Drug Discov Today. 2009 Oct;14(19-20):964-72. Epub 2009 Jul 26.

Understanding CYP2D6 interactions.

de Groot MJ, Wakenhut F, Whitlock G, Hyland R.

Source

World Wide Medicinal Chemistry (WWMC), United Kingdom. marcel.degroot@pfizer.com

Abstract

Owing to the polymorphic nature of CYP2D6, clinically significant issues can arise when drugs rely on that enzyme either for clearance, or metabolism to an active metabolite. Available screening methods to determine if the compound is likely to cause drug-drug interactions, or is likely to be a victim of inhibition of CYP2D6 by other compounds will be described. Computational models and examples will be given on strategies to design out the CYP2D6 liabilities for both heme-binding compounds and non-heme-binding compounds.

PMID:: 19638317; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Other Literature Sources

Labome Researcher Resource - ExactAntigen/Labome

Medical

Drug Reactions - MedlinePlus Health Information

Supplemental Content

Related citations

Review Substrate specificity, inhibitors and regulation of human cytochrome P450 2D6 and implications in drug development. [Curr Med Chem. 2009]
Review Substrate specificity, inhibitors and regulation of human cytochrome P450 2D6 and implications in drug development.
Zhou SF, Liu JP, Lai XS. Curr Med Chem. 2009; 16(21):2661-805.
A molecular model of CYP2D6 constructed by homology with the CYP2C5 crystallographic template: investigation of enzyme-substrate interactions. [Drug Metabol Drug Interact. 2003]
A molecular model of CYP2D6 constructed by homology with the CYP2C5 crystallographic template: investigation of enzyme-substrate interactions.
Lewis DF, Dickins M, Lake BG, Goldfarb PS. Drug Metabol Drug Interact. 2003; 19(3):189-210.
Generation and validation of rapid computational filters for cyp2d6 and cyp3a4. [Drug Metab Dispos. 2003]
Generation and validation of rapid computational filters for cyp2d6 and cyp3a4.
Ekins S, Berbaum J, Harrison RK. Drug Metab Dispos. 2003 Sep; 31(9):1077-80.
Review Prediction of drug metabolism: the case of cytochrome P450 2D6. [Curr Top Med Chem. 2003]
Review Prediction of drug metabolism: the case of cytochrome P450 2D6.
Vermeulen NP. Curr Top Med Chem. 2003; 3(11):1227-39.
Exploration of catalytic properties of CYP2D6 and CYP3A4 through metabolic studies of levorphanol and levallorphan. [Drug Metab Dispos. 2010]
Exploration of catalytic properties of CYP2D6 and CYP3A4 through metabolic studies of levorphanol and levallorphan.
Bonn B, Masimirembwa CM, Castagnoli N Jr. Drug Metab Dispos. 2010 Jan; 38(1):187-99.

See reviews... See all...

Cited by 1 PubMed Central article

Understanding the determinants of selectivity in drug metabolism through modeling of dextromethorphan oxidation by cytochrome P450. [Proc Natl Acad Sci U S A. 2011]
Understanding the determinants of selectivity in drug metabolism through modeling of dextromethorphan oxidation by cytochrome P450.
Oláh J, Mulholland AJ, Harvey JN. Proc Natl Acad Sci U S A. 2011 Apr 12; 108(15):6050-5. Epub 2011 Mar 28.

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Compound (MeSH Keyword)
PubChem chemical compound records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.
Cited in PMC
Full-text articles in the PubMed Central Database that cite the current articles.

Recent activity

Clear Turn Off Turn On

Understanding CYP2D6 interactions.
Understanding CYP2D6 interactions.
Drug Discov Today. 2009 Oct ;14(19-20):964-72. Epub 2009 Jul 26 .

PubMed
Aspirin and clopidogrel resistance.
Aspirin and clopidogrel resistance.
Hematology Am Soc Hematol Educ Program. 2007 :114-20.

PubMed
The 'Nefertiti lift': a new technique for specific re-contouring of the jawline.
The 'Nefertiti lift': a new technique for specific re-contouring of the jawline.
J Cosmet Laser Ther. 2007 Dec ;9(4):249-52.

PubMed
Massively parallel pyrosequencing in HIV research.
Massively parallel pyrosequencing in HIV research.
AIDS. 2008 Jul 31 ;22(12):1411-5.

PubMed
Arachnid toxinology in Australia: from clinical toxicology to potential applicat...
Arachnid toxinology in Australia: from clinical toxicology to potential applications.
Toxicon. 2006 Dec 1 ;48(7):872-98. Epub 2006 Jul 21 .

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Display Settings:

Send to:

Understanding CYP2D6 interactions.

Source

Abstract

Publication Types, MeSH Terms, Substances

Publication Types

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Medical

Supplemental Content

Related citations

Cited by 1 PubMed Central article

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information