nausea (in 2% of patients). Less common side effects (<1%) include a headache, increased or lowered blood cell counts (granulocytopenia, anemia, lymphocytosis, monocytosis), increased liver enzymes, and allergic reactions. Brivudine is approved for use in a number of European countries including Austria, Belgium, Germany, Greece, Italy, Portugal, Spain, and Switzerland.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tolfenamic acid is a selective COX-2 inhibitor, which was marketed in Europe for the treatment of acute migraine disorders. Tolfenamic acid is currently unavailable for human use, however, it may be prescribed for veterinary purposes.

Showing 311 - 320 of 713 results