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

Approval Year

Substance Class Protein
Created
by admin
on Fri Jun 25 20:34:43 UTC 2021
Edited
by admin
on Fri Jun 25 20:34:43 UTC 2021
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
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
CYP2D6
Common Name English
Code System Code Type Description
CAS
330597-62-1
Created by admin on Fri Jun 25 20:34:44 UTC 2021 , Edited by admin on Fri Jun 25 20:34:44 UTC 2021
PRIMARY
FDA UNII
8E4LAA4357
Created by admin on Fri Jun 25 20:34:44 UTC 2021 , Edited by admin on Fri Jun 25 20:34:44 UTC 2021
PRIMARY
UNIPROT
P10635
Created by admin on Fri Jun 25 20:34:44 UTC 2021 , Edited by admin on Fri Jun 25 20:34:44 UTC 2021
PRIMARY
Related Record Type Details
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%).
INHIBITOR -> METABOLIC ENZYME
LOW
Ki
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
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
INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITOR
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
NON-SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
N-demethylation of diphenhydramine is mainly catalyzed by CYP2D6 as a high-affinity P450 isozyme at a clinically relevant concentration.
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
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
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Pharmacological action: Tricyclic antidepressant drug (TCA)
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
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
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
WEAK INHIBITOR->METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
SUBSTRATE -> METABOLIC ENZYME
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
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
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
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
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
INHIBITOR -> METABOLIC ENZYME
In vitro studies have shown that vilazodone is a moderate inhibitor of CYP2C19 and CYP2D6
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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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
Metabolizing reaction by CYP2D6: N-demethylation
SUBSTRATE -> METABOLIC ENZYME
IN-VITRO
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
INHIBITOR -> METABOLIC ENZYME
POTENT
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
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Metabolizing reaction by CYP2D6: N-demethylation Pharmacological action: Phenothiazine antipsychotic
SUBSTRATE
Unidentified
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
CYP2C8
IC50
SUBSTRATE -> METABOLIC ENZYME
Metabolizing reaction by CYP2D6: Demethylatio
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
INHIBITOR -> 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
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
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> 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
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
Metabolizing reaction by CYP2D6: O-demethylation
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
Pharmacological action: Tricyclic antidepressant drug (TCA)
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL