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Restrict the search for
telotristat ethyl
to a specific field?
Status:
Investigational
Source:
NCT00838591: Phase 2 Interventional Completed Asthma
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.
Status:
Investigational
Source:
NCT01507194: Phase 2 Interventional Completed Postoperative Nausea and Vomiting
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Vestipitant, also known as GW597599, is a neurokinin1 receptor antagonist that was being developed by GlaxoSmithKline for the treatment of postoperative nausea and vomiting. Vestipitant is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It was under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus and insomnia. Vestipitant was shown to improve sleep maintenance in patients with primary insomnia, with no associated next-day cognitive impairment. The effects on wake after sleep onset and total sleep time were maintained following repeated dosing. Vestipitant has anxiolytic properties and a good safety profile. Vestipitant was investigated for potential effect against chronic tinnitus as a stand-alone treatment and in conjunction with a selective serotonin reuptake inhibitor, paroxetine. Although well-tolerated vestipitant, alone or in combination with paroxetine, was not effective in ameliorating tinnitus in this patient group.
Class (Stereo):
CHEMICAL (RACEMIC)
IROLAPRIDE is an antiemetic agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Class (Stereo):
CHEMICAL (RACEMIC)
Etacepride is a neuroleptic and antiemetic agent.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lodazecar is a benzodiazepine derivative, which does not bind to the brain benzodiazepine receptor. The drug shares some similarity in tertiary structure with the cholesterol molecule. Oral administration of lodazecar in the cholesterol-fed rat is associated with significant changes in plasma lipoproteins and in key enzymes controlling hepatic cholesterol metabolism. In human the treatment reduced both the fractional and the absolute cholesterol absorption and increased fecal neutral sterol excretion by about 50%, serum plant sterol levels were reduced, most probably because of diminished sterol absorption. Biliary cholesterol secretion was unchanged.
Class (Stereo):
CHEMICAL (ACHIRAL)
Coumazoline is a vasoconstrictor developed as a nasal decongestant by a French corporation Labez. Intravenous administration of the compound to dogs lead to a marked and prolonged drop in the temperature of the gingival mucosa. In rats, coumazoline caused slowing of the dye diffusion on the surface of the skin. The compound did not influence the ciliary motility, as was measured on an isolated guinea pig trachea.
Class (Stereo):
CHEMICAL (RACEMIC)
Bervastatin (also known as LS 2904), a synthetic HMG-CoA reductase inhibitor that was developed for the treatment of hyperlipidemia. However, information about further development is not available.
Class (Stereo):
CHEMICAL (ACHIRAL)
Benzethidine an opioid analgesic that was forbidden for use.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Binospirone (MDL-73,005-EF) acts as a potent, highly selective 5-HT1A ligand: as an antagonist at postsynaptic 5-HT1A receptors and also acts as a highly efficacious partial agonist at somatodendritic autoreceptors. Experiments on rodents have shown, that it also possesses anxiolytic properties.
