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

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Showing 851 - 860 of 13501 results

Status:
Investigational
Source:
INN:pobilukast
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pobilukast is the Leukotriene D4 receptor antagonist. Pobilukast significantly attenuated the Salmonella enteritidis endotoxin-induced thrombocytopenia but had no effect on either the endotoxin-induced early leukopenia or late leukocytosis. Additionally, Pobilukast significantly reduced the endotoxin-induced hemoconcentration and improved survival to 30% at 48 hr. Pobilukast dose-dependently inhibited the immediate hemodynamic changes after leukotriene D4 (LTD4) injections. Pobilukast also attenuated the increase in vascular permeability and the prolonged decrease in CO, suggesting that the observed cardiac and vascular effects of LTs were mediated by stimulation of LT receptors. A shift toward the right of the dose-response curves to histamine with pobilukast compared to that with placebo in three subjects was demonstrated, whereas the active compound did not exhibit any protective effect against histamine in the remaining nine subjects. It was concluded that there is a leukotriene component to the bronchial responses to histamine in some, but not all, subjects. Pobilukast had been in phase II clinical trial for the treatment of asthma. However, this development was discontinued.
Status:
Investigational
Source:
NCT04500132: Phase 2 Interventional Completed COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

EC-18 (now known as mosedipimod), a synthetic copy of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) that was developed by Enzychem Lifescience for oral administration for the treatment of immune and inflammatory related diseases, including psoriasis, rheumatoid arthritis, asthma, atopic dermatitis, and sepsis. The US Food and Drug Administration (FDA) has granted Orphan Drug Designation to EC-18 for the treatment of Acute Radiation Syndrome (ARS) and for the for the neutropenia treatment. Besides, the EC-18 is participating in phase II clinical trials to investigate the efficacy and safety of the agent for chemoradiation-induced oral mucositis and chemotherapy-induced neutropenia. This drug has a multimodal mechanism of action. It stimulates calcium influx into T lymphocytes and increases the production of various cytokines. In addition, EC-18 enhances the cytolytic activity of natural killer (NK) cells and suppresses the expression of the transmembrane protein tumor cell toll-like receptor 4 (TLR-4) on cancer cells, thus suppresses tumor cell proliferation.
Status:
Investigational
Source:
INN:parvaquone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Parvaquone, an antitheilerial compound that was developed for the treatment of East Coast fever. Experiments on animals have shown that this drug was effective in the treatment of cattle infected with Theileria annulata.
Status:
Investigational
Source:
JAN:LANPERISONE HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Lanperisone (NK433) is muscle relaxant. It acts by blocking voltage-gated sodium channels.
Status:
Investigational
Source:
INN:nitroclofene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nitroclofene is an anthelminthic drug. Nitroclofene is a selective inhibitor of the fumarate reductase system of the adult liver fluke at a concentration of 4 umol/L. The enzyme plays an important role in the process of energy utilization. Consequently, it possesses good flukicidal activity against both Fasciola hepatica and F. gigantica.
Status:
Investigational
Source:
NCT00999284: Phase 1 Interventional Completed Visual Acuity
(1996)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



ZK 200775, also known as fanapanel, an antagonist at the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor, possesses neuroprotective efficacy in patients with acute ischemic stroke. However, the phase II of clinical trials had revealed, that this compound had led to the neuronal dysfunction and the glial cell toxicity had occurred. In addition, was shown, that the antagonization of AMPA receptors by ZK200775 lead to alterations of color and dark vision, visual acuity, cone electroretinogram (ERG) modalities and the pattern-reversal visual evoked potentials and to a lesser extent on the scotopic ERG. At the same time, ZK 200775 did not alter eye morphology, the functioning of the extraocular muscles, binocular vision, visual fields or the pupil.
Status:
Investigational
Source:
NCT02088645: Phase 1 Interventional Active, not recruiting Thyroid Cancer, Medullary
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Perafensine is an isoquinoline derivative shown to be active in tests predictive of antidepressant activity. Perafensine is a potent antagonist of reserpine-induced effects and inhibits norepinephrine uptake into rat hypothalamic synaptosomes. Perafensine induced the biosynthesis of microsomal drug-metabolizing enzymes – in treated rats methylayapanine O-demethylase, ethoxycoumarin O-deethylase and cytochrome P-450 contents were increased and ketamine N-demethylase was decreased.
Status:
Investigational
Source:
INN:pelrinone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Pelrinone, a cardiotonic drug, is a phosphodiesterase III inhibitor that was studied in clinical trials phase II for the treatment of patients with heart failure.
Status:
Investigational
Source:
INN:bromebric acid [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bromebric Acid (Cytembena) is a derivative of bromoacrylic acid with cytostatic and antineoplastic activity. Chemical structure of Bromebric Acid is not related to any previous antineoplastic agent. In animal tumor screens, Jelinek and Semonsky noted antineoplastic activity of Cytembena against sarcoma 180, atlenocarcinoina of the lactic gland in mice, Ehrlich’s ascitic carcinoma, Yoshida’s ascitic sarcoma, and Zojdeln’s heap