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

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Showing 2541 - 2550 of 34988 results

Status:
Investigational
Source:
NCT00606697: Phase 2 Interventional Completed Sleep Initiation and Maintenance Disorders
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Vofopitant (previously known as GR205171), a tetrazole-derivative, was developed as a neurokinin1 receptor antagonist. Vofopitant was studied in clinical trials phase II for the treatment of primary insomnia and posttraumatic stress disorder. However, these studies were discontinued due to lack of effectiveness. In addition, vofopitant participated in phase I for patients with bipolar disorder. However, this study was terminated because of the slow recruitment; trial unlikely to reach completion.
Status:
Investigational
Source:
INN:melquinast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Melquinast is an antiasthmatic, antiallergic substance not acting primarily as antihistamines.
Ruboxistaurin is an orally bioavailable, selective, potent inhibitor of protein kinase C β developed for treating diabetic retinopathy. In vitro and in vivo non-clinical models have demonstrated that Ruboxistaurin decreases PKC β activity and ameliorates many of the effects of PKC β on pathologic processes in the retina. Ruboxistaurin prevents the slowing of retinal blood flow that is observed by fluorescein video angiography in the eyes of diabetic rats. It is also reported to cause regression of retinal neovascularization produced by laser-induced major branch vein occlusions in a porcine model. Ruboxistaurin positively affected the diabetes-induced retinal blood flow abnormalities in a Phase Ib study in diabetic patients. Ruboxistaurin is in phase III clinical trials for the treatment of diabetic nephropathy and diabetic macular edema. Eli Lilly had submitted Ruboxistaurin for approval in the US and the EU; however, the company subsequently discontinued development as it was unable to demonstrate sufficient efficacy
Status:
Investigational
Source:
INN:etibendazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Etibendazole (R34803 or methyl [5-(2-(4-fluorophenyl)-1,3-dioxolan-2-yl)-1H-benzimidazole-2-yl] carbamate), a benzimidazole derivative, is a microtubule inhibitor. Etibendazole exerts antihelmintic activity.
Status:
Investigational
Source:
NCT00743925: Phase 2 Interventional Completed Acute Coronary Syndrome
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.
Status:
Investigational
Source:
NCT00514501: Phase 2 Interventional Completed Acute Coronary Syndrome
(2007)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Iodofiltic Acid I-123 is a single-photon branching free fatty acid radiopharmaceutical with potential application in single-photon emission computed tomography (SPECT). Assessment of fatty acid metabolism by radionuclide techniques has a potential role for the early detection of myocardial ischaemia and the assessment of the severity of ischaemic heart disease. The Iodofiltic Acid I-123 scan is preferable because it can provide suitable information for risk stratification just after an acute myocardial infarction (AMI) without requiring the patient to exercise; it can also detect previous ischaemic insult even after recovery of myocardial perfusion, the so- called "ischaemic memory".
Status:
Investigational
Source:
INN:isalsteine
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

ISALSTEINE is a mucolytic agent.
Status:
Investigational
Source:
INN:isoxaprolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

ISOXAPROLOL is a potent beta-adrenoceptor antagonist with antihypertensive properties. It was effective in lowering blood pressure in acute trials on spontaneously hypertensive rats at a dosage of 15 mg/kg.
Status:
Investigational
Source:
INN:pentorex
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Pentorex (Modatrop) is phenylisopropylamine derivative. It is a central adrenergic stimulant drug related to phentermine, which is used as an anorectic to assist with weight loss. Pentorex is sympathomimetic agent.
Status:
Investigational
Source:
NCT00598507: Phase 2 Interventional Completed Melanoma
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sagopilone (BAY86-5302; ZK 219477; ZK-EPO) is a synthetic epothilone, an analog of patupilone that was developed by Bayer HealthCare as an anticancer agent. Epothilones are 16-member ring macrolides have demonstrated potent antiproliferative activity in several different multidrug-resistant and paclitaxel-resistant tumor cell lines in vitro and in vivo. Sagopilone binds to tubulin and induces microtubule polymerization, which may result in the induction of G2/M arrest, and apoptosis. Sagopilone is not a substrate for the P-glycoprotein efflux pump and so may exhibit activity in multidrug-resistant tumors. This drug was studied in clinical trials phase II in patients with recurrent ovarian cancer, in metastatic melanoma patients, for the treatment of advanced stage breast cancer and in the treatment of Glioblastoma patients. However, the development of this drug was discontinued, because of its adverse effects, including peripheral neuropathy.

Showing 2541 - 2550 of 34988 results