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Restrict the search for
icosapent ethyl
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Chromocarb is benzo-γ-pyrone derivative with vasoprotection activity used to eliminate lipoperoxidation post-vitrectomy. Peroral treatment of rats with chromocarb significantly reduced the degradation of the vascular wall by intravenous collagenase, as demonstrated by a lesser permeability increase of the blood-brain barrier, a shorter recovery time, lower hydroxyproline levels in the cerebrospinal fluid and a lesser decrease of the collagen content of the brain capillary basal lamina.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.
Class (Stereo):
CHEMICAL (RACEMIC)
Orconazole, an imidazole derivative, was developed by Janssen Pharmaceutical as an antifungal agent, however, this drug has never been marketed
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.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
INN:butoprozine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Butoprozine increased the action potential duration like amiodarone, depressed the plateau phase like verapamil and decreased the amplitude and the maximum rate of depolarization. Butoprozine injected intravenously depressed sino-atrial node function, lengthened A-V nodal conduction time and the A-V nodal refractory period, and prolonged the atrial refractory period. Thus butoprozine acted preferentially on parts of the myocardial tissue where the slow inward current seems to be particularly involved. In this respect, butoprozine was more active than amiodarone, but in contrast to this drug, butoprozine did neither prolong the ventricular monophasic action potential duration nor the ventricular refractory period.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Trovirdine [LY 300046, LY 300082, PETT 1] is a NNRT inhibitor of HIV-1 RT, which progressed through Phase II trials for the treatment of HIV infection. Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM. Cell culture experiments demonstrated that LY300046 was a potent inhibitor of the replication of HIV-1 in human T-cell lines and human PBL, including spread of the virus from infected to uninfected T cells. It was potent against patient isolates as well as laboratory isolates of HIV-1 but was not active against HIV-2 or simian immunodeficiency virus.
Class (Stereo):
CHEMICAL (RACEMIC)
Batanopride, previously known as BMY-25801, a 5-hydroxytryptamine 3 receptor antagonist, was studied against emesis for cancer patients that were treated by chemotherapy procedure. Batanopride had the dose-limiting side effects including hypotension and long QT syndrome that is why any further experiments for its medical application were discontinued.
Status:
Investigational
Source:
NCT04528758: Early Phase 1 Interventional Suspended Coronary Artery Disease
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00244322: Phase 2 Interventional Completed Alzheimer's Disease
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Semagacestat (LY-450139) was a gamma secretase inhibitor being developed as a treatment for Alzheimer's disease by Eli Lilly. It was hoped that the drug would help to delay the onset of severe Alzheimer's disease, and thereby help preserve cognitive and executive functioning and in turn improve patient quality of life. Semagacestat (LY-450139) is designed to inhibit gamma secretase, an enzyme that is involved in the cleavage of APP to beta-amyloid. By decreasing production of beta-amyloid, it is hoped that gamma secretase inhibitors will exert a disease-modifying effect in Alzheimer's disease and thus slow or halt the destruction of nerve cells – the final stage in the amyloid cascade hypothesis. In March 2008 semagacestat (LY-450139) advanced to Phase III development, where it was evaluated in the IDENTITY (Interrupting Alzheimer's Dementia by EvaluatiNg Treatment of AmyloId PaThologY) trial, the first Phase III trial for this new anti-dementia drug. In August 2010, Eli Lilly announced its decision to halt the development of Semagacestat. The decision was taken after analysing the preliminary results of the second Phase III clinical trial of the drug, which indicated that semagacestat failed to slow disease progression. The drug, in fact, worsened cognition and the ability to perform day-to-day activities.
