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Restrict the search for
tyrosine
to a specific field?
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:
INN:dapolsertib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04066244: Phase 2 Interventional Terminated Amyotrophic Lateral Sclerosis
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
BLZ 945, an orally active antagonist of the colony-stimulating factor1
receptor (CSF1R), is being developed by Novartis and Celgene Corporation for the treatment of advanced solid tumors and tumor-induced osteolytic lesions in bone and skeletal-related events. Phase I/II development for solid tumors is underway in the US, Italy, Spain, and Singapore. Preclinical trials were ongoing for tumor-induced osteolysis in Europe and the US. However, no recent reports of development had been identified for this indication.
Status:
Investigational
Source:
NCT03123393: Phase 2 Interventional Terminated Diffuse Large B-cell Lymphoma
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
TAK-659 is an investigational, reversible, and potent dual inhibitor of SYK and FLT-3 kinases. TAK-659 inhibited the pro-survival, proliferative, chemoresistant, and activation effects promoted by the microenvironment. Combination of TAK-659 with other BCR inhibitors showed a synergistic effect in inducing apoptosis. Combination of TAK-659 and ibrutinib induced significantly higher cytotoxicity toward CLL cells. TAK-659 suppressed splenomegaly and tumor development in an LMP2A/Myc mouse model in nanomolar concentrations. In addition, TAK-659 also blocked metastasis of tumor cells into bone marrow. A phase Ib/II study of TAK-659 is underway in patients with relapsed or refractory acute myelogenous leukemia
Status:
Investigational
Source:
NCT04486911: Phase 2 Interventional Active, not recruiting Breast Cancer
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
INN:tamnorzatinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02983617: Phase 2 Interventional Completed Chronic Lymphocytic Leukemia
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Entospletinib (GS-9973) is an adenosine triphosphate competitive inhibitor of Syk that disrupts kinase activity, which is currently in clinical trials for multiple B-cell malignancies. The most common treatment-emergent serious adverse events included dyspnea, pneumonia, febrile neutropenia, dehydration, and pyrexia.
Status:
Investigational
Source:
NCT03598699: Phase 2 Interventional Completed Dry Eye
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT02954991: Phase 2 Interventional Terminated Carcinoma, Non-Small-Cell Lung
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Glesatinib (MGCD265) is an orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. Glesatinib binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs. Studies in a gastric cancer xenograft model revealed that, in addition to the typically reported cellular activities, glesatinib in combination with erlotinib disrupted the glycolysis pathway, suggesting a novel mechanism of action for this drug. Glesatinib has been studied in a variety of advanced solid tumors including NSCLC, as a monotherapy and in combination with either docetaxel or erlotinib. In an ongoing phase 1 study in patients with MET positive or AXL-rearranged advanced solid tumors, glesatinib demonstrated preliminary single-agent activity, with all three patients with MET dysregulated NSCLC (two with METex14 alterations and one with increased GCN) showing significant tumor regression at the first assessment. A phase 2 study is currently recruiting patients with MET-dysregulated (mutated or amplified) advanced or metastatic NSCLC.
Status:
Investigational
Source:
NCT02629692: Phase 1/Phase 2 Interventional Active, not recruiting Healthy (For Part A)
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
