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

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Showing 431 - 440 of 11247 results

Status:
Investigational
Source:
NCT04017546: Phase 1 Interventional Completed AML
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03678610: Not Applicable Interventional Completed Infertility
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ionomycin is an ionophore produced by the bacterium Streptomyces conglobatus. The molecules act as a motile Ca2+ carrier and enhances Ca2+ influx by direct stimulation of store-regulated cation entry across biological membranes. It is highly specific for divalent cations. Ion selectivity is as follows: Ca2+ > Mg2+ >> Sr2+ = Ba2+ Binding of Sr2+ and Ba2+ is insignificant and binding to monovalent cations or rubidium is negligible. La2+ is also bound to some extent. Complexation with a cation is always in a 1:1 stoichiometry and pH-dependent. Essentially no binding of Ca2+ occurs below pH 7.0 and maximum binding takes place at pH 9.5. At the micromolar level, ionomycin can activate Ca2+/Calmodulin dependent kinase and phosphatase to stimulate gene expression. Ionomycin has been shown to induce central demyelination, inhibit adrenal bovine TREK-1 channels, and to regulate cell division of mature human B cells [1]. It is used to study the effects of calcium flux on endoplasmic reticulum (ER) stress, mitochodrial stress and intrinsic apoptosis mechanisms. It is also used to stimulate the intracellular production of the cytokines, interferon, perforin, IL-2, and IL-4 usually in conjunction with PMA.
Status:
Investigational
Source:
NCT03041116: Phase 3 Interventional Terminated Pantothenate Kinase-Associated Neurodegeneration
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Phosphopantothenic acid is an amidoalkyl phosphate that is the 4-phosphate derivative of (R)-pantothenic acid. Phosphopantothenic acid is not permeable to cell membranes due to its anionic character, consistent with the observation that systemic administration of Phosphopantothenic acid does not restore CoA levels in cellular and mouse models
Status:
Investigational
Source:
NCT02117258: Phase 2 Interventional Completed Metastatic Pancreatic Adenocarcinoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nastorazepide (Z-360) is a selective, orally available, gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. It is currently under development as a therapeutic drug for pancreatic cancer, gastroesophageal reflux disease and peptic ulcers. The most commonly reported adverse events were nausea, abdominal pain, vomiting and fatigue.
Motesanib (AMG 706), a novel nicotinamide, was identified as a potent, orally bioavailable inhibitor of the VEGFR1/Flt1, VEGFR2/kinase domain receptor/Flk-1, VEGFR3/Flt4 and Kit receptors. Motesanib was expected to reduce vascular permeability and blood flow in human tumours. A phase III trial of motesanib in combination with paclitaxel and carboplatin in non-squamous NSCLC has been terminated by Takeda and subsequently the development was discontinued. Motesanib has also been investigated up to phase II in breast, thyroid, colorectal and gastrointestinal stromal tumours. However, development has been discontinued in these indications.
Status:
Investigational
Source:
NCT01052012: Phase 3 Interventional Completed Postoperative Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lambda-cyhalothrin (λ-cyhalothrin), a mixture of isomers of cyhalothrin belongs to a class of insecticides known as synthetic pyrethroids. Synthetic pyrethroids are often preferred to the real thing as an active ingredient because they offer the added bonus of remaining effective for longer period. λ-cyhalothrin was the most commonly used pyrethroid insecticide for vegetable farming in Benin. Experiments have shown that λ-cyhalothrin residues in lettuce and cabbage from farms and markets in Parakou and Cotonou were relatively safe for consumption.
Status:
Investigational
Source:
NCT00773929: Phase 1 Interventional Completed Solid Tumors
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor 2 (VEGFR2) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity. TAK-593 selectively binds to and inhibits VEGFR and PDGFR, which may result in the inhibition of angiogenesis and tumor cell proliferation. It was in the phase I of clinical trial in subjects with nonhematologic advanced cancer and it was discontinued.
Status:
Investigational
Source:
NCT03098797: Phase 2/Phase 3 Interventional Completed Barth Syndrome
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Elamipretide or SS-31 (D-Arg-2', 6'-dimethyltyrosine-Lys-Phe-NH2) is a mitochondria-targeted antioxidant. Elamipretide, is a peptide compound that readily penetrates cell membranes, and targets the inner mitochondrial membrane where it binds reversibly to cardiolipin. In preclinical or clinical studies, elamipretide increases mitochondrial respiration, improves the electron transport chain function and ATP production and reduces formation of pathogenic ROS levels. This elamipretide-cardiolipin association has been shown to normalize the structure of the inner mitochondrial membrane, thereby improving mitochondrial function. Functional benefit is achieved through improvement of ATP production and interruption and potential reversal of damaging oxidative stress. Stealth BioTherapeutics is investigating elamipretide in late stage clinical studies in three primary mitochondrial diseases—primary mitochondrial myopathy, Barth syndrome and Leber’s hereditary optic neuropathy – as well as an earlier stage clinical study in dry age-related macular degeneration.
Status:
Investigational
Source:
NCT02929862: Phase 1/Phase 2 Interventional Completed Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02295865: Phase 2 Interventional Completed Psoriasis
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Toreforant (JNJ-38518168) is an orally active, selective histamine H4 receptor antagonist. Toreforant was investigated as an agent for the treatment of active rheumatoid arthritis. While some improvement in rheumatoid arthritis signs/symptoms through week 12 was observed in the phase IIa study, no efficacy was observed with toreforant at lower doses in a subsequent phase IIb study. Toreforant has been tested in clinical studies in patients with asthma and psoriasis. Toreforant failed to provide therapeutic benefit in population of patients with uncontrolled, eosinophilic, persistent asthma. Toreforant efficacy at 30 and 60 mg was greater than placebo but did not meet predefined success criterion in patients with moderate-to-severe psoriasis.