Abstract | BACKGROUND: 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 | Christophe Le Tourneau, Lillian L Siu |
Journal | Expert opinion on investigational drugs
(Expert Opin Investig Drugs)
Vol. 17
Issue 8
Pg. 1247-54
(Aug 2008)
ISSN: 1744-7658 [Electronic] England |
PMID | 18616420
(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
|