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

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Showing 621 - 630 of 13408 results

Status:
Investigational
Source:
NCT01348737: Phase 1 Interventional Completed Alzheimer's Disease
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



AZD3839 is a potent and selective BACE1 inhibitor with about 14-fold selectivity over BACE2. In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels and decreases the formation of sAPPβ. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons. AZD3839 causes in vitro BACE1 inhibition in the cell assay with the IC50 value of 16.7 nM. In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation. AZD3839 has been used in phase I clinical trials studying the basic science of Safety and Tolerability. However future development has been discontinued.
Status:
Investigational
Source:
INN:flotegatide (¹⁸F) [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

FLOTEGATIDE F-18, a radiolabelled tripeptide with arginine-glycine-aspartic acid (R-G-D) motif, is a positron emission tomography (PET) tracer targeting integrin alpha-V/beta-3. It was under development as a diagnostic agent for cancer and atherosclerosis.
Status:
Investigational
Source:
NCT01716910: Early Phase 1 Interventional Completed Synbiotics
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Volixibat (SHP626; formerly LUM002) is a potent inhibitor of the apical sodium-dependent bile acid transporter (ASBT) that was developed for the treatment of nonalcoholic steatohepatitis. Volixibat participated in phase II clinical trial to investigate its safety, effectiveness in adults with nonalcoholic steatohepatitis. However, this study was discontinued, without any further explanation for the possible causes. In addition, volixibat was studied in a clinical trial in healthy adults and in patients with type 2 diabetes mellitus, where was shown that the drug was generally well tolerated.
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with potential antineoplastic, anti-inflammatory and antiangiogenic activities. Pexmetinib inhibited leukemic proliferation, prevented activation of downstream effector kinases and abrogated the effects of TNF-alpha on healthy hematopoietic stem cells. In ex vivo stimulated human whole blood, LPS-induced cytokines was inhibited by Pexmetinib with an IC50 value ranging from 50-120 nM. ARRY-614 inhibited the release of IL-6 from SEA- or LPS-challenged mice with an ED50 value less than 10 mg/kg. Combining Pexmetinib with lenalidomide inhibited both pro-inflammatory cytokines and tumor growth in vivo with higher potency, compared with either agent alone. In dose escalation or expansion cohorts, treatment with Pexmetinib either once daily or twice daily was applied to forty-five patients. Pexmetinib reduced the levels of circulating biomarkers and the p38 MAPK activation of bone marrow.
Status:
Investigational
Source:
INN:teplinovivint [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03801889: Phase 2 Interventional Withdrawn Iron Overload
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



SP-420 is iron chelator developed by University Of Florida Research Foundation for the treatment of iron overload disease
Status:
Investigational
Source:
INN:milataxel [INN]
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.