Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 05:50:59 GMT 2023
by
admin
on
Sat Dec 16 05:50:59 GMT 2023
|
Protein Type | ENZYME |
Protein Sub Type | CYTOCHROME P450 |
Sequence Origin | HUMAN |
Sequence Type | COMPLETE |
Record UNII |
L9DP834D1P
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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 |
Code System | Code | Type | Description | ||
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L9DP834D1P
Created by
admin on Sat Dec 16 05:51:07 GMT 2023 , Edited by admin on Sat Dec 16 05:51:07 GMT 2023
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P11712
Created by
admin on Sat Dec 16 05:51:07 GMT 2023 , Edited by admin on Sat Dec 16 05:51:07 GMT 2023
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PRIMARY | |||
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329978-01-0
Created by
admin on Sat Dec 16 05:51:07 GMT 2023 , Edited by admin on Sat Dec 16 05:51:07 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
ceritinib also inhibits CYP2C9 in vitro.
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
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INHIBITOR -> METABOLIC ENZYME | |||
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INDUCER -> TARGET | |||
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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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INHIBITOR -> METABOLIC ENZYME |
POTENT
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SUBSTRATE -> METABOLIC ENZYME | |||
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Alosetron is metabolized by human microsomal cytochrome P450 (CYP), shown in vitro to involve enzymes 2C9 (30%), 3A4 (18%), and 1A2 (10%).
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides phenthoate
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INHIBITOR -> METABOLIC ENZYME |
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides fenitrothion
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INHIBITOR -> METABOLIC ENZYME |
POTENT
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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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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INHIBITOR -> TARGET |
MINOR
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Contribution of CYP2C9 to the total clearance of erdafitinib is estimated to be 39%
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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 |
WEAK
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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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INHIBITOR -> METABOLIC ENZYME |
In the direct inhibition assays, upadacitinib inhibited CYP2C9 with an IC50 value of 40.3 μM
IC50
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INHIBITOR -> METABOLIC ENZYME |
In vitro, ozenoxacin caused mild inhibition of CYP3A4 and CYP2C9 at high concentrations (≥100 μM).
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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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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
NINGETINIB M1 FORMATION
MINOR
Vmax
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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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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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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INDUCER -> METABOLIC ENZYME |
Delafloxacin was a mild inducer (less than 2 fold) of CYP2C9 at a concentration of 100 μM
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SUBSTRATE -> METABOLIC ENZYME |
Clearance of gliclazide in CYP2C9*2 and *3 was significantly reduced compared to the wild-type.
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Ki
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
Clearance of glimepiride CYP2C9*2 and *3 was significantly reduced compared to the wild-type.
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INDUCER -> 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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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 |
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
With the primary amine (SKF26754), the CYP2C9 reaction was the most inhibited.
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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INHIBITOR -> METABOLIC ENZYME |
POTENT
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INDUCER -> METABOLIC ENZYME |
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Not time dependent
IC50
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NON-INHIBITOR -> 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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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 |
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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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 |
IC50
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
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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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INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
in vitro studies utilizing human liver microsomes show that zafirlukast inhibits the cytochrome P450 CYP3A4 and CYP2C9 isoenzymes at concentrations close to the clinically achieved total plasma concentrations
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NON-INHIBITOR -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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NON-SUBSTRATE -> METABOLIC ENZYME |
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NON-INHIBITOR -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
Fidaxomicin and OP-1118 exhibited inhibitory potential for prominent intestinal CYP isoenzymes (CYP3A4, CYP2C9, and CYP2C19) in in vitro studies with human liver microsomes, based on estimated intestinal concentrations (fidaxomicin [I]2, 800 μg/mL).
IC50
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
POTENT
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INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
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INHIBITOR -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INHIBITOR -> METABOLIC ENZYME |
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides profenofos
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SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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INHIBITOR -> METABOLIC ENZYME |
MODERATE
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INHIBITOR -> METABOLIC ENZYME |
Edaravone inhib it e d CYP2C9, BCRP, OAT3, and induced CYP1A2 in vitro.
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides malathion
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SUBSTRATE -> METABOLIC ENZYME |
CYP1A2, CYP2C9, and CYP2C19 are involved in the metabolism of diphenhydramine as low-affinity P450 isozymes.
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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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NON-SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
IC50
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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 |
CYP2C9 genotype had a significant effect on the exposure of siponimod, with CYP2C9 *3/*3, CYP2C9 *1/*3, and CYP2C9 *2/*3 individuals having the largest effect.
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
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SUBSTRATE -> METABOLIC ENZYME |
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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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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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INDUCER -> METABOLIC ENZYME |
WEAK
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NON-INHIBITOR -> METABOLIC ENZYME | |||
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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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TISSUE EXPRESSION -> PARENT |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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Molecular Formula | CHEMICAL |
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