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Human Cytochromes Mediating in vitro...

Wei, Zixuan.

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Human Cytochromes Mediating in vitro Metabolism of Lurasidone.

Record Type:	Electronic resources : Monograph/item
Title/Author:	Human Cytochromes Mediating in vitro Metabolism of Lurasidone./
Author:	Wei, Zixuan.
Published:	Ann Arbor : ProQuest Dissertations & Theses, : 2019,
Description:	37 p.
Notes:	Source: Masters Abstracts International, Volume: 80-12.
Contained By:	Masters Abstracts International80-12.
Subject:	Pharmacology. -
Online resource:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=13812424
ISBN:	9781392197554

Human Cytochromes Mediating in vitro Metabolism of Lurasidone.
Wei, Zixuan.

Human Cytochromes Mediating in vitro Metabolism of Lurasidone. - Ann Arbor : ProQuest Dissertations & Theses, 2019 - 37 p.

Source: Masters Abstracts International, Volume: 80-12.

Thesis (M.S.)--Sackler School of Graduate Biomedical Sciences (Tufts University), 2019.

This item must not be sold to any third party vendors.

The objective of this study was to develop an in vitro metabolic profile for lurasidone to determine pharmacokinetic parameters Vmax and Km, and to model potential drug-drug interactions. Lurasidone was first approved for clinical use in the United States in 2010 as a second-generation antipsychotic drug. Clinical studies have shown it has been a successful agent when used to treat patients with schizophrenia. It is also approved as an adjunctive therapy with lithium or valproate for the treatment of bipolar I disorder associated with major depressive episodes (MDEs). The in vitro metabolic profile of lurasidone has been mentioned in the product label and in review articles, but the scientific data has not been published (Greenblatt et al., 2018). We set up an UPLC-MS/MS assay to analyze the biotransformation of lurasidone. Since cytochrome (CYP) P450 3A enzymes are reported to be the principal isoform responsible for metabolizing lurasidone, the main metabolite ID-14283 was measured to calculate Vmax and Km. This was done by in vitro incubations with human liver microsomes (HLM) from adults. Based on the inhibition screen study, lurasidone is mainly metabolized by CYP3A4 in vitro. Ketoconazole and ritonavir were evaluated as potential inhibitors; the average IC50 value were 1.10 μM and 3.43 μM, respectively. These data suggest that clinical interactions of lurasidone with CYP3 inhibitors are likely, though validation is needed in clinical studies.

ISBN: 9781392197554Subjects--Topical Terms:

634543
Pharmacology.

Human Cytochromes Mediating in vitro Metabolism of Lurasidone.
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520 $a The objective of this study was to develop an in vitro metabolic profile for lurasidone to determine pharmacokinetic parameters Vmax and Km, and to model potential drug-drug interactions. Lurasidone was first approved for clinical use in the United States in 2010 as a second-generation antipsychotic drug. Clinical studies have shown it has been a successful agent when used to treat patients with schizophrenia. It is also approved as an adjunctive therapy with lithium or valproate for the treatment of bipolar I disorder associated with major depressive episodes (MDEs). The in vitro metabolic profile of lurasidone has been mentioned in the product label and in review articles, but the scientific data has not been published (Greenblatt et al., 2018). We set up an UPLC-MS/MS assay to analyze the biotransformation of lurasidone. Since cytochrome (CYP) P450 3A enzymes are reported to be the principal isoform responsible for metabolizing lurasidone, the main metabolite ID-14283 was measured to calculate Vmax and Km. This was done by in vitro incubations with human liver microsomes (HLM) from adults. Based on the inhibition screen study, lurasidone is mainly metabolized by CYP3A4 in vitro. Ketoconazole and ritonavir were evaluated as potential inhibitors; the average IC50 value were 1.10 μM and 3.43 μM, respectively. These data suggest that clinical interactions of lurasidone with CYP3 inhibitors are likely, though validation is needed in clinical studies.
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