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

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Showing 1091 - 1100 of 10251 results

Status:
Investigational
Source:
INN:nabazenil
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Nabazenil is a synthetic cannabinoid receptor agonist, which has anticonvulsant properties. Nabazenil was undergoing preclinical trials with HG Pars in the USA.
Status:
Investigational
Source:
NCT00640523: Phase 2 Interventional Completed Chronic Lymphocytic Leukemia (CLL)
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Forodesine hydrochloride is the salt of the synthetic high-affinity transition-state analog forodesine (BCX-1777, immucillin-H), a substrate designed to mimic the properties or the geometry of the transition state of reaction. It is an anticancer drug that has been developed for the treatment of different hematologic malignancies. In December 2006, orphan designation (EU/3/06/421) was granted by the European Commission to Napp Pharmaceuticals Research Limited, United Kingdom, for forodesine hydrochloride for the treatment of acute lymphoblastic leukemia. Forodesine hydrochloride has been evaluated in Phase I/Phase II clinical trials for several cancer types including chronic lymphocytic leukemia (CLL), B-Cell acute lymphoblastic leukemia and refractory cutaneous T-cell lymphoma (CTCL). Forodesine is a potent purine nucleoside phosphorylase (PNP) inhibitor that acts by elevating plasma 2'-deoxyguanosine (dGuo) and intracellular deoxyguanosine triphosphate, which in turn affects deoxynucleotide-triphosphate pools and induces cell death by apoptosis. Forodesine in the presence of dGuo inhibited the proliferation of CEM-SS (T-acute lymphoblastic leukemia) cells with an IC50 of 0.015 uM. This inhibition by forodesine and dGuo was accompanied by a 154-fold and 8-fold elevation of endogenous dGuo triphosphate (dGTP) and deoxyadenosine triphosphate (dATP) pools, respectively. Cytotoxic activity of forodesine in the presence of dGuo was selective to T lymphocytes. It is a 10- to 100-fold more potent inhibitor of human lymphocyte proliferation than other known PNP inhibitors such as PD141955 and BCX-34.8
Status:
Investigational
Source:
INN:filenadol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FILENADOL is an analgesic drug with antinociceptive and anti-inflammatory properties. It reduces the hyperalgesic effects of inflammatory mediators besides inhibiting partially the synthesis of eicosanoids.
Status:
Investigational
Source:
NCT00277810: Phase 2/Phase 3 Interventional Completed Alzheimer Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LECOZOTAN, a benzodioxanylpiperazine derivative, is a selective serotonin 1A receptor antagonist. It was in development for the symptomatic treatment of cognitive deficits in Alzheimer's disease.
Status:
Investigational
Source:
NCT00082368: Phase 2 Interventional Completed Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tariquidar, a non-competitive, specific P-glycoprotein (Pgp) inhibitor, is an anthranilamide derivative with multidrug resistance properties. Tariquidar binds to the ATP-binding cassette (ABC) transport protein Pgp, thereby inhibiting transmembrane transport of anticancer drugs resulting in their increased intracellular concentrations augmenting cytotoxicity of an anticancer drug. Tariquidar was discovered by Xenova Group and was developed for the treatment of multidrug resistance in cancer. In October 2002 the US Food and Drug Administration (FDA) has granted fast track review status to tariquidar for the treatment of multi-drug resistance in first-line treatment of non-small cell lung cancer (NSCLC) patients. Tariquidar is still undergoing research as an adjuvant against multidrug resistance in cancer.
Status:
Investigational
Source:
USAN:Azamethiphos
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Azamethiphos, an organothiophosphate insecticide, initially was used in 1991 for the treatment against sea lice. However, because of reduced sensitivity in 1999, the use of this compound was terminated. Azamethiphos was re-introduced in 2008; it’s the main component of Salmosan, a pesticide presently used for treatment against sea lice. Salmosan is applied as a bath treatment and then released into the surrounding seawater
Status:
Investigational
Source:
NCT03345095: Phase 3 Interventional Completed Newly Diagnosed Glioblastoma
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Marizomib is a natural beta-lactone produced by the marine bacterium Salinispora tropica. Marizomib has a broad inhibition profile for the 20S proteasome and has been shown to inhibit the CT-L (beta5) CT-T-laspase-like (C-L, beta1) and trypsin-like (T-L, beta2) activities of the 20S proteasome. The drug is being tested in phase II clinical trials for the treatment of Multiple Myeloma and Malignant Glioma and in phase I in patients with Non-small Cell Lung Cancer, Pancreatic Cancer, Melanoma or Lymphoma
Patamostat (E-3123) is a protease inhibitor in vivo and in vitro. Inhibitory activity was shown toward trypsin, thrombin, plasmin, cathepsin-B and kallikrein. Patamostat is effective toward experimental pancreatitis and disseminated intravascular coagulation (animal models).
Status:
Investigational
Source:
INN:ocinaplon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ocinaplon is anxiolytic in rodents and primates, including humans, with a magnitude of effect comparable to benzodiazepines. It was evaluated to treat Generalised anxiety disorder. The mechanism of action by which ocinaplon produces its anxiolytic effects is by allosteric modulating of GABA-A receptors. The serious adverse event detected in the ocinaplon group was icterus following transaminase elevations. Due to liver complications that occurred in Phase III, development of ocinaplon is discontinued.
Status:
Investigational
Source:
INN:sulbenox
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Sulbenox is substituted tetrahydrobenzothiophene derivative patented by American Cyanamid Co as the animal growth-promoting agent. In preclinical studies, Sulbenox found to be an effective growth promoter in sheep, mice, and rats.

Showing 1091 - 1100 of 10251 results