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

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Showing 1531 - 1540 of 3321 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Padeliporfin is a vascular-acting photosensitizer consisting of a water-soluble, palladium-substituted bacteriochlorophyll derivative with antineoplastic activity. After administration, the drug is activated locally when the tumor bed is exposed to low-power laser light; reactive oxygen species (ROS) are formed upon activation and ROS-mediated necrosis may occur at the site of interaction between the photosensitizer, light and oxygen. Padeliporfin is approved in Europe for the treatment of adult patients with previously untreated, unilateral, low-risk, adenocarcinoma of the prostate and is marketed under tradename TOOKAD.
Status:
Possibly Marketed Outside US
Source:
NCT00856817: Phase 4 Interventional Terminated Atherosclerotic Cardiovascular Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Heme arginate (or haem arginate, brand name NORMOSANG) has been used to treat acute porphyrias. NORMOSANG successful uses in Europe and South Africa, but it has not been approved for use in the United States. Heme arginate consists of haem complexed with the amino acid arginine. This forms a stable compound. Haem arginate works by replenishing haem stores within the body. By negative feedback, haem arginate inhibits the initial rate-limiting enzyme of the haem synthetic pathway, ALA synthase (Delta-aminolevulinic acid dehydratase). The most frequent complication is phlebitis at the site of infusion. This can be reduced by giving the infusion of haem arginate in a protein buffer such as stabilized human serum or human serum albumin. In addition, there were studies, which revealed, that heme arginate induced beneficial effects in some myelodysplastic syndrome (MDS) patients and had very few side effects. In addition was shown, that heme arginate could be useful in the treatment of thalassemia intermedia.
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.
Status:
Possibly Marketed Outside US
Source:
NCT04614233: Phase 4 Interventional Terminated Overweight and Obesity
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oleoylethanolamide (oleic monoethanolamide, OEA), the naturally occurring amide of ethanolamine and oleic acid, is an endogenous lipid that modulates feeding, body weight, and lipid metabolism by binding with high affinity to the ligand-activated transcription factor, peroxisome proliferator-activated receptor-alpha (PPAR-alpha). OEA reveals the pharmacological properties in the treatment of obesity, atherosclerosis and other diseases. It was shown, that OEA can be used to control hunger in Prader-Willi syndrome, in addition, it exhibited neuroprotective properties in Parkinson's disease experiments. OEA is an endogenous ligand of the orphan receptor GPR119, a G protein-coupled receptor (GPCR) expressed predominantly in the human and rodent pancreas and gastrointestinal tract and in rodent brain, suggesting that the reported effects of OEA on food intake may be mediated, at least in part, via the GPR119 receptor. Recently was shown, that OEA was an effective inhibitor of hyperpigmentation through activation of ERK, Akt and p38 pathways, inhibition of the CREB pathway, and subsequent down-regulation of MITF, TRP-1 and tyrosinase production. Therefore, OEA could be a useful therapeutic agent for use in the treatment of hyperpigmentation and could be an effective component in whitening and lightening cosmetics.
Status:
Possibly Marketed Outside US
Source:
Japan:Secalciferol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Secalciferol (24,25-DIHYDROXYVITAMIN D 3/24R,25(OH)(2)D(3)) is suggested to be an essential hormone for the process of bone fracture healing, it has a physiological role in human bone and mineral metabolism, leading to an enhancement of osteocalcin synthesis. Secalciferol is possibly to bind a nuclear protein vitamin D receptor (VDR) to the ligand binding domain, which is stereo-specific for Secalciferol. The downstream effect will be triggered after the binding, including the inhibition of calcium channel to regulate the calcium homeostasis, and the following reduction of p53 and Pi-induced cytochrome C translocation
Status:
Possibly Marketed Outside US
Source:
NCT01998620: Phase 4 Interventional Unknown status Hepatitis B
(2013)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



S-Adenosylmethionine (often referred to as SAMe) is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. SAM is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma (HCC), HepG2 cells and colon cancer cells. Because of structural instability, stable salt forms of SAM are required for its use as an oral drug. The commonly used salts: tosylate, butanedisulfonate, disulfate tosylate, disulfate ditosylate, and disulfate monotosylate. SAMe has been marketed in some European countries since the mid-1980s for the treatment of depression and for other medical conditions such as osteoarthritis (joint disease that causes joint pain and stiffness), fibromyalgia (widespread pain and stiffness). In addition, it is used to treat liver disease and migraine headaches. However, it is not formally approved in the UK for the treatment of depression, and in the USA, it is classified only as a dietary supplement. Some research suggests that it is more effective than placebo in treating mild-to-moderate depression and is just as effective as antidepressant medications without the side effects (headaches, sleeplessness, and sexual dysfunction). In addition, antidepressants tend to take 6 to 8 weeks to begin working, while It seems to begin more quickly. Researchers are not sure how SAMe works to relieve depression. But they speculate it might increase the amount of serotonin in the brain just as some antidepressants do. Many studies have examined injectable forms of SAMe, not oral supplements.
Status:
Possibly Marketed Outside US
Source:
NCT03388853: Phase 4 Interventional Completed COPD
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Doxofylline (7-(1, 3-dioxalan-2-ylmethyl) theophylline) is a novel xanthine bronchodilator which differs from theophylline in that it contains a dioxalane group in position 7. Doxofylline is indicated for the treatment of bronchial asthma, pulmonary disease with spastic bronchial component and Chronic Obstructive Pulmonary Disease (COPD). Doxofylline does not directly inhibit any of the known HDAC enzymes, and did not inhibit any phosphodiesterase (PDE) enzyme sub types or act as an antagonist at any of the known adenosine receptors, except for PDE2A(1), and adenosine A(2A) and only at the highest tested concentration (10(-4) M). Doxofylline has greatly decreased affinity towards adenosine A1 and A2 receptors, which explain its better safety profile. Moreover, it does not interfere with calcium influx into the cells nor antagonize calcium channel blockers. Doxofylline has been shown to be a more potent bronchodilator with fewer side effects than theophylline. This drug should not be administered together with other xanthine derivatives, including beverages and foods containing caffeine.
Status:
Possibly Marketed Outside US
Source:
BESTATIN by Nippon Kayaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ubenimex is a dipeptide, which specificallyinhibits the activity of leukotriene A4 hydrolase, aminopeptidase B and leucine aminopeptidase of the cell membrane. The drug was isolated from Streptomyces oliooreticuli in 1976 in Nippon Kayaku, Japan and approved for the treatment of acute non-lymphocytic leukemia under the name Bestatin. In the USA the drug is currentlu in Phase II for the treatment of pulmonary arterial hypertension and lymphedema.
Status:
Possibly Marketed Outside US
Source:
NCT00156988: Phase 4 Interventional Completed Burns
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ceric ammonium nitrate is the orange-red, water-soluble cerium salt used as the specialized oxidizing agent in organic synthesis and a standard oxidant in quantitative analysis. Ceric ammonium nitrate is essentially an oxidizing agent that comprises one electron that allows intramolecular and intermolecular carbon to hetero and carbon to carbon atom bond formation. In addition, it is utilized as an oxidizing agent for secondary alcohols that turn it into benzylic and ketones alcohols, which are oxidized into aldehydes.
Temoporfin is a photosensitizer (based on chlorin) used in photodynamic therapy for the treatment of squamous cell carcinoma of the head and neck. It is marketed in the European Union under the brand name Foscan. It is used in patients in whom other treatments have stopped working, and who are not suitable for radiotherapy (treatment with radiation), surgery or systemic chemotherapy (medicines used to treat cancer; ‘systemic’ means that they are given as treatments throughout the body). When Foscan is injected, temoporfin is distributed within the body, including within the tumour. When it is illuminated with laser light of a specific wavelength, temoporfin is activated and reacts with oxygen in the cells to create a highly reactive and toxic type of oxygen. This kills the cells by reacting with and destroying their components, such as their proteins and DNA. By restricting the illumination to the tumour, cell damage is limited to the tumour cells, leaving other areas of the body unaffected. The U.S. Food and Drug Administration (FDA) declined to approve Foscan in 2000. The EU approved its use in June 2001.

Showing 1531 - 1540 of 3321 results