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

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Showing 781 - 790 of 8093 results

Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.
Status:
Investigational
Source:
INN:ciclazindol [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Ciclazindol is an indole derivative and monoamine uptake inhibitor patented by pharmaceutical company John Wyeth and Brother Ltd. as an antidepressant. Besides that, Ciclazindol is effective anorectic agent, inducing weight loss in rats and man. Ciclazindol was shown to inhibit ATP-sensitive K+ (K(ATP)) channel currents and stimulate insulin secretion from CRI-G1 insulin-secreting cells. The inhibition of KATP channel currents by ciclazindol is unaffected by the removal of intracellular Mg2+ ions and after trypsinization of the cytoplasmic surface of excised patches, treatments known to abolish sulphonylurea sensitivity.
Status:
Investigational
Source:
INN:ciprefadol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ciprefadol is an opioid analgesic drug. It binds with a high affinity to mu (Ki 4.2 nM) and kappa (Ki 2.5 nM) opioid receptors. In vivo, ciprefadol displays mixed antagonist/agonist activity in the mouse writhing and the rat tail heat tests: in low doses, the compound inhibits the analgesic effect of morphine, while at higher doses it displays analgesic effect. Chronic administration of ciprefadol to rhesus monkeys produced a marked physical dependence more severe than that of morphine, and its effect was consistent with what would be expected of a potent, long-lasting morphine-like agonist.
Status:
Investigational
Source:
INN:naxaprostene
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naxaprostene (CG 4305) is a prostacyclin analogue, which causes concentration dependent inhibition of thrombocyte function. Naxaprostene is more selective for IP receptors and tends towards partial agonism. Naxaprostene prevented thrombotic arterial occlusion in rabbits.
Status:
Investigational
Source:
INN:butilfenin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Butilfenin is N-substituted iminodiacetic acid derivative that was studied as tridentate ligand to form a technetium-99m complex.
Status:
Investigational
Source:
INN:metaterol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Metaterol is a beta-adrenoceptor agonist. It exerts sympathomimetic and broncholytic properties.
Status:
Investigational
Source:
INN:diacetamate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Diacetamate (Acetaminophen Acetate, Acetaminophen Impurity, diacetyl-p-aminophenol) is a acetaminophen synthetic impurity. Acetaminophen-aspirin mixtures have lower stability due to acetylation of the former by the latter, producing diacetyl-p-aminophenol.
Status:
Investigational
Source:
NCT00538343: Phase 2 Interventional Terminated Brain Metastases
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Berubicin, an anthracycline derivative, is a DNA binding agent and potent topoisomerase II poison. Reata Pharmaceuticals were developing it as a treatment for brain cancer as it can breach the blood-brain barrier. It had also been in early clinical trials for the treatment of lung cancer and malignant gliomas. However, studies have been terminated. In October 2006, it was granted orphan drug designation from the FDA for the treatment of malignant gliomas. According to a CNS Pharmaceuticals media release in April 2018, berubicin will be studied for glioblastoma patients, these investigations will be funded in part by an equity crowdfunding campaign.
Status:
Investigational
Source:
NCT00389792: Phase 2 Interventional Completed Atrial Fibrillation
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Budiodarone is a chemical analog of amiodarone with mixed ion channel electrophysiological activity. Budiodarone was developed to capitalize on the proven efficacy of amiodarone and to avoid its side effects. Budiodarone has a short plasma half-life (7 h) and a lower volume of distribution (13 L/kg). It is cleared from the body in 48 h. Like amiodarone, Budiodarone has balanced, multiple cardiac ion channel inhibiting activity, giving it properties of all four Vaughan Williams antiarrhythmic drug classes. Budiodarone, unlike amiodarone, undergoes rapid metabolism by plasma and tissue esterases. In clinical trials, Budiodarone effectively reduces the number and duration of atrial tachycardia/atrial fibrillation episodes.
Status:
Investigational
Source:
INN:edifolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Edifolone (SC-35135) is a structurally unique class Ia antiarrhythmic agent. It acts as a sodium channel antagonist. Edifolone development has been discontinued.