Christophe Le Tourneau1, Lillian L Siu. 1. University of Toronto, University Health Network, Princess Margaret Hospital, Division of Medical Oncology and Hematology, 610 University Avenue, Suite 5-718, Toronto M5G 2M9, Canada.
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.
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: Edwin Choy; Karla Ballman; James Chen; Mark A Dickson; Rashmi Chugh; Suzanne George; Scott Okuno; Raphael Pollock; Rajiv M Patel; Antje Hoering; Shreyaskumar Patel Journal: Sarcoma Date: 2018-10-24
Authors: Dusan Ruzic; Nemanja Djoković; Tatjana Srdić-Rajić; Cesar Echeverria; Katarina Nikolic; Juan F Santibanez Journal: Pharmaceutics Date: 2022-01-16 Impact factor: 6.321