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The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method
Joint Authors
Hu, Lufeng
Cai, Jinzhang
Zhang, Qingwei
Lin, Kezhi
Zheng, Yuancai
Source
Issue
Vol. 2015, Issue 2015 (31 Dec. 2015), pp.1-7, 7 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2015-08-19
Country of Publication
Egypt
No. of Pages
7
Main Subjects
Abstract EN
MGCD0103, an isotype-selective histone deacetylase inhibitor (HDACi), has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agents.
In order to investigate the effects of MGCD0103 on the metabolic capacity of cytochrome P450 (CYP) enzymes, a cocktail method was employed to evaluate the activities of human CYP2B1, CYP1A2, CYP2C11, CYP2D6, CYP3A4, and CYP2C9.
The rats were randomly divided into MGCD0103 group (Low, Medium, and High) and control group.
The MGCD0103 group rats were given 20, 40, and 80 mg/kg (Low, Medium, and High) MGCD0103 by continuous intragastric administration for 7 days.
Six probe drugs, bupropion, phenacetin, tolbutamide, metoprolol, testosterone, and omeprazole, were given to rats through intragastric administration, and the plasma concentrations were determined by UPLC-MS/MS.
Statistical pharmacokinetics difference for tolbutamide in rats were observed by comparing MGCD0103 group with control group.
Continuous 7-day intragastric administration of MGCD0103 slightly induces the activities of CYP2C11 of rats.
American Psychological Association (APA)
Cai, Jinzhang& Zhang, Qingwei& Lin, Kezhi& Hu, Lufeng& Zheng, Yuancai. 2015. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. BioMed Research International،Vol. 2015, no. 2015, pp.1-7.
https://search.emarefa.net/detail/BIM-1055790
Modern Language Association (MLA)
Cai, Jinzhang…[et al.]. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. BioMed Research International No. 2015 (2015), pp.1-7.
https://search.emarefa.net/detail/BIM-1055790
American Medical Association (AMA)
Cai, Jinzhang& Zhang, Qingwei& Lin, Kezhi& Hu, Lufeng& Zheng, Yuancai. The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method. BioMed Research International. 2015. Vol. 2015, no. 2015, pp.1-7.
https://search.emarefa.net/detail/BIM-1055790
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1055790