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

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Showing 731 - 740 of 13268 results

Status:
Investigational
Source:
INN:trethinium tosilate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Trethinium is tetrahydroisoquinoline derivative. It is an antihypertensive agent.
Status:
Investigational
Source:
NCT01901341: Phase 3 Interventional Terminated Opioid-Induced Constipation
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Bevenopran (also known as CB-5945), a peripherally acting mu-opioid receptor antagonist that was studied for the treatment of opioid-induced constipation. Due to difficulties with enrollment, phase III of clinical trials were terminated early.
Status:
Investigational
Source:
INN:tandamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tandamine was developed as a selective serotonin reuptake inhibitor for the treatment of depression. Tandamine participated in clinical trials in hospitalized depressed patients, where it showed that the well-tolerated drug could be of some benefit for retarded depressions. In addition, was found in human volunteers, that tandamine possessed significant anticholinergic activity, to reduce appetite and to produce sedation. However, this drug has never been marketed.
Status:
Investigational
Source:
INN:broparestrol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Broparestrol, (Z)- is an isomer of Broparestrol -- synthetic, nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that has been used in Europe as a dermatological agent and for the treatment of breast cancer. Broparestrol, (Z)- and Broparestrol, (E)- demonstrates antiestrogenic activity but, unlike broparestrol, were never marketed.
Status:
Investigational
Source:
NCT04450602: Not Applicable Interventional Completed Androgenetic Alopecia
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01359696: Phase 1 Interventional Completed Solid Tumor
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01966679: Phase 2 Interventional Completed Autism Spectrum Disorder
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02098278: Phase 2 Interventional Completed Lipoprotein Lipase Deficiency, Familial
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01020799: Phase 2 Interventional Completed Major Depressive Disorder
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02465060: Phase 2 Interventional Active, not recruiting Advanced Lymphoma
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AZD-4547 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival. AZD-4547 is a selective FGFR inhibitor targeting FGFR1/2/3 with IC50 of 0.2 nM/2.5 nM/1.8 nM in cell-free assays, weaker activity against FGFR4, VEGFR2 (KDR), and little activity observed against IGFR, CDK2, and p38. Compared to FGFR1-3, AZD-4547 displays weaker activity against FGFR4 with IC50 of 165 nM. AZD-4547 only inhibits recombinant VEGFR2 (KDR) kinase activity with IC50 of 24 nM, in the in vitro selectivity test against a diverse panel of representative human kinases. AZD-4547 is under clinical investigation for the treatment of FGFR-dependent tumors. It is in phase II clinical studies for the treatment of breast cancer; gastric cancer; lung cancer; oesophageal cancer and in phase II/III clinical studies for the treatment of non-small cell lung cancer.