Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs

The cytochrome P450 (CYP) enzyme family is the major enzyme system catalyzing the phase I metabolism of xenobiotics, including pharmaceuticals and toxic compounds in the environment. A major part of the CYP-dependent xenobiotic metabolism is due to polymorphic and inducible enzymes, which may, quant...

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Published in:Applied Sciences
Main Authors: Domenico Iacopetta, Jessica Ceramella, Alessia Catalano, Elisabetta Scali, Domenica Scumaci, Michele Pellegrino, Stefano Aquaro, Carmela Saturnino, Maria Stefania Sinicropi
Format: Article
Language:English
Published: MDPI AG 2023-05-01
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Online Access:https://www.mdpi.com/2076-3417/13/10/6045
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author Domenico Iacopetta
Jessica Ceramella
Alessia Catalano
Elisabetta Scali
Domenica Scumaci
Michele Pellegrino
Stefano Aquaro
Carmela Saturnino
Maria Stefania Sinicropi
author_facet Domenico Iacopetta
Jessica Ceramella
Alessia Catalano
Elisabetta Scali
Domenica Scumaci
Michele Pellegrino
Stefano Aquaro
Carmela Saturnino
Maria Stefania Sinicropi
author_sort Domenico Iacopetta
collection DOAJ
container_title Applied Sciences
description The cytochrome P450 (CYP) enzyme family is the major enzyme system catalyzing the phase I metabolism of xenobiotics, including pharmaceuticals and toxic compounds in the environment. A major part of the CYP-dependent xenobiotic metabolism is due to polymorphic and inducible enzymes, which may, quantitatively or qualitatively, alter or enhance drug metabolism and toxicity. Drug–drug interactions are major mechanisms caused by the inhibition and/or induction of CYP enzymes. Particularly, CYP monooxygenases catalyze hydroxylation reactions to form hydroxylated metabolites. The secondary metabolites are sometimes as active as the parent compound, or even more active. The aim of this review is to summarize some of the significative examples of common drugs used for the treatment of diverse diseases and underline the activity and/or toxicity of their metabolites.
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spelling doaj-art-e66727d3fb814ad08ec0e0842897fb8e2025-08-20T00:58:40ZengMDPI AGApplied Sciences2076-34172023-05-011310604510.3390/app13106045Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of DrugsDomenico Iacopetta0Jessica Ceramella1Alessia Catalano2Elisabetta Scali3Domenica Scumaci4Michele Pellegrino5Stefano Aquaro6Carmela Saturnino7Maria Stefania Sinicropi8Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata, 87036 Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata, 87036 Rende, ItalyDepartment of Pharmacy-Drug Sciences, University of Bari “Aldo Moro”, 70126 Bari, ItalyDepartment of Health Sciences, Magna Graecia University, 88100 Catanzaro, ItalyResearch Center on Advanced Biochemistry and Molecular Biology, Department of Experimental and Clinical Medicine, Magna Græcia University of Catanzaro, 88100 Catanzaro, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata, 87036 Rende, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata, 87036 Rende, ItalyDepartment of Science, University of Basilicata, 85100 Potenza, ItalyDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata, 87036 Rende, ItalyThe cytochrome P450 (CYP) enzyme family is the major enzyme system catalyzing the phase I metabolism of xenobiotics, including pharmaceuticals and toxic compounds in the environment. A major part of the CYP-dependent xenobiotic metabolism is due to polymorphic and inducible enzymes, which may, quantitatively or qualitatively, alter or enhance drug metabolism and toxicity. Drug–drug interactions are major mechanisms caused by the inhibition and/or induction of CYP enzymes. Particularly, CYP monooxygenases catalyze hydroxylation reactions to form hydroxylated metabolites. The secondary metabolites are sometimes as active as the parent compound, or even more active. The aim of this review is to summarize some of the significative examples of common drugs used for the treatment of diverse diseases and underline the activity and/or toxicity of their metabolites.https://www.mdpi.com/2076-3417/13/10/6045metaboliteshydroxylationmonooxygenasesCYP450hydroxylated metabolites
spellingShingle Domenico Iacopetta
Jessica Ceramella
Alessia Catalano
Elisabetta Scali
Domenica Scumaci
Michele Pellegrino
Stefano Aquaro
Carmela Saturnino
Maria Stefania Sinicropi
Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
metabolites
hydroxylation
monooxygenases
CYP450
hydroxylated metabolites
title Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
title_full Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
title_fullStr Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
title_full_unstemmed Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
title_short Impact of Cytochrome P450 Enzymes on the Phase I Metabolism of Drugs
title_sort impact of cytochrome p450 enzymes on the phase i metabolism of drugs
topic metabolites
hydroxylation
monooxygenases
CYP450
hydroxylated metabolites
url https://www.mdpi.com/2076-3417/13/10/6045
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