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Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor.

AbstractBACKGROUND:
Histone deacetylases (HDACs), which target histones as well as non-histone proteins as substrates, have the potential to regulate aberrant gene expression and restore normal growth control in malignancies.
OBJECTIVE:
This review provides an updated summary of preclinical and clinical experience with the oral isotype-selective HDAC inhibitor MGCD0103 in cancer.
METHODS:
Data presented in abstract form from international conferences or journal articles found within a PubMed search of article up to May 2008 are described in this review.
RESULTS/CONCLUSIONS:
MGCD0103 appears tolerable and exhibits favorable pharmacokinetic and pharmacodynamic profiles with evidence of target inhibition in surrogate tissues. Clinical and pharmacodynamic data support a three-times-weekly administration at a 90-mg fixed dose. MGCD0103 displays promising antitumor activity in hematological and lymphoproliferative diseases.
AuthorsChristophe Le Tourneau, Lillian L Siu
JournalExpert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 17 Issue 8 Pg. 1247-54 (Aug 2008) ISSN: 1744-7658 [Electronic] England
PMID18616420 (Publication Type: Journal Article, Review)
Chemical References
  • Antineoplastic Agents
  • Benzamides
  • Histone Deacetylase Inhibitors
  • Isoenzymes
  • Pyrimidines
  • mocetinostat
Topics
  • Animals
  • Antineoplastic Agents (administration & dosage, pharmacokinetics, pharmacology, therapeutic use)
  • Benzamides (administration & dosage, pharmacokinetics, pharmacology, therapeutic use)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Clinical Trials as Topic
  • Histone Deacetylase Inhibitors
  • Humans
  • Isoenzymes
  • Neoplasms (drug therapy)
  • Pyrimidines (administration & dosage, pharmacokinetics, pharmacology, therapeutic use)
  • Substrate Specificity

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