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

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Showing 731 - 740 of 14117 results

GSK 1059615, a pyridinylquinoline derivative, is a novel PI3K kinase and mTOR dual inhibitor. GSK1059615 was in phase I clinical trial in patients with solid tumors or lymphoma, but this study was terminated prematurely due to lack of sufficient exposure following single- and repeat dosing. In addition, recently was shown, that GSK 1059615 in xenograft mice models possessed anti-head and neck squamous cell carcinoma (HNSCC) cell activity.
Status:
Investigational
Source:
NCT01802320: Phase 2 Interventional Completed Colon Mucinous Adenocarcinoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MK-2206 is an oral selective allosteric inhibitor of Akt that targets all three isoforms of human Akt (Akt-1, Akt-2 and Akt-3). In a phase I study of solid tumors, MK-2206 demonstrated evidence of target modulation and anti-proliferative activity as a single agent and in combination with other agents. Current ongoing trials of MK-2206 include monotherapy and combination therapy in breast cancer, colorectal cancer, haematological malignancies, non-small cell lung cancer and other. Detected treatment-related adverse event are: rash, fatigue, hyperglycemia.
Status:
Investigational
Source:
NCT01279083: Phase 1/Phase 2 Interventional Completed Open-angle Glaucoma
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Evodenoson (ATL-313) is an agonist of adenosine A2A receptor. It exerts anti-inflammatory activity through activation of adenosine A2A receptors on CD4+ T cells and neutrophils. Evodenoson demonstrates efficacy in animal models of sepsis, myocardial infarction, allograft rejection and enteritis.
Status:
Investigational
Source:
NCT00690053: Phase 1 Interventional Completed Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:metynodiol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Metynodiol, a progestin agent that has never been marketed.
Status:
Investigational
Source:
NCT00385489: Phase 1 Interventional Completed Healthy
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



LXR-623 is a is a highly selective and orally bioavailable synthetic agonist of Liver X receptors (LXR) alpha and beta that has shown promise in animal models of atherosclerosis. In nonhuman primates with normal lipid levels, LXR-623 significantly reduced total (50-55%) and LDL-cholesterol (LDLc) (70-77%) in a time- and dose-dependent manner and increased expression of the target genes ABCA1 and ABCG1 in peripheral blood cells of rats, mice and monkeys. LXR-623 demonstrated efficacy for reducing lesion progression in the murine LDLR(-/-) atherosclerosis model with no associated increase in hepatic lipogenesis either in this model or Syrian hamsters and displayed a unique and favorable pharmacological profile suggesting it may be suitable for evaluation in patients with atherosclerotic dyslipidemia. Results from a single ascending-dose study of the safety, pharmacokinetics, and pharmacodynamics of LXR-623 in healthy humans confirmed the effect of LXR-623 concentration on ABCA1 and ABCG1 expression. LXR-623 was absorbed rapidly with peak concentrations (Cmax) achieved at about 2 hours and increased Cmax and area under the concentration-time curve in a dose-proportional manner. The mean terminal disposition half-life was between 41 and 43 hours independently of dose. Central nervous system—related adverse events were observed at the 2 top doses tested. LXR-623 showed brain penetration and caused tumor regression in a glioblastoma (GBM) mouse model which characterize it as a potentially potent, highly-specific anti-GBM therapy.
Status:
Investigational
Source:
INN:gadocoletic acid
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Gadocoletic acid (also Gadoletic acid trisodium salt, or B22956/1) is a magnetic resonance contrast agent. Based on results from animal imaging experiments and pharmacokinetic data it was suggested that gadocoletic acid trisodium salt has strong potential for clinical use in Magnetic Resonance Coronary Angiography and Myocardial Perfusion Imaging. The small molecules of gadocoletic acid are bound after injection to large human serum albumin molecules in coronary vessels with the result of high vessel/muscle contrast. The ability of B229563− (anion) to bind to more than one site on the albumin molecule allows a positive correlation between dose and blood relaxation rate enhancement at doses higher than 0.05 mmol/kg, the dose that produces roughly a total plasma concentration equimolar to the albumin concentration at equilibrium distribution. Gadocoletic acid is thought to be highly efficacious in inversion recovery-prepared 3D gradient-recalled echo, navigator echo-gated coronary angiography in humans already at doses below 0.1 mmol/kg.
Status:
Investigational
Source:
JAN:SODIUM ACENEURAMATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sodium aceneuramate is a sodium salt of aceneuramic acid (sialic acid). It is an effective inhalant expectorant. Inhalation of sodium aceneuramate repaired inflammation in the airway, and caused bronchitic rabbits to produce sputa with a low viscosity, similar to normal air-way secretions. Sodium aceneuramate protected the mucociliary transport impaired bycigarette smoke in a dose-dependent manner. The results suggest that sodium aceneuramate may participate in the defense mechanism in the airway against irritant gases. Sodium aceneuramate inhibited bronchial anaphylaxis and the release of histamine into bronchoalveolar lavages. Sodium aceneuramate has an action which elevates the viscoelasticity of secretions in the respiratory tract.
Status:
Investigational
Source:
NCT00002352: Not Applicable Interventional Completed Cytomegalovirus Infections
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lobucavir is a new anti-cytomegalovirus infection agent, manufactered by Bristol Myers Squibb, Inc. Lobucavir is a cyclobutyl analog of guanine with broad spectrum antiviral activity against most herpes viruses and Hepatitis B. Lobucavir was shown to inhibit herpes simplex virus (HSV) DNA polymerase after phosphorylation by the HSV thymidine kinase. The drug was well tolerated with few side effects. Lobucavir had been in phase III clinical trial for the treatment of Hepatitis B, Herpes simplex virus infections and in phase II for the treatment of Cytomegalovirus infections. All these studies were discontinued.
Status:
Investigational
Source:
NCT00436852: Phase 2 Interventional Completed Disseminated Neuroblastoma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


ABT-751 is an orally bioavailable antimitotic sulfonamide, which binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, leads to a block in the cell cycle at the G2M phase, resulting in cellular apoptosis. ABT-751 had been in phase Ⅱ clinical studies for the treatment of breast cancer; colorectal cancer; non-small cell lung cancer; renal cancer, prostate cancer, but these researches have been discontinued.