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

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Showing 30601 - 30610 of 34955 results

Status:
Investigational
Source:
USAN:Amicibone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Amicibone is an antitussive agent.
Status:
Investigational
Source:
Clin Pharmacol Ther. May 2021;109(5):1274-1281.: Not Applicable Human clinical trial Completed Multiple System Atrophy/blood
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01052012: Phase 3 Interventional Completed Postoperative Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lambda-cyhalothrin (λ-cyhalothrin), a mixture of isomers of cyhalothrin belongs to a class of insecticides known as synthetic pyrethroids. Synthetic pyrethroids are often preferred to the real thing as an active ingredient because they offer the added bonus of remaining effective for longer period. λ-cyhalothrin was the most commonly used pyrethroid insecticide for vegetable farming in Benin. Experiments have shown that λ-cyhalothrin residues in lettuce and cabbage from farms and markets in Parakou and Cotonou were relatively safe for consumption.
Status:
Investigational
Source:
NCT03042702: Phase 2 Interventional Completed Ovarian Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


4-Isothioureidobutyronitrile (Kevetrin) is a small molecule that has demonstrated the potential of becoming a breakthrough cancer treatment by inducing activation of p53. It is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Upon intravenous administration, 4-thioureidobutyronitrile activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. 4-Thioureidobutyronitrile may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells. Cellceutix continues to build upon the successful Phase 1 trial evaluating Kevetrin in treating advanced solid tumors conducted at Dana-Farber Cancer Institute and Beth Israel Deaconess Medical Center. Kevetrin, in IV form, was shown to safely modulate, in a non-genotoxic manner, the key tumor suppressor protein p53 as measured through increased expression of p21, a key downstream biomarker of p53. Cellceutix is advancing Kevetrin under an Orphan Drug designation from the Food and Drug Administration (FDA) for the treatment of ovarian cancer, pancreatic cancer and childhood retinoblastoma.
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
INN:furterene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Furterene is a diuretic of the aminopteridine series, with aldosterone antagonist activity. Furterene is able to antagonize aldosterone at the mineralocorticoid receptor in the kidneys. It thereby increases sodium excretion while inhibiting potassium excretion.
Status:
Investigational
Source:
NCT00942656: Not Applicable Interventional Completed Cardiovascular Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Rumenic acid is the major conjugated linoleic acid (CLA), probably because of successive desaturation and chain elongation and can be considered as the principal dietary form. In experiments on rodents was shown that rumenic acid possessed the protective effect against colitis, which was associated with the activation of the Nrf2 pathway.
Status:
Investigational
Source:
INN:fandofloxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fandofloxacin is a difluoroquinolone derivative. This compound possesses an antibacterial spectrum comparable to those of rufloxacin and ciprofloxacin in vivo. Fandofloxacin showed a rapid and nearly complete absorption, and a long residence time in the body. Because it has been reported that the in vivo antibacterial activity of Fandofloxacin is comparable or superior to other quinolones, despite the fact that its in vitro activity is significantly lower than that of the other compounds, the pharmacokinetics of this antibiotic may be responsible, at least in part, for the enhanced in vivo antibacterial activity of Fandofloxacin. Fandofloxacin is an inhibitor of bacterial DNA gyrase. The toxicities and adverse effects of Fandofloxacin observed in various toxicology studies and clinical trials were less than those of commercially available drugs. It has been in phase II clinical trial for the treatment of Urinary tract infections. However, this research has been discontinued in 2008.
Status:
Investigational
Source:
NCT01168479: Phase 3 Interventional Completed Prostate Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Imazapic is a selective herbicide for both the pre- and post-emergent control of some annual and perennial grasses and some broadleaf weeds. Imazapic kills plants by inhibiting the production of branched chain amino acids, which are necessary for protein synthesis and cell growth. It has been useful for weed control in natural areas, particularly in conjunction with the establishment of native warm-season prairie grasses and certain legumes. Imazapic is relatively non-toxic to terrestrial and aquatic mammals, birds, and amphibians. It has a low level of toxicity to birds but is more toxic to aquatic life and honey bees. It has a high potential for bioaccumulation. Imazapic has an average half-life of 120 days in soil. It is may be persistent in soil systems but usually degrades quickly in aquatic systems via photolysis. It has a high aqueous solubility, is volatile and, based on its chemical properties, is moderately mobile and may leach to groundwater.
Status:
Investigational
Source:
Clin Pharmacol Ther. May 2021;109(5):1274-1281.: Not Applicable Human clinical trial Completed Multiple System Atrophy/blood
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 30601 - 30610 of 34955 results