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

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Showing 61 - 70 of 94 results

Status:
US Previously Marketed
First approved in 2006

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade names Sebivo (Europe) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance. Telbivudine is a synthetic thymidine nucleoside analogue; it is the L-isomer of thymidine. It is taken orally in a dose of 600 mg once daily with or without food. TYZEKA is the trade name for telbivudine, a synthetic thymidine nucleoside analogue with activity against hepatitis B virus (HBV). The chemical name for telbivudine is 1-((2S,4R,5S)-4-hydroxy-5-hydroxymethyltetrahydrofuran-2-y1)-5-methyl-1H-pyrimidine-2,4-dione, or 1-(2-deoxy-β-L-ribofuranosyl)-5-methyluracil. Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination, resulting in inhibition of HBV replication. Telbivudine is an inhibitor of both HBV first strand (EC50 value = 1.3 ± 1.6 µM) and second strand synthesis (EC50 value = 0.2 ± 0.2 µM). Telbivudine 5'-triphosphate at concentrations up to 100 µM did not inhibit human cellular DNA polymerases α, β, or γ. No appreciable mitochondrial toxicity was observed in HepG2 cells treated with telbivudine at concentrations up to 10 µM.
Hygromycin B is a water-soluble antibiotic purified from the bacterium Streptomyces hydroscopicus.It kills bacteria, fungi and higher eukaryotic cells by inhibiting protein synthesis. It has been reported to interfere with translocation and to cause mistranslation at the 70S ribosome.Hygromycin B is used as a selective agent in molecular genetics experiments on a wide variety of eukaryotic and prokaryotic species. Under the trade name Hygromix, Hygromycin B is used in chickens as an aid in the control of infections of the following intestinal parasites: large roundworms (Ascaris galli), cecal worms (Heterakis gallinae) and capillary worms (Capillaria obsignata) and in Swine as an aid in the control of infections of the following intestinal parasites: large roundworms (Ascaris suis), nodular worms (Oesophagostomum dentatum) and whipworms (Trichuris suis).
Status:
Possibly Marketed Outside US
Source:
Dairyland Brand Teat Dip by Stearns Packaging Corporation
(1978)
Source URL:
First approved in 1978
Source:
Dairyland Brand Teat Dip by Stearns Packaging Corporation
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rhodamine B is a fluorescent dye whose quantum yield is strongly dependent on temperature in the range of 0°C to 100°C, making it ideal for liquid based systems. It is a cell-permeant fluorogenic dye most often used as a conjugate to antibodies and proteins for fluorescence detection in microscopy. Rhodamine B is widely used in industrial purposes, such as printing and dyeing in textile, paper, paints, leathers etc. Rhodamine B was tested for use as a biomarker in oral rabies vaccines for raccoons, to identify animals that have eaten a vaccine bait. It has also been used as an anterograde and retrograde tracer in neurons and in nanoparticles to detect apoptosis.
Status:
Possibly Marketed Outside US
Source:
PERACON
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Conditions:

Isoaminile is a cough suppressant that acts by influencing the cough centre.
Status:
Possibly Marketed Outside US
Source:
NCT00950430: Phase 4 Interventional Enrolling by invitation Alzheimer's Disease
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pittsburgh compound B (PiB) is a radioactive analog of thioflavin T, which can be used in positron emission tomography scans to image beta-amyloid plaques in the brains of patients with Alzheimer’s disease. 11C-PIB specifically binds to Aβ40 and Aβ42 fibrils and insoluble plaques containing the aforementioned Aß peptides with no detectable binding to soluble Aβ forms or neurofibrillary tangles under PET study conditions. Furthermore, this radiotracer does not bind to neurofibrillary tangles (NFTs) in the neuronal regions of the brain during postmortem autopsies. A typical injected dose ranges from 250-450 MBq and the imaging time normally varies between 40 and 90 minutes. The quantification of 11C-PIB has demonstrated to elicit a profound difference in neuronal cortical binding between individuals recognized with Alzheimer's disease and age-matched cognitively normal controls.
Polymyxin B is a lipopeptide antibiotic isolated from Bacillus polymyxa. Its basic structure consists of a polycationic peptide ring and a tripeptide side chain with a fatty acid tail. Polymyxin B is a mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components. Polymyxin B acts on Gram-negative bacteria by interacting with lipopolysaccharide (LPS) of the outer membrane and destabilizing it. Polymyxin B is indicated for the treatment of many bacterial diseases such as meningeal infections, urinary tract infections and bacteremia.

Showing 61 - 70 of 94 results