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

Abstract:

BACKGROUND: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.

authors

Le Tourneau C,Siu LL

doi

10.1517/13543784.17.8.1247

subject

Has Abstract

pub_date

2008-08-01 00:00:00

pages

1247-54

issue

8

eissn

1354-3784

issn

1744-7658

journal_volume

17

pub_type

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