Phase 1 study of the oral isotype specific histone deacetylase inhibitor MGCD0103 in leukemia.

No abstract is available for this paper.

• Publication year

  2008

• Venue

  Blood

• Publication date

  2008-08-15

• Fields of study

  Medicine

• Identifiers
  DOI 10.1182/blood-2007-10-115873PMID 18495956PMCID PMC4081529
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Phase I study of MGCD0103 given as a three-times-per-week oral dose in patients with advanced solid tumors.

  2008cited by this paper
• Phase 1 study of the histone deacetylase inhibitor vorinostat (suberoylanilide hydroxamic acid [SAHA]) in patients with advanced leukemias and myelodysplastic syndromes.

  2008cited by this paper
• Evaluation of the Pharmacodynamic Effects of MGCD0103 from Preclinical Models to Human Using a Novel HDAC Enzyme Assay

  2008cited by this paper
• Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.

  2008cited by this paper
• Clinical Trials and Observations

  2008cited by this paper
• MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo

  2008cited by this paper
• Antitumor effect of the histone deacetylase inhibitor LAQ824 in combination with 13-cis-retinoic acid in human malignant melanoma

  2007cited by this paper
• Will broad-spectrum histone deacetylase inhibitors be superseded by more specific compounds?

  2007cited by this paper
• Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias.

  2007cited by this paper
• Phase 2 trial of oral vorinostat (suberoylanilide hydroxamic acid, SAHA) for refractory cutaneous T-cell lymphoma (CTCL).

  2007cited by this paper
• Safety and clinical activity of the combination of 5-azacytidine, valproic acid, and all-trans retinoic acid in acute myeloid leukemia and myelodysplastic syndrome.

  2007cited by this paper
• Assays for pharmacodynamic analysis of histone deacetylase inhibitors

  2006cited by this paper
• Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies

  2006cited by this paper
• Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.

  2006cited by this paper
• Gemcitabine plus CI-994 offers no advantage over gemcitabine alone in the treatment of patients with advanced pancreatic cancer: results of a phase II randomized, double-blind, placebo-controlled, multicenter study.

  2006cited by this paper
• Phase 1/2 study of the combination of 5-aza-2'-deoxycytidine with valproic acid in patients with leukemia.

  2006cited by this paper
• Anticancer activities of histone deacetylase inhibitors

  2006cited by this paper
• Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma.

  2005cited by this paper
• Phase I study of an oral histone deacetylase inhibitor, suberoylanilide hydroxamic acid, in patients with advanced cancer.

  2005cited by this paper
• A phase 1 and pharmacodynamic study of depsipeptide (FK228) in chronic lymphocytic leukemia and acute myeloid leukemia.

  2004cited by this paper
• Chronic Oral Administration of CI-994: A Phase I Study

  2004cited by this paper
• The discovery of NVP-LAQ824: from concept to clinic.

  2003cited by this paper
• Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101.

  2003cited by this paper
• Phase I clinical trial of histone deacetylase inhibitor: suberoylanilide hydroxamic acid administered intravenously.

  2003cited by this paper
• Histone-deacetylase inhibitors: novel drugs for the treatment of cancer

  2002cited by this paper
• Histone deacetylase: a target for antiproliferative and antiprotozoal agents.

  2001cited by this paper
• Histone acetylases and deacetylases in cell proliferation.

  1999cited by this paper
• Nuclear histone acetylases and deacetylases and transcriptional regulation: HATs off to HDACs.

  1997cited by this paper
• Histone acetylation in chromatin structure and transcription

  1997cited by this paper
• On the biological role of histone acetylation.

  1990cited by this paper

• IHCH9033, a novel class I HDAC inhibitor, synergizes with FLT3 inhibitor and rescues quizartinib resistance in FLT3-ITD AML via enhancing DNA damage response

  2025cites this paper
• Targeting HDAC8 sensitizes tyrosine kinase inhibitors in the elimination of B-cell acute lymphoblastic leukemia cells through degradation of HIF-1α

  2025cites this paper
• Epigenetics-targeted drugs: current paradigms and future challenges

  2024cites this paper
• Histone deacetylase inhibitors for leukemia treatment: current status and future directions

  2024cites this paper
• The Class I Histone Deacetylase Inhibitor as a Potent Therapeutic Target for Treating Glioblastoma and Mocetinostat as a Novel Inhibitor in the Induction Death of Cancer Cells

  2024influential citation
• Prediction of survival with lower intensity therapy among older patients with acute myeloid leukemia

  2023cites this paper
• The ubiquitin ligase RNF5 determines acute myeloid leukemia growth and susceptibility to histone deacetylase inhibitors

  2021cites this paper
• Microtubule associated proteins as targets for anticancer drug development.

  2021cites this paper
• Treatment of Newly Diagnosed AML in Unfit Patients

  2021cites this paper
• Discovery of novel hit compounds as potential HDAC1 inhibitors: The case of ligand- and structure-based virtual screening

  2021cites this paper
• Recent Progress in Histone Deacetylase Inhibitors as Anticancer Agents.

  2020cites this paper
• RNF5 Regulation of RBBP4 Defines Acute Myeloid Leukemia Growth and Susceptibility to Histone Deacetylase Inhibitors

  2020cites this paper
• Novel therapeutic strategies for MLL-rearranged leukemias.

  2020cites this paper
• Histone Deacetylase Inhibitors in Combinatorial Anticancer Therapy

  2020cites this paper
• Computer-Driven Development of an in Silico Tool for Finding Selective Histone Deacetylase 1 Inhibitors

  2020cites this paper
• Histone deacetylase inhibitor MGCD0103 causes cell cycle arrest, apoptosis, and autophagy in liver cancer cells

  2020cites this paper
• Small Molecules Targeting HATs, HDACs, and BRDs in Cancer Therapy

  2020cites this paper
• Short-term organoid culture for drug sensitivity testing of high-grade serous carcinoma.

  2020cites this paper
• Singlet Anticancer Therapy Through Epi-Weapons Histone Deacetylase Inhibitors and Its Shortcomings

  2020cites this paper
• Low-intensity regimens versus standard-intensity induction strategies in acute myeloid leukemia

  2020cites this paper
• Recent Progress of Oridonin and Its Derivatives for the Treatment of Acute Myelogenous Leukemia.

  2020cites this paper
• Histone deacetylase inhibitor based prodrugs.

  2020cites this paper
• Recent Studies on HDAC Inhibitors Acting against Prostate Cancer

  2020cites this paper
• Safety and efficacy of oral panobinostat plus chemotherapy in patients aged 65 years or younger with high-risk acute myeloid leukemia.

  2019cites this paper
• Zinc-dependent Deacetylase (HDAC) Inhibitors with Different Zinc Binding Groups.

  2019cites this paper
• HDAC Inhibitors in Acute Myeloid Leukemia

  2019influential citation
• Chromatin dynamics at the core of kidney fibrosis.

  2018cites this paper
• Histone Deacetylase Inhibitors: A Prospect in Drug Discovery

  2018cites this paper
• Selective DOT1L, LSD1, and HDAC Class I Inhibitors Reduce HOXA9 Expression in MLL-AF9 Rearranged Leukemia Cells, But Dysregulate the Expression of Many Histone-Modifying Enzymes.

  2018cites this paper
• The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity.

  2018cites this paper
• Tissue-Nonspecific Alkaline Phosphatase Is Required for MC3T3 Osteoblast–Mediated Protection of Acute Myeloid Leukemia Cells from Apoptosis

  2018cites this paper
• Phase I/II study of mocetinostat in combination with gemcitabine for patients with advanced pancreatic cancer and other advanced solid tumors

  2018cites this paper
• HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.

  2018cites this paper
• Zinc binding groups for histone deacetylase inhibitors

  2018cites this paper
• Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies.

  2018cites this paper
• Prospects of targeted therapy of acute leukemias in children

  2017cites this paper
• Emerging therapies for acute myeloid leukemia

  2017cites this paper
• Complete molecular remission in relapsed and refractory acute myeloid leukaemia with MLL‐AF9 treated with chidamide‐based chemotherapy

  2017cites this paper
• Phase 1 dose-escalation study of oral abexinostat for the treatment of patients with relapsed/refractory higher-risk myelodysplastic syndromes, acute myeloid leukemia, or acute lymphoblastic leukemia

  2017cites this paper
• Clinical Applications of Histone Deacetylase Inhibitors

  2017cites this paper
• Histone deacetylase inhibitors reduce differentiating osteoblast-mediated protection of acute myeloid leukemia cells from cytarabine

  2017cites this paper
• Emerging epigenetics in cancer chemoprevention by dietary phytochemicals

  2017cites this paper
• A phase 2 study of mocetinostat, a histone deacetylase inhibitor, in relapsed or refractory lymphoma

  2017cites this paper
• Exploration of the binding pocket of histone deacetylases: the design of potent and isoform-selective inhibitors.

  2017cites this paper
• Phase II Study of Mocetinostat ( MGCD 0103 ) In Patients with Relapsed and Refractory Classical Hodgkin Lymphoma

  2016cites this paper
• Treatment options for patients with myelodysplastic syndromes after hypomethylating agent failure.

  2016cites this paper
• Regulation of Autophagy in Chronic Lymphocytic Leukemia: The Role of Histone Deacetylase Inhibitors

  2016cites this paper
• Chidamide, a novel histone deacetylase inhibitor, inhibits the viability of MDS and AML cells by suppressing JAK2/STAT3 signaling.

  2016cites this paper
• Emerging biological therapies for the treatment of myelodysplastic syndromes

  2016cites this paper
• Targeting histone deacetylases: A novel therapeutic strategy for atrial fibrillation.

  2016cites this paper
• Chapter 13 – Clinical Applications of Epigenetic Drugs

  2016cites this paper
• Identification of a cancer stem cell-specific function for the histone deacetylases, HDAC1 and HDAC7, in breast and ovarian cancer

  2016cites this paper
• DNA Methylation and Chromatin Remodeling: The Blueprint of Cancer Epigenetics

  2016cites this paper
• Histone deacetylases 1 and 2 cooperate in regulating BRCA1, CHK1, and RAD51 expression in acute myeloid leukemia cells

  2016cites this paper
• Epigenetic regulators and their impact on therapy in acute myeloid leukemia

  2016cites this paper
• Small Molecular Inhibitors Targeting Chromatin Regulating Proteins for Cancer.

  2016cites this paper
• Lost in translation? Ten years of development of histone deacetylase inhibitors in acute myeloid leukemia and myelodysplastic syndromes

  2016cites this paper
• Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia.

  2016cites this paper
• Inhibition of histone deacetylases induces formation of multipolar spindles and subsequent p53-dependent apoptosis in nasopharyngeal carcinoma cells

  2016cites this paper
• The safety profile of vorinostat (suberoylanilide hydroxamic acid) in hematologic malignancies: A review of clinical studies.

  2016cites this paper
• Metabolic changes in rats after intragastric administration of MGCD0103 (Mocetinostat), a HDAC class I inhibitor.

  2015cites this paper
• Epigenetic Drugs: A Hope to Treat Cancer

  2015cites this paper
• EPACs: epigenetic regulators that affect cell survival in cancer.

  2015cites this paper
• Development of an ELISA-Based HDAC Activity Assay for Characterization of Isoform-Selective Inhibitors

  2015cites this paper
• Navigating into the chemical space between MGCD0103 and SAHA: novel histone deacetylase inhibitors as a promising lead

  2015cites this paper
• Recent advances in cancer therapeutics.

  2015cites this paper
• Development of Epigenetic Targeted Therapies in Hematological Malignancies: From Serendipity to Synthetic Lethality

  2015cites this paper
• Histone Deacetylase Inhibitors Target the Leukemic Microenvironment by Enhancing a Nherf1-Protein Phosphatase 1α-TAZ Signaling Pathway in Osteoblasts*

  2015cites this paper
• A phase I trial of two sequence-specific schedules of decitabine and vorinostat in patients with acute myeloid leukemia

  2015cites this paper
• Potential use of histone deacetylase inhibitors in cancer therapy

  2015cites this paper
• The role of mutations in epigenetic regulators in myeloid malignancies

  2015cites this paper
• Impact of Histone Deacetylase Inhibitors on microRNA Expression and Cancer Therapy: A Review

  2015influential citation
• Epigenetic Therapy in Acute Myeloid Leukemia: Current and Future Directions.

  2015cites this paper
• Analysis of class I and II histone deacetylase gene expression in human leukemia

  2015cites this paper
• Novel agents for the treatment of childhood acute leukemia

  2015cites this paper
• Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents

  2015cites this paper
• Histone acetyltransferases and histone deacetylases in B- and T-cell development, physiology and malignancy

  2015cites this paper
• Epigenetic deregulation in myeloid malignancies.

  2015cites this paper
• The Role of HDACs as Leukemia Therapy Targets using HDI

  2015cites this paper
• Histone deacetylase inhibitors and epigenetic regulation in lymphoid malignancies

  2015cites this paper
• Synergistic antitumor interactions between MK-1775 and panobinostat in preclinical models of pancreatic cancer.

  2015cites this paper
• Results of phase 2 randomized study of low‐dose decitabine with or without valproic acid in patients with myelodysplastic syndrome and acute myelogenous leukemia

  2015cites this paper
• Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next

  2014cites this paper
• Phase I study of anti-VEGF monoclonal antibody bevacizumab and histone deacetylase inhibitor valproic acid in patients with advanced cancers

  2014cites this paper
• Liquid chromatography mass spectrometry determination of mocetinostat (MGCD0103) in rat plasma and its application to a pharmacokinetic study

  2014influential citation
• Clinical development of demethylating agents in hematology.

  2014cites this paper
• Pharmacophore modelling, validation, 3D virtual screening, docking, design and in silico ADMET simulation study of histone deacetylase class-1 inhibitors

  2014cites this paper
• Small molecule inhibitors in acute myeloid leukemia: from the bench to the clinic

  2014cites this paper
• New strategies for relapsed acute myeloid leukemia: fertile ground for translational research

  2014cites this paper
• Toxicological and metabolic considerations for histone deacetylase inhibitors

  2013influential citation
• HDAC inhibition by SNDX-275 (Entinostat) restores expression of silenced leukemia-associated transcription factors Nur77 and Nor1 and of key pro-apoptotic proteins in AML

  2013cites this paper
• Biologics: Targets and Therapy

  2013cites this paper
• Combating the epigenome: epigenetic drugs against non-Hodgkin's lymphoma.

  2013cites this paper
• [Histone deacetylase inhibitors - molecular mechanisms of actions and clinical applications].

  2013cites this paper
• Epigenetic Alterations in Pancreatic Cancer

  2013cites this paper
• Preclinical data and early clinical experience supporting the use of histone deacetylase inhibitors in multiple myeloma.

  2013cites this paper
• A perspective on dietary phytochemicals and cancer chemoprevention: oxidative stress, nrf2, and epigenomics.

  2013cites this paper
• Histone deacetylase inhibitors: recent outcomes from clinical trials and the implications for oncology treatment approaches

  2013cites this paper
• Sulforaphane enhances Nrf2 expression in prostate cancer TRAMP C1 cells through epigenetic regulation.

  2013cites this paper
• Panobinostat Synergistically Enhances the Cytotoxic Effects of Cisplatin, Doxorubicin or Etoposide on High-Risk Neuroblastoma Cells

  2013cites this paper