U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
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Approval Year

Substance Class Protein
Created
by admin
on Mon Mar 31 21:24:29 GMT 2025
Edited
by admin
on Mon Mar 31 21:24:29 GMT 2025
Protein Type ENZYME
Protein Sub Type CYTOCHROME P450
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
8E4LAA4357
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CYP2D6
Preferred Name English
CYTOCHROME P450 2D6
Common Name English
CYTOCHROME P450, FAMILY 2, SUBFAMILY D, POLYPEPTIDE 6
Common Name English
CYTOCHROME P 450 2D6
Common Name English
HUMAN CYTOCHROME P450 2D6
Common Name English
Code System Code Type Description
CAS
330597-62-1
Created by admin on Mon Mar 31 21:24:30 GMT 2025 , Edited by admin on Mon Mar 31 21:24:30 GMT 2025
PRIMARY
FDA UNII
8E4LAA4357
Created by admin on Mon Mar 31 21:24:30 GMT 2025 , Edited by admin on Mon Mar 31 21:24:30 GMT 2025
PRIMARY
UNIPROT
P10635
Created by admin on Mon Mar 31 21:24:30 GMT 2025 , Edited by admin on Mon Mar 31 21:24:30 GMT 2025
PRIMARY
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SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SELECTIVE
SUBSTRATE -> METABOLIC ENZYME
At higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms with estimated relative contributions of 3A4 (42%), 1A2 (26%), 2B6 (16%), 2C8 (6%), 2D6 (5%), 2C19 (5%) and 2C9 (< 1%).
NON-INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
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NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Lofexidine exposures were approximately 30% greater with co-administration of paroxetine a strong inhibitor of CYP2D6.
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
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SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITOR
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Strong Inhibitors(2) 5-fold increase in AUC or > 80% decrease in CL
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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N-demethylation of diphenhydramine is mainly catalyzed by CYP2D6 as a high-affinity P450 isozyme at a clinically relevant concentration.
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INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
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INHIBITOR -> METABOLIC ENZYME
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bufuralol substrate
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In vitro studies suggest that mephedrone metabolic disposition is regulated by the highly polymorphic isoenzyme of CYP2D6 (Pedersen et al., 2013).
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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SUBSTRATE -> METABOLIC ENZYME
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COMPETITIVE INHIBITOR
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SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
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SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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Abiraterone is an inhibitor of CYP2D6, in vivo. In vitro studies with human hepatic microsomes showed that abiraterone has the potential to inhibit CYP1A2, CYP2D6, CYP2C8 and to a lesser extent CYP2C9, CYP2C19 and CYP3A4/5.
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITION
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
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Based on in vitro assessment, CYP3A4 (41.9%) was the predominant cytochrome P450 (CYP) isoform responsible for the metabolism of belumosudil although CYP2D6 (21.7%), CYP2C8 (14.2%), CYP1A2 (<5%), CYP2C19 (<5%), and UGT1A9 may also contribute to a lesser extent
INHIBITOR -> METABOLIC ENZYME
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SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Inhibits at clinically relevant concentrations.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
WEAK INHIBITOR->METABOLIC ENZYME
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INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
Interaction with CYP2D6 substrates is not expected to be clinically significant.
MINOR
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
NON-INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
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NON-SUBSTRATE -> METABOLIC ENZYME
Intentionally designed to limit CYP2D6 based metabolism
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> TARGET
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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2.1% conversion to M1
SUBSTRATE -> METABOLIC ENZYME
O-demethylation, mediated by CYP2D6 was greater in extensive metabolizers of CYP2D6 than in poor metabolizers
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
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In vitro studies have shown that vilazodone is a moderate inhibitor of CYP2C19 and CYP2D6
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IC50
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Ki
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
IN-VIVO
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
MODERATE
INHIBITOR -> METABOLIC ENZYME
Eliglustat also exhibited time-dependent inhibition (TDI) of CYP2D6.
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
CYP2C8
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
IC50
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
WEAK
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Rifamycin is an inhibitor of CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4/5 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose clinically relevant inhibition of these enzymes in vivo is unlikely.
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
TISSUE EXPRESSION -> PARENT
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Cobimetinib is a reversible inhibitor of CYP3A4 and CYP2D6 in vitro.
REVERSIBLE
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
In vitro, lumefantrine significantly inhibits the activity of CYP2D6 at therapeutic plasma concentrations
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
IC50
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
MINOR

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
Heme binding [1_443] CYS HEME-CYSTEINE (OXIDIZED) G0HAF1JK3T
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL