Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Mon Mar 31 21:39:38 GMT 2025
by
admin
on
Mon Mar 31 21:39:38 GMT 2025
|
| Protein Type | ENZYME |
| Protein Sub Type | CYTOCHROME P450 |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
081I12ZA58
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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Common Name | English | ||
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Preferred 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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P33261
Created by
admin on Mon Mar 31 21:39:39 GMT 2025 , Edited by admin on Mon Mar 31 21:39:39 GMT 2025
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PRIMARY | |||
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391962-06-4
Created by
admin on Mon Mar 31 21:39:39 GMT 2025 , Edited by admin on Mon Mar 31 21:39:39 GMT 2025
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ALTERNATIVE | |||
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330589-90-7
Created by
admin on Mon Mar 31 21:39:39 GMT 2025 , Edited by admin on Mon Mar 31 21:39:39 GMT 2025
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PRIMARY | |||
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081I12ZA58
Created by
admin on Mon Mar 31 21:39:39 GMT 2025 , Edited by admin on Mon Mar 31 21:39:39 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
Ki
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Ki
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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 | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
MODERATE
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NON-INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
Zanubrutinib is a weak inducer of CYP3A4 and CYP2C19 in vivo.
WEAK
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
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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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INDUCER -> TARGET | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK
|
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|
SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE INHIBITION
IC50
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
CYP2C19 preferentially metabolized (R)-methadone,
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
|
INHIBITOR -> METABOLIC ENZYME | |||
|
NON-SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
|
||
|
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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|
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 |
|
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|
SUBSTRATE -> METABOLIC ENZYME |
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
CYP1A2, CYP2C9, and CYP2C19 are involved in the metabolism of diphenhydramine as low-affinity P450 isozymes.
|
||
|
INDUCER -> METABOLIC ENZYME |
POTENT
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
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INDUCER -> METABOLIC ENZYME |
POTENT
|
||
|
INHIBITOR -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
INHIBITOR -> METABOLIC ENZYME |
In vitro studies have shown that vilazodone is a moderate inhibitor of CYP2C19 and CYP2D6
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
Responsible for a drug interaction with clobazam. Mean increase in clozabam and N-desmethylclozabam levels was 60% and 500%, respectively, after 4 weeks of concomitant therapy.
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||
|
INHIBITOR -> METABOLIC ENZYME |
Pretomanid is a weak time-dependent inhibitor of CYP2C8 and CYP2C19.
TIME-DEPENDENT INHIBITION
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NON-INHIBITOR -> 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 | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
INDUCER -> METABOLIC ENZYME |
POTENT
|
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
INDUCER -> METABOLIC ENZYME |
POTENT
|
||
|
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 |
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IN VITRO
|
||
|
INHIBITOR -> METABOLIC ENZYME |
TIME-DEPENDENT INHIBITION
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
|
INHIBITOR -> METABOLIC ENZYME | |||
|
|
NON-INHIBITOR -> METABOLIC ENZYME |
IC50
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
|
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|
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
EXTENT PERCENTAGE
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
NON-INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> TARGET |
Ki
|
||
|
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INDUCER -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
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|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
Ospemifene is primarily metabolized by CYP3A4, 2C9, and 2C19 responsible for approximately 40 to 50%, ~25%, and ~25%, respectively, of its clearance.
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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NON-SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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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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INDUCER -> METABOLIC ENZYME | |||
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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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INDUCER -> METABOLIC ENZYME |
mRNA levels in at least 2 hepatocyte cultures. Up 10 micromolar OTESECONAZOLE
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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INHIBITOR -> METABOLIC ENZYME | |||
|
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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|
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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 |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
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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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INHIBITOR -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
SELECTIVE
|
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INHIBITOR -> METABOLIC ENZYME |
|
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
MIXED INHIBITION
MAJOR
Ki
|
||
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INHIBITOR -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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|
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
|
||
|
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0?20%), and FMO3 (0?33%) in vitro.
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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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INHIBITOR -> METABOLIC ENZYME |
Inhibits at clinically relevant concentrations.
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME |
|
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INHIBITOR -> METABOLIC ENZYME |
Moderate inhibitor
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
In vitro metabolism studies involving recombinant enzymes indicated that CYP3A4, CYP1A1, CYP3A5, CYP2C9, CYP2C19 and CYP2B6 were responsible for the oxidative metabolism of voxelotor.
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SUBSTRATE -> METABOLIC ENZYME |
|
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INDUCER -> METABOLIC ENZYME |
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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|
INHIBITOR -> TARGET |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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|
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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 | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
|
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| Heme binding | [1_435] | CYS | HEME-CYSTEINE (OXIDIZED) | G0HAF1JK3T |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
|