Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Mon Oct 21 19:44:35 UTC 2019
by
admin
on
Mon Oct 21 19:44:35 UTC 2019
|
Protein Type | ENZYME |
Protein Sub Type | CYTOCHROME P450 |
Sequence Origin | HUMAN |
Sequence Type | COMPLETE |
Record UNII |
L0423Z5LDW
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Record Status |
Validated (UNII)
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Record Version |
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-
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Code System | Code | Type | Description | ||
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P10632
Created by
admin on Mon Oct 21 19:44:35 UTC 2019 , Edited by admin on Mon Oct 21 19:44:35 UTC 2019
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PRIMARY | |||
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121225712
Created by
admin on Mon Oct 21 19:44:35 UTC 2019 , Edited by admin on Mon Oct 21 19:44:35 UTC 2019
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PRIMARY | |||
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330207-13-1
Created by
admin on Mon Oct 21 19:44:35 UTC 2019 , Edited by admin on Mon Oct 21 19:44:35 UTC 2019
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PRIMARY |
Related Record | Type | Details | ||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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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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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
LOW
Ki
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INHIBITOR -> METABOLIC ENZYME | |||
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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 | |||
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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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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
MODERATE
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||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
CYP2C8
IC50
|
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
MAJOR
Ki
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||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
Glasdegib is metabolized primarily by the CYP3A4 pathway, with minor contributions by CYP2C8 and UGT1A9
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
|
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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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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INHIBITOR -> METABOLIC ENZYME |
MAJOR
IC50
|
||
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> TARGET |
MINOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
|
||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
TISSUE EXPRESSION -> PARENT | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
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 |
Ki
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> 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.
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
In vivo, the sum of enzalutamide and M2 exposure was increased by 2.2-fold and 1.3-fold when it was co-administered with gemfibrozil (strong CYP2C8 inhibitor) or itraconazole (strong CYP3A4 inhibitor), respectively. If the co-administration of enzalutamide with a strong CYP2C8 inhibitor cannot be avoided, the daily enzalutamide dose should be reduced to 80 mg.
|
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
In vitro data suggests that avatrombopag weakly induces CYP2C8 and CYP2C9
WEAK
|
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METABOLIC ENZYME -> INHIBITOR | |||
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INDUCER -> 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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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> TARGET |
Ki
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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