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Restrict the search for
beta carotene
to a specific field?
Status:
Investigational
Source:
INN:levomoprolol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levomoprolol (L-moprolol) is a beta-adrenergic blocker which was introduced as an oral medication for treatment of systemic hypertension. It was found to be effective in 2% eyedrops in reducing the intraocular pressure in glaucoma. Observations on glaucoma patients treated with the eyedrop for 1.5 to 2.5 years was without undesirable side effects. L-moprolol and dipivefrin had an equivalent effect in lowering the intraocular pressure. The association of the two drugs caused a further reduction of intraocular pressure.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Drocinonide is a synthetic glucocorticoid used as anti-inflammatory agent. It was shown that drocinonide phosphate potassium is effective ocular anti-inflammatory agent that does not show a strong tendency to elevate the intra-ocular pressure. Drocinonide phosphate potassium forms an insoluble complex with neomycin sulfate in aqueous solution. Dibasic sodium phosphate can be employed in an ophthalmic formulation to prevent the formation of this precipitate without affecting the stability of the steroid or the bioactivity of the antibiotic.
Status:
Investigational
Source:
INN:dexpramipexole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dexpramipexole (also known as KNS-760704/R-pramipexole) was originally developed by University of Virginia researchers to treat Amyotrophic Lateral Sclerosis and then was licensed to global biotechnology company Biogen Idec for further development. However, on phase III clinical trial the study of this drug was discontinued. Biogen said the drug neither slowed the loss of muscle function nor prolonged the lives of patients with ALS, often called Lou Gehrig’s disease. Nor did it show any efficacy in secondary endpoints of the clinical trial, or work in any sub-group of patients—about a big a failure as a company could have a Phase III trial. In addition, was discovered, that dexpramipexole was able to bind to beta-subunit of the mitochondrial F1/FO ATP synthase complex and increased its activity, thus reduced ischemic brain injury. These findings, together with the excellent brain penetration and favorable safety profile in humans, make dexpramipexole a drug with realistic translational potential for the treatment of stroke.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Amibegron (SR 58611A or SR 58611) is a highly selective agonist for atypical beta3-adrenoceptors. It stimulates neuronal activity in a specific area of the prefrontal cortex and also inhibits intestinal motility. Amibegron was in phase III trials worldwide for the treatment of depression and generalised anxiety disorder but development of the product was discontinued in 2008. Amibegron has been tested for its potential as a treatment for irritable bowel syndrome.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Binodenoson, a selective adenosine A(2A) receptor agonist, was being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging. Binodenoson for injection under the brand name CorVue was developed for use in patients with or at risk for coronary artery disease (CAD) who are unable to perform a cardiac exercise stress test. CorVue was designed to minimize side effects such as dyspnea, flushing, heart block, and chest pain. Binodenoson did not achieve FDA approval in 2009 due to concerns over equivalence of its efficacy with adenosine.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
FLAVODILOL is an antihypertensive agent.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Telatinib (Bay-579352) developed by Bayer is an orally available and highly potent inhibitor of tyrosine kinases VEGFR2,VEGFR3, PDGFR and c-Kit. Telatinib is a potent inhibitor of angiogenesis. Telatinib caused a significant decrease in endothelium-dependent and endothelium-independent vasodilation. Telatinib demonstrates anti-tumor activity in various cancer models. Telatinib is ready for phase III clinical trials for the treatment of gastric cancer. In 2010, it has been granted orphan drug status by the FDA. Most frequent adverse events were pain, nausea, voice changes and fatigue.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Talibegron (ZD2079) is a β3 adrenoceptor agonist and insulin sensitiser. It was developed as a potential treatment for obesity and non-insulin-dependent diabetes mellitus. Talibegron hydrochloride had been in phase II clinical trials by AstraZeneca for the treatment of type 2 diabetes and obesity. However, this research has been discontinued.
Status:
Investigational
Source:
INN:sulfonterol [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Sulfonterol is a benzenemethanol derivative patented by Smith Kline and French Laboratories as a bronchodilator. Sulfonterol acts as a β-adrenergic partial agonist.
Status:
Investigational
Source:
INN:tarenflurbil [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Tarenflurbil (Flurizan or R-flurbiprofen) is the single enantiomer of the racemate NSAID flurbiprofen. Tarenflurbil is a first in class, selective amyloid-beta42 (A42) lowering agent (SALA), which acts by modulating the activity of gamma-secretase, an enzyme that converts amyloid precursor protein to amyloid-beta. The reduction of A42 may prevent the development of the amyloid plaques thought to be a key pathological process associated with Alzheimer’s disease. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease. In a brief statement issued June 30, Myriad Genetics reports that tarenflurbil (Flurizan) failed to have a significant effect in a phase 3 trial of patients with mild Alzheimer's disease (AD). The failure of Flurizan™ is generally attributed to its insufficient pharmacodynamics, i.e., inadequate ability to penetrate the brain and engage its target protein at doses sufficient to yield an effect. Two additional Phase 3 trials were terminated and further development of Flurizan™ was discontinued. Separate clinical development of Flurizan™ for prostate cancer has also been discontinued following negative Phase 2 results. Tarenflurbil activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in the arrest of tumour cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumour cells. Tarenflurbil does not inhibit the enzyme cyclooxygenase. The Fraunhofer Institute for Molecular Biology and Applied Ecology is currently developing tarenflurbil for the treatment of relapsing, remitting multiple sclerosis.
