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Ref Type Journal Article
PMID (28753594)
Authors Besse L, Kraus M, Besse A, Bader J, Silzle T, Mehrling T, Driessen C
Title The first-in-class alkylating HDAC inhibitor EDO-S101 is highly synergistic with proteasome inhibition against multiple myeloma through activation of multiple pathways.
Journal Blood cancer journal
Vol 7
Issue 7
Date 2017 Jul 28
URL
Abstract Text

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Tinostamustine Tinostamustine 1 4
Drug Name Trade Name Synonyms Drug Classes Drug Description
Tinostamustine EDO-S101 Chemotherapy - Alkylating 14 HDAC Inhibitor 38 Tinostamustine (EDO-S101) comprises the structure of the DNA alkylating drug bendumustine combined with the pan-HDAC inhibitor vorinostat, which may both induce DNA damage and inhibit DNA repair resulting in increased tumor cell death (PMID: 28753594).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown lymphoma not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Velcade (bortezomib) worked synergistically to decrease viability of lymphoma cell lines in culture (PMID: 28753594). 28753594
Unknown unknown multiple myeloma not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, the combination of Velcade (bortezomib) and EDO-S101 induced cell-cycle arrest and apoptosis, and worked synergistically to decrease viability of multiple myeloma cell lines in culture (PMID: 28753594). 28753594
Unknown unknown lymphoma not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Kyprolis (carfilzomib) worked synergistically to decrease viability of a lymphoma cell lines in culture (PMID: 28753594). 28753594
Unknown unknown acute myeloid leukemia not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, the combination of EDO-S101 and Kyprolis (carfilzomib) decreased viability of primary acute myeloid leukemia cells in culture (PMID: 28753594). 28753594
Unknown unknown triple-receptor negative breast cancer not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Velcade (bortezomib) worked synergistically to decrease viability of triple negative breast cancer cell lines in culture (PMID: 28753594). 28753594
Unknown unknown chronic lymphocytic leukemia not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, the combination of EDO-S101 and Velcade (bortezomib) decreased viability of primary chronic lymphocytic leukemia cells in culture (PMID: 28753594). 28753594
Unknown unknown triple-receptor negative breast cancer not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Kyprolis (carfilzomib) worked synergistically to decrease viability of triple negative breast cancer cell lines in culture (PMID: 28753594). 28753594
Unknown unknown acute myeloid leukemia not applicable Bortezomib + Tinostamustine Preclinical - Patient cell culture Actionable In a preclinical study, the combination of EDO-S101 and Velcade (bortezomib) decreased viability of primary acute myeloid leukemia cells in culture (PMID: 28753594). 28753594
Unknown unknown acute promyelocytic leukemia not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Kyprolis (carfilzomib) worked synergistically to decrease viability of an acute promyelocytic leukemia cell line in culture (PMID: 28753594). 28753594
Unknown unknown multiple myeloma not applicable Carfilzomib + Tinostamustine Preclinical - Patient cell culture Actionable In a preclinical study, the combination of Kyprolis (carfilzomib) and EDO-S101 worked synergistically to decrease viability of multiple myeloma cell lines and primary cells in culture, including a cell line with resistance to Velcade (bortezomib) (PMID: 28753594). 28753594
Unknown unknown multiple myeloma not applicable Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, treatment with EDO-S101 induced apoptosis and decreased viability of a multiple myeloma cell line in culture (PMID: 28753594). 28753594
Unknown unknown multiple myeloma not applicable Delanzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, the combination of Delanzomib (CEP-1877) and EDO-S101 worked synergistically to decrease viability of a multiple myeloma cell line in culture (PMID: 28753594). 28753594
Unknown unknown chronic lymphocytic leukemia not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, the combination of EDO-S101 and Kyprolis (carfilzomib) decreased viability of primary chronic lymphocytic leukemia cells in culture (PMID: 28753594). 28753594
Unknown unknown acute promyelocytic leukemia not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Velcade (bortezomib) worked synergistically to decrease viability of an acute promyelocytic leukemia cell line in culture (PMID: 28753594). 28753594
Unknown unknown acute monocytic leukemia not applicable Carfilzomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Kyprolis (carfilzomib) worked synergistically to decrease viability of an acute monocytic leukemia cell line in culture (PMID: 28753594). 28753594
Unknown unknown acute monocytic leukemia not applicable Bortezomib + Tinostamustine Preclinical - Cell culture Actionable In a preclinical study, EDO-S101 and Velcade (bortezomib) worked synergistically to decrease viability of an acute monocytic leukemia cell line in culture (PMID: 28753594). 28753594