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Non-CYP Enzymes

Scientific Resources Non-CYP Enzymes

While Cytochrome P450 (CYP) enzymes are well-known and profiled for their role in metabolism of many small molecule drugs, other enzymes can play critical roles in a drug compound’s metabolism and overall disposition in a similar way. Here we offer resources which explore research involving drug interactions with non-CYP enzymes such as UGTs, SULTs, MAO-A, MAO-B, AO, XO, and others.

 

Webinars

Highlights of the In Vitro Sections of the Draft ICH Drug Interaction Studies Guideline and Comparison with Current Guidance

Presenter: Brian Ogilvie, Ph.D, Vice President of Scientific Consulting at XenoTech In June 2022, the ICH released the first draft of its harmonized Drug Interaction Studies Guideline (M12). The...
Webinars

Role of Sulfotransferases (SULTs) in Drug Metabolism and Potential for Drug-Drug Interactions

Presenter: Maciej Czerwinski, Ph.D., XenoTech Director of Scientific Consulting Abstract: Continuing our series on non-CYP-mediated metabolism pathways, we will be discussing another of the most requested...
Drug Metabolism Non-CYP Enzymes
Publications

In Vitro Strategies for Evaluating Non-CYP Metabolism Pathways

While cytochrome P450 (CYP)-mediated metabolism continues to be of primary concern for the majority of new small molecule drug candidates, efforts to develop compounds that...
Webinars

Role of UDP-Glucuronosyltransferases (UGTs) in Drug Metabolism and Drug-Drug Interactions

Presenter: Maciej Czerwinski, Ph.D., XenoTech Director of Scientific Consulting Abstract: The importance of glucuronidation for metabolism of xenobiotics in humans is illustrated by the abundance and...
Pallavi Limaye Director Scientific Consulting
Webinars

Underprediction of Drug Clearance by Aldehyde Oxidase (AO)–Mediated Drug Metabolism: Important Considerations for In Vitro Assessment

Presenter: Pallavi Limaye, Ph.D., DABT, XenoTech Director of Scientific Consulting Abstract: Aldehyde oxidase (AO) enzyme has gained increasing attention in drug development as one of the...
Webinars

An Overview of Non CYP-Mediated Metabolism Pathways and In Vitro Evaluation Strategies

Presenter: Andrew G. Taylor, Ph.D., Technical Support Manager for Services at XenoTech Abstract: Although cytochrome P450 (CYP)-mediated metabolism continues to be of major importance for...
Brian Ogilvie Presenting Regulatory Updates
Scientific Posters

Comparison Between the Final US FDA, Japan PMDA and EMA In Vitro DDI Guidance

Comparison Between the Final US FDA (2020), the Final Japan PMDA (2018), and Final EMA (2013) In Vitro DDI Guidance Documents: Are We Finally Harmonized?...
Scientific Posters

An assessment of in vitro inhibition of CYPs, UGTs and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Full Title An assessment of in vitro inhibition of CYPs, UGTs and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides Presented at the 2019 Marbach Castle Drug-Drug...
GLP Study
Blog

To GLP or not to GLP?

That is the question. . . Knowing the answer may save you time and money Good Laboratory Practices (GLP) are...

Cypex Portfolio of Recombinant Enzymes
Blog

Cypex Expands Portfolio of Recombinant Enzymes

As a distributor for Cypex in the US and Canada, XenoTech is proud to offer this portfolio of products based on patented...

Publications

An assessment of the in vitro inhibition of cytochrome P450 enzymes (CYP), UDP-glucuronsyltransferases (UGT) and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Faraz Kazmi, Phyllis Yerino, Chase McCoy, Andrew Parkinson, David B Buckley and Brian W Ogilvie Oligonucleotides represent an expanding class of pharmacotherapeutics in development for...
Scientific Posters

Evaluation of interspecies metabolic activities for non-CYP enzymes

Presented at the 32nd Annual Meeting of Japanese Society for the Study of Xenobiotics (JSSX) in Tokyo, Japan Full Title “Evaluation of interspecies metabolic activities...
Scientific Posters

Effects of organ preservation solution on aldehyde oxidase and xanthine oxidase activity in pooled human liver S9

Full Title Effects of organ preservation solution on aldehyde oxidase and xanthine oxidase activity in pooled human liver S9 Authors Kevin C. Lyon, Chad Pope,...
UGT Assays
Blog

UGT Activities, Concomitant Drugs, and DDI

If you have concerns about how your compound may affect UDP-glucuronosyltransferase (UGT) induction and/or inhibition when combined with other therapeutic...

Scientific Posters

In Vitro Evaluation of Ketoconazole and its Alternatives as Non-CYP Inhibitors

Full Title The In Vitro Evaluation of Ketoconazole and its Alternative Clinical CYP3A4/5 Inhibitors (Ritonavir, Clarithromycin and Itraconazole) as Inhibitors of Non-CYP Enzymes Abstract Ketoconazole...
Scientific Posters

Evaluation of Chemical Inhibitors for UDP-glucuronosyltransferase UGT Reaction Phenotyping Assays

Full Title Evaluation of Chemical Inhibitors for UDP-glucuronosyltransferase (UGT) Reaction Phenotyping Assays in Human Liver Microsomes Abstract In the development of a new chemical entity (NCE)...
Scientific Posters

UGT Inhibition Studies in the Presence or Absence of Alamethicin

Full Title UGT Inhibition Studies in the Presence or Absence of Alamethicin: Evaluation of UGT1A1 and UGT2B7 Inhibition in Human Liver Microsomes and Recombinant Enzymes...
Publications

A long-standing mystery solved: The formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UGT2B10 is an obligatory requirement

Faraz Kazmi, Joanna E. Barbara, Phyllis Yerino and Andrew Parkinson Desloratadine (Clarinex®), the major active metabolite of loratadine (Claritin®), is a non-sedating long-lasting antihistamine widely used for...
Scientific Posters

Induction of UDP-Glucuronosyltransferases in Cultures of Fresh and Immortalized Human Hepatocytes

Full Title Induction of UDP-Glucuronosyltransferases in Cultures of Fresh and Immortalized Human Hepatocytes Abstract We have examined the induction of UDP-glucuronosyltransferases (UGTs) in primary cultures...
Publications

In vitro inhibition of human liver cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes by rose bengal: system-dependent effects on inhibitory potential

Faraz Kazmi, Lois J. Haupt, Jennifer R. Horkman, Brian D. Smith, David B. Buckley, Eric A. Wachter, and Jamie M. Singer 1. Rose bengal (4,5,6,7-tetrachloro-2′,4′,5′,7′-tetraiodofluorescein)...
Scientific Posters

Selection of human liver S9 and cytosol fractions for evaluating clearance by aldehyde oxidase (AO)

Full Title Selection of human liver S9 and cytosol fractions for evaluating clearance by aldehyde oxidase (AO): The impact of low versus high AO activity lots. Abstract Aldehyde oxidase...
Publications

Catechol and aldehyde moieties of 3,4-dihydroxyphenylacetaldehyde contribute to tyrosine hydroxylase inhibition and neurotoxicity

Lydia M. Vermeer , Virginia R. Florang , Jonathan A. Doorn Parkinson’s disease (PD) is a progressive neurodegenerative disorder which leads to the selective loss...
Publications

Activator Protein-1 Regulation of Murine Aldehyde Dehydrogenase 1a1

Previously we demonstrated that aldehyde dehydrogenase (ALDH) 1a1 is the major ALDH expressed in mouse liver and is an effective catalyst in metabolism of lipid aldehydes...
Scientific Posters

Microsomes and S9 Prepared from Renal Tissue Yield High CYP, FMO and UGT Activities that are Stable…

Presented at the JSSX/ISSX Meeting, Maui, HI October 2005. Abstracts published in Drug Metabolism Reviews, Vol. 37, Supplement 2 Full Title Microsomes and S9 prepared...
Scientific Posters

Microsomes Prepared from Eluted Enterocytes Yield High Cytochrome P450 and UGT Activities that are…

Full Title Microsomes Prepared from Eluted Enterocytes Yield High Cytochrome P450 and UGT Activities that are Stable over Multiple Freeze/Thaw Cycles Abstract Enterocytes in the...