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

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Showing 801 - 810 of 12523 results

Status:
Investigational
Source:
INN:demiditraz [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Demiditraz is used in veterinary as acaricide/tick repellant.
Status:
Investigational
Source:
INN:dioxethedrin
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Dioxethedrin is the ephedrine derivative. It is the beta-adrenergic agonist. As a bronchodilator and sympathomimetic agent is was used in antitussive syrup Bexol.
Status:
Investigational
Source:
NCT00952588: Phase 2/Phase 3 Interventional Completed Acute Myeloid Leukemia
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Barasertib (AZD1152) is a dihydrogen phosphate prodrug of a pyrazoloquinazoline Aurora kinase inhibitor [AZD1152–hydroxyquinazoline pyrazol anilide (HQPA)] and is converted rapidly to the active AZD1152-HQPA in plasma. AstraZeneca was developing the aurora kinase inhibitor, barasertib (AZD 1152) as a therapeutic for cancer. AZD1152-HQPA is a highly potent and selective inhibitor of Aurora B (Ki, 0.36nmol/L) compared with Aurora A (Ki, 1,369nmol/L) and has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumour cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis. Barasertib (AZD1152) potently inhibited the growth of human colon, lung, and haematologic tumour xenografts (mean tumour growth inhibition range, 55% to ≥100%; P < 0.05) in immunodeficient mice. Detailed pharmacodynamic analysis in colorectal SW620 tumour-bearing athymic rats treated i.v. with Barasertib (AZD1152) revealed a temporal sequence of phenotypic events in tumours: transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells (>4N DNA, 2.3-fold higher compared with controls). Histologic analysis showed aberrant cell division that was concurrent with an increase in apoptosis in AZD1152-treated tumours. Bone marrow analyses revealed transient myelosuppression with the drug that was fully reversible following cessation of Barasertib (AZD1152) treatment. Barasertib (AZD1152) was in phase III for the treatment of Acute myeloid leukaemia, but later these studies were discontinued.
Status:
Investigational
Source:
INN:acridorex
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Acridorex (BS 7573a) is an anorectic agent.
Status:
Investigational
Source:
INN:oxysonium iodide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:ubisindine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ubisindine is an antitussive, antiarrhythmic agent.
Status:
Investigational
Source:
Cancer. Aug 1993;72(4):1184-91.: Phase 2 Human clinical trial Completed Neoplasm Recurrence, Local/mortality
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00300339: Phase 2 Interventional Completed Intermittent Claudication
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trelanserin, also known as SL-650472, is a serotonin 5-HT2A and 5-HT1B receptors antagonist. It was predicted to be histamine receptor H1 antagonist too. Trelanserin blocked serotonin-induced increases in blood pressure, rate pressure product and circumflex coronary artery flow and reduced serotonin-induced ischemic myocardial segment length shortening. Thus, trelanserin opposes serotonin-induced myocardial dysfunction in a dog model of exercise-induced ischemia. Trelanserin also blocked sumatriptan-induced vasoconstriction in ischemic and normally perfused hindlimbs in dogs.
Status:
Investigational
Source:
INN:imiloxan
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Imiloxan is a highly selective alpha2B adrenoceptor antagonist and was developed for depression in the 1980s. In Phase 1 clinical trials imiloxan dosing led to hypersensitivity reactions; the molecule's development was discontinued.
Status:
Investigational
Source:
NCT00028873: Phase 2 Interventional Completed Breast Cancer
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LANIQUIDAR is a P-glycoprotein inhibitor. It was used in trials studying the treatment of breast cancer.