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Restrict the search for
vitamin a
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Status:
Investigational
Source:
NCT02542787: Phase 2 Interventional Completed Spasticity in People With Multiple Sclerosis
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Status:
Investigational
Source:
NCT00150397: Phase 2 Interventional Completed Asthma
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tofimilast is a potent phosphodiesterase-4 (PDE4) inhibitor with low oral bioavailability and no emesis-associated behaviors in ferrets at plasma concentrations up to 152 ng/ml. Tofimilast exhibited an apparent slower absorption through the rat lung after administration as a dry powder, although absorption half-life values were <1 h and therefore the significance of a formulation effect for this compound is questionable. Tofimilast was tested as a therapeutic agent against asthma and chronic obstructive pulmonary disease but development has been discontinued due to lack of efficacy.
Status:
Investigational
Source:
NCT03920254: Phase 2/Phase 3 Interventional Terminated Ulcerative Colitis (UC)
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01806675: Phase 1/Phase 2 Interventional Completed Adult Giant Cell Glioblastoma
(2013)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Status:
Investigational
Source:
NCT02089061: Phase 1 Interventional Completed Acute Coronary Syndromes
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Bristol-Myers Squibb developed BMS-919373, a selective IKur inhibitor for use in atrial fibrillation, acute coronary syndromes, and paroxysmal atrial fibrillation. IKur is a repolarizing K+ current encoded by the KCNA5 gene and is expressed predominantly in the atrium of human. IKur is a potential atrial-selective target for the treatment of atrial fibrillation. BMS-919373 participated in phase II clinical trials to evaluate the effect on atrial fibrillation burden in patients with paroxysmal atrial fibrillation. In addition, in phase I clinical trials for patients with acute coronary syndromes. However, further, developments have been discontinued.
Status:
Investigational
Source:
INN:asengeprast [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02326441: Phase 1 Interventional Completed Advance Malignancies
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
KX-02 is a compound demonstrating dual inhibitory activity against Src kinase and tubulin polymerization. It readily crosses the blood-brain-barrier in mice. It is under development for the treatment of solid tumors.
Status:
Investigational
Source:
NCT04576793: Phase 2 Interventional Recruiting Alzheimer Disease
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT03013998: Phase 1/Phase 2 Interventional Recruiting Previously Untreated Relapsed Refractory Acute Myeloid Leukemia
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
HCI-2084 (wider known as TP-0903) is developing by Tolero Pharmaceuticals for the treatment of different cancers. HCI-2084 is a small molecule AXL receptor tyrosine kinase (RTK) inhibitor. AXL is involved in maintaining a mesenchymal phenotype in cancer cells that enhanced cell survival in stressed environments, and increased resistance to targeted therapies compared to epithelial cells. AXL overexpression has been observed in multiple tumor types that have acquired resistance to various agents. TP-0903 is participating in phase I/II clinical trial in patients with previously treated chronic lymphocytic leukemia (CLL). This study will investigate the safety, pharmacokinetics, pharmacodynamics, and clinical activity of TP-0903. Besides, phase I is currently being conducted in patients with advanced solid tumors in the presence of TP-0903. In addition, TP-0903 was investigated in neuroblastoma (NB) cells, where this drug makes NB cells more vulnerable to the conventional chemotherapeutics.
Status:
Investigational
Source:
NCT02082977: Phase 1 Interventional Terminated Cancer
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma. EZH2 inactivation by GSK126 is also effective in killing MM cells and CSCs as a single agent or in combination with bortezomib. Clinical trial of GSK126 in patients with MM may be warranted. GSK126 is undergoing phase I trials for hypermethylation-related cancers. GSK126 is in phase I diffuse large B cell lymphoma and follicular lymphoma. GSK126 inhibits cell migration and angiogenesis in solid tumor cell lines through down-regulation of VEGF-A expression. Thus, it may be considered as a novel anticancer drug candidate for solid tumor.