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

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Showing 671 - 680 of 14117 results

Status:
Investigational
Source:
NCT00063219: Phase 2 Interventional Completed Carcinoma, Non-Small-Cell Lung
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Milataxel, a taxane that binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization. Milataxel has completed phase II clinical trials for non-small cell lung cancer patients, and for colorectal cancer patients. Besides, it was studied for malignant mesothelioma. However, the drug has been discontinued due to toxicity issues at the dose level of 35 mg/m 2.
Status:
Investigational
Source:
NCT02648178: Not Applicable Interventional Completed Nicotine Dependence, Other Tobacco Product
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01638403: Phase 3 Interventional Completed Treatment of Excessive Daytime Sleepiness in Narcolepsy
(2010)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Diclobutrazol is the active ingredient of a broad-spectrum systemic fungicide for use on cereals. Diclobutrazol sprays appear promising for the control of coffee rust, apple mildew and scab, grape powdery mildew and various other crop diseases. Diclobutrazol has a systemic action and is translocated mainly acropetally. It eradicative action, increased by vapour effect, is very strong. Diclobutrazol is of low toxicity to mammals and other animals. It is also of low toxicity to birds, fish and invertebrates. Diclobutrazol inhibited spore germination and mycelia growth of a wide range of fungi. Stereoselective inhibition of human CYP3A4 and Candida albicans CYP51 was observed with enantiomers of the azole antifungal compound diclobutrazol. The RR(+) configuration at its asymmetric carbon center was most active.
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:
NCT01460420: Phase 1/Phase 2 Interventional Completed Hematologic Malignancies
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

(±)-quinuclidinyl benzilate (3-quinuclidinyl benzilate), is a specific muscarinic cholinergic receptor antagonist. It binds potently but reversibly to the muscarinic cholinergic receptors of mammalian brain and peripheral tissues. 3-quinuclidinyl benzilate was invented by Hoffmann-La Roche Inc in 1951, while investigating antispasmodic agents resembling tropine for the treatment of gastrointestinal conditions. In the 1960s 3-quinuclidinyl benzilate, was developed and weaponized as a new chemical agent for battlefield use as a psychochemical. Assigned the NATO code BZ it is classified as a hallucinogenic chemical warfare agent that affects both the peripheral and central nervous systems (CNS). It is one of the most potent anticholinergic psychomimetics known, with only small doses necessary to produce incapacitation. The primary route of absorption is through the respiratory system but absorption also can occur through the skin or gastrointestinal tract. BZ is odorless and is usually disseminated as an aerosol. Data regarding the health effects of BZ in humans following inhalation exposure are limited to military application studies. Pharmacologic activity of 3-quinuclidinyl benzilate is similar to other anticholinergic drugs (eg, atropine) but with a much longer duration of action. It was shown that I[3H]-3-quinuclidinyl benzilate accumulated in various brain regions after intravenous injection. The specific binding of [3-3H]3-quinuclidinyl-benzilate and [125I]3-quinuclidinyl-(3-iodo-4-hydroxy-benzilate) to rat brain subcellular fractions is parallel in myelin, synaptic plasma membrane and mitochondrial fractions with a 3-4-fold enrichment observed in synaptic plasma membrane over crude mitochondrial fractions. These findings suggested the use of 3-quinuclidinyl benzilate as a binding probe useful in assaying low levels of muscarinic receptor in tissue culture and other biological sources including labeling the receptor in vivo for autoradiographic studies. M2 muscarinic acetylcholine receptor (M2 receptor), essential for the physiologic control of cardiovascular function through activation of G protein-coupled inwardly-rectifying potassium channels, was shown to bind 3-quinuclidinyl benzilate with high affinity in vitro.
Status:
Investigational
Source:
NCT00095797: Phase 1 Interventional Completed Adult Acute Basophilic Leukemia
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



XK-469 (2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]-propionic acid) is a novel synthetic quinoxaline phenoxypropionic acid derivative. The R-isomer of XK-469 was approximately twice as effective as the S-isomer of XK-469R. R( )-isomers induce reversible protein DNA crosslinks in mammalian cells. It acts as a selective topoisomerase IIβ inhibitor. A phase I study was performed to determine the safety and pharmacokinetics of XK-469, (R)- in patients with various neoplasms.
Status:
Investigational
Source:
NCT04434937: Phase 2 Interventional Completed Lymphoma
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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:
NCT00815763: Phase 3 Interventional Completed Ischemic Stroke
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT01440517: Phase 2 Interventional Terminated Diabetes Mellitus
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Maraciclatide Tc-99m is radiolabelled with technetium 99m cyclic peptide maraciclatide (NC100692 or diamine dioxime-Lys-Cys-Arg-Gly-Asp-Cyc-Phe-Cys-polyethylene glycol). Maraciclatide Tc-99m binds vitronectin receptors (αvβ3 and αvβ5 integrins) with high affinity. Maraciclatide Tc-99m is used in single-photon emission computed tomography (SPECT) imaging of vitronectin receptors that are upregulated and expressed preferentially on proliferating endothelial cells. Maraciclatide Tc-99m is being developed as a diagnostic agent to determine neoplasia and cardiovascular diseases.