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ZL277 is a prodrug of belinostat with enhanced bioavailability and efficacy as a pan histone deacetylase (HDAC) inhibitor. In this study, we investigated the metabolism and pharmacokinetics of ZL277 in liver S9 fractions, liver microsomes, liver cytosol,
Changde Zhang +2 more
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Belinostat: clinical applications in solid tumors and lymphoma
Expert Opinion on Investigational Drugs, 2011Histone deacetylase (HDAC) inhibitors have recently emerged as a novel and active class of anticancer agents. Belinostat is one member of the class that has been tested as a single agent and in combination with other chemotherapies and biological agents in the treatment of solid tumors and lymphoma.A literature search of pre-clinical and clinical ...
L Rhoda Molife, Johann S de Bono
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BACKGROUND: The objective of this study was to evaluate the efficacy of belinostat, a histone deacetylase inhibitor, when added to paclitaxel/carboplatin in the empiric first-line treatment of patients with carcinoma of unknown primary site (CUP).METHODS:
Gedske Daugaard +2 more
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Belinostat for the treatment of peripheral T-cell lymphomas
Drugs of Today, 2014Belinostat is a novel histone deacetylase (HDAC) inhibitor that is being developed in various solid tumors and hematologic malignancies. HDACs have been found to be important in the epigenetic regulation of cancer progression and inhibition of these molecules in preclinical studies induces cancer cell apoptosis and prevents tumor growth.
J, McDermott, A, Jimeno
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Reversal of platinum drug resistance by the histone deacetylase inhibitor belinostat
Lung Cancer, 2017To investigate and elucidate the mechanism for the potentiation of cisplatin anticancer activity by belinostat in platinum (Pt)-resistant lung cancer cells.Combination of cisplatin and belinostat was investigated in two pairs of parental and cisplatin-resistant non-small cell lung cancer (NSCLC) cell lines.
Kenneth K W To, Liwu Fu
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Belinostat for the treatment of T-cell lymphoma
Expert Opinion on Orphan Drugs, 2014Introduction: T-cell lymphomas are a rare and heterogeneous group of malignant diseases that, for the most part, are associated with a very poor prognosis. Advances in understanding lymphoma biology and molecular pathogenesis coupled with interesting empiric observations have yielded many promising new therapeutic targets.
Ahmed Sawas, Owen A O’Connor
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Belinostat: a new broad acting antineoplastic histone deacetylase inhibitor
Expert Opinion on Investigational Drugs, 2009Belinostat is a potent hydroxamate-type histone deacetylase inhibitor with a broad antineoplastic activity in a spectrum of preclinical tumor models and with demonstrated clinical efficacy in the still very early clinical trial program. Belinostat has been relatively well tolerated following both i.v.
Peter Gimsing
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Belinostat: First Global Approval
Drugs, 2014Belinostat [Beleodaq(®) (US)], a small-molecule hydroxamate-type inhibitor of class I, II and IV histone deacetylase (HDAC) enzymes, has been developed by TopoTarget and Spectrum Pharmaceuticals for the treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL).
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The successful design and synthesis of a novel Pt complex of the histone deacteylase inhibitor belinostat are reported. Molecular modelling assisted in the identification of a suitable malonate derivative of belinostat (mal-p-Bel) for complexation to ...
Darren M Griffith +2 more
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Belinostat for the treatment of relapsed or refractory peripheral T-cell lymphoma
Future Oncology, 2015The prognosis of patients with relapsed/refractory peripheral T-cell lymphoma (PTCL) remains poor and current treatments are typically of limited benefit. Histone deacetylase (HDAC) inhibitors have proven effective for the treatment of relapsed/refractory PTCL.
Armin, Rashidi, Amanda F, Cashen
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