Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 04:51:42 GMT 2023
by
admin
on
Sat Dec 16 04:51:42 GMT 2023
|
Protein Type | ENZYME |
Protein Sub Type | CYTOCHROME P450 |
Sequence Origin | HUMAN |
Sequence Type | COMPLETE |
Record UNII |
8E4LAA4357
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Record Status |
Validated (UNII)
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Record Version |
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-
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Name | Type | Language | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
Code System | Code | Type | Description | ||
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330597-62-1
Created by
admin on Sat Dec 16 04:51:54 GMT 2023 , Edited by admin on Sat Dec 16 04:51:54 GMT 2023
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PRIMARY | |||
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8E4LAA4357
Created by
admin on Sat Dec 16 04:51:54 GMT 2023 , Edited by admin on Sat Dec 16 04:51:54 GMT 2023
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PRIMARY | |||
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P10635
Created by
admin on Sat Dec 16 04:51:54 GMT 2023 , Edited by admin on Sat Dec 16 04:51:54 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
SELECTIVE
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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%).
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NON-INHIBITOR -> METABOLIC ENZYME |
IC50
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INHIBITOR -> METABOLIC ENZYME |
LOW
Ki
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Lofexidine exposures were approximately 30% greater with co-administration of paroxetine a strong inhibitor of CYP2D6.
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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INHIBITOR -> METABOLIC ENZYME |
Ki
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK INHIBITOR
|
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Strong Inhibitors(2)
5-fold increase in AUC
or > 80% decrease in CL
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
Ki
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME |
N-demethylation of diphenhydramine is mainly catalyzed by CYP2D6 as a high-affinity P450 isozyme at a clinically relevant concentration.
MAJOR
|
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|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
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|
SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: O-demethylation
|
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|
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).
|
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SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: 2- and 8-Hydroxylation
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
Inhibition of bufuralol 1′-hydroxylation. Could be clinically relevant concentration in liver is within these values.
COMPETITIVE INHIBITOR
Ki
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
Pharmacological action: Tricyclic antidepressant drug (TCA)
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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.
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
WEAK INHIBITION
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
IC50
|
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SUBSTRATE -> METABOLIC ENZYME |
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
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INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
|
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Inhibits at clinically relevant concentrations.
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SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: N-demethylation
Pharmacological action: Phenothiazine antipsychotic
SUBSTRATE
Unidentified
|
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
WEAK INHIBITOR->METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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INHIBITOR -> METABOLIC ENZYME |
Interaction with CYP2D6 substrates is not expected to be clinically significant.
MINOR
IC50
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: Demethylatio
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: 2-Hydroxylation
|
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
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|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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NON-INHIBITOR -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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NON-INHIBITOR -> METABOLIC ENZYME |
IC50
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
Ki
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NON-SUBSTRATE -> METABOLIC ENZYME |
Intentionally designed to limit CYP2D6 based metabolism
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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INHIBITOR -> TARGET | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
2.1% conversion to M1
|
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SUBSTRATE -> METABOLIC ENZYME |
O-demethylation, mediated by CYP2D6 was greater in extensive metabolizers of CYP2D6 than in poor metabolizers
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME |
In vitro studies have shown that vilazodone is a moderate inhibitor of CYP2C19 and CYP2D6
|
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME |
Ki
|
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INHIBITOR -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
IN-VIVO
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
|
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INHIBITOR -> METABOLIC ENZYME |
MODERATE
|
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INHIBITOR -> METABOLIC ENZYME |
Eliglustat also exhibited time-dependent inhibition (TDI) of CYP2D6.
Ki
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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INHIBITOR -> METABOLIC ENZYME |
CYP2C8
IC50
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
IC50
|
||
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
WEAK
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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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.
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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TISSUE EXPRESSION -> PARENT | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
WEAK
|
||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Cobimetinib is a reversible inhibitor of CYP3A4 and CYP2D6 in vitro.
REVERSIBLE
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME |
Metabolizing reaction by CYP2D6: N-demethylation
|
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
In vitro, lumefantrine significantly inhibits the activity of CYP2D6 at therapeutic plasma concentrations
|
||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
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|
NON-SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
|
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|
INHIBITOR -> METABOLIC ENZYME |
POTENT
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
POTENT
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
IN-VITRO
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Molecular Formula | CHEMICAL |
|
||||
MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
|