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

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Showing 11411 - 11420 of 13268 results

Status:
Investigational
Source:
INN:propanocaine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Propanocaine is a benzyl alcohol derivative with local anesthetics activity
Status:
Investigational
Source:
INN:fotemustine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

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:pentacynium chloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pentacynium bis-methylsulphate (presidal) is a salt of pentacynium, which was studied as a ganglion-blocking agent to treat hypertension. Glaxo Wellcome developed this drug; however, information about the further use of pentacynium is not available.
Status:
Investigational
Source:
NCT00832546: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
Status:
Investigational
Source:
INN:bifepramide [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Bifepramide, (+)- belong to the class of parasympatholytic agents that reduce the activity of the parasympathetic nervous system.
Status:
Investigational
Source:
NCT03570931: Phase 2/Phase 3 Interventional Active, not recruiting Infantile Neuroaxonal Dystrophy
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:norboletone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Norbolethone is a 19-nor anabolic steroid first synthesized in 1966. During the 1960s it was administered to humans in efficacy studies concerned with short stature and underweight conditions. It has never been reported by doping control laboratories prior to 2001. Norbolethone matches the description for what is described as a "designer steroid. " In fact, Norbolethone was given in clinical trials over 30 years ago and never given the green light. No supply was ever manufactured, and no test was ever developed to detect this substance, yet ironically, it was suspected of being used in the 2000 Olympics based on blood and urine assays done by the IOC. Norbolethone was used in the treatment of idiopathic underweight, prevention of indomethacin-induced intestinal ulcers.
Status:
Investigational
Source:
INN:alphamethadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Alphamethadol is a synthetic opioid analgesic. Alphamethadol is composed of two isomers itself, L-α-methadol, and D-α-methadol. L-α-methadol is an important active metabolite of levacetylmethadol (LAAM), a medication therapy for individuals addicted to opiates that provides an alternative to methadone. Isomers of Alphamethadol bind to and activate the μ-opioid receptor; they are active as opioid analgesics.
Status:
Investigational
Source:
INN:namoxyrate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Xenbucin is an antihyperlipidemic agent. Information about the current use of this agent is not available.

Showing 11411 - 11420 of 13268 results