Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 10:03:37 GMT 2023
by
admin
on
Sat Dec 16 10:03:37 GMT 2023
|
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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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 | ||
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Common Name | English |
Code System | Code | Type | Description | ||
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P10632
Created by
admin on Sat Dec 16 10:03:47 GMT 2023 , Edited by admin on Sat Dec 16 10:03:47 GMT 2023
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PRIMARY | |||
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330207-13-1
Created by
admin on Sat Dec 16 10:03:47 GMT 2023 , Edited by admin on Sat Dec 16 10:03:47 GMT 2023
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PRIMARY | |||
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L0423Z5LDW
Created by
admin on Sat Dec 16 10:03:47 GMT 2023 , Edited by admin on Sat Dec 16 10:03:47 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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INHIBITOR -> METABOLIC ENZYME |
Human hepatic CYP2C8 activities after incubation with different pesticides showed that CYP2C8 activities were inhibited extensively by malathion (100,90%).
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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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 |
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 |
MAJOR
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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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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 | |||
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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 |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
MAJOR
IC50
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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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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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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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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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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
MODERATE
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
Human hepatic CYP2C8 activities after incubation with different pesticides showed that CYP2C8 activities were inhibited extensively by phenthoate (100,90%).
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INDUCER -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
IC50
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NON-SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
Ki
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INHIBITOR -> METABOLIC ENZYME |
CYP2C8
IC50
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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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INHIBITOR -> METABOLIC ENZYME |
MAJOR
Ki
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Glasdegib is metabolized primarily by the CYP3A4 pathway, with minor contributions by CYP2C8 and UGT1A9
MINOR
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INHIBITOR -> METABOLIC ENZYME |
clascoterone cream, 1%, has no clinically meaningful effect on the PK of drugs metabolized by CYP 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 or 3A4.
IC50
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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NON-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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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> TARGET |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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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 |
MINOR
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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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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INHIBITOR -> 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 |
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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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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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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TISSUE EXPRESSION -> PARENT | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IN VITRO
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
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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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SUBSTRATE -> 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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INHIBITOR -> METABOLIC ENZYME |
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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 |
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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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INDUCER -> METABOLIC ENZYME |
More than two-fold increase in mRNA expression concentration dependence. Use of mitapivat should be avoided with substrates of CYP3A, CYP2B6, or CYP2C that have narrow therapeutic index.
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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INDUCER -> METABOLIC ENZYME |
In vitro data suggests that avatrombopag weakly induces CYP2C8 and CYP2C9
WEAK
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INHIBITOR -> METABOLIC ENZYME |
INHIBITOR
PLASMA
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INHIBITOR -> METABOLIC ENZYME |
inhibitions between 59 and 84% were
observed with profenofos
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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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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
IC50
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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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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INDUCER -> TARGET | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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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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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
inhibitions between 59 and 84% were
observed with fenitrothion
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INHIBITOR -> TARGET |
Ki
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Molecular Formula | CHEMICAL |
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MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) | CHEMICAL |
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