U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Created
by admin
on Sat Jun 26 16:45:26 UTC 2021
Edited
by admin
on Sat Jun 26 16:45:26 UTC 2021
Protein Type ENZYME
Protein Sub Type CYTOCHROME P450
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
L9DP834D1P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CYTOCHROME P450 2C9
Common Name English
CYP2C9
Common Name English
CYTOCHROME P 450 MP-4
Common Name English
CYTOCHROME P 450 2C9
Common Name English
HUMAN CYTOCHROME P450 2C9
Common Name English
S-MEPHENYTOIN 4-HYDROXYLASE
Common Name English
LIMONENE 6-MONOOXYGENASE
Common Name English
Code System Code Type Description
FDA UNII
L9DP834D1P
Created by admin on Sat Jun 26 16:45:46 UTC 2021 , Edited by admin on Sat Jun 26 16:45:46 UTC 2021
PRIMARY
UNIPROT
P11712
Created by admin on Sat Jun 26 16:45:46 UTC 2021 , Edited by admin on Sat Jun 26 16:45:46 UTC 2021
PRIMARY
CAS
329978-01-0
Created by admin on Sat Jun 26 16:45:46 UTC 2021 , Edited by admin on Sat Jun 26 16:45:46 UTC 2021
PRIMARY
Related Record Type Details
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
ceritinib also inhibits CYP2C9 in vitro.
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Edaravone inhib it e d CYP2C9, BCRP, OAT3, and induced CYP1A2 in vitro.
NON-SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
INHIBITOR -> METABOLIC ENZYME
INDUCER -> TARGET
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided.
MODERATE
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
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
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides phenthoate
INHIBITOR -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides fenitrothion
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
IC50
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
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> 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.
INHIBITOR -> TARGET
MINOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Contribution of CYP2C9 to the total clearance of erdafitinib is estimated to be 39%
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
In the direct inhibition assays, upadacitinib inhibited CYP2C9 with an IC50 value of 40.3 ?M
IC50
INHIBITOR -> METABOLIC ENZYME
In vitro, ozenoxacin caused mild inhibition of CYP3A4 and CYP2C9 at high concentrations (?100 ?M).
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INDUCER -> METABOLIC ENZYME
Delafloxacin was a mild inducer (less than 2 fold) of CYP2C9 at a concentration of 100 ?M
INDUCER -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
Ki
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Ki
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
With the primary amine (SKF26754), the CYP2C9 reaction was the most inhibited.
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
POTENT
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
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 ?g/mL).
IC50
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
INHIBITOR -> METABOLIC ENZYME
WEAK
IC50
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides profenofos
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
MODERATE
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
CYP2C9 activity was extensively inhibited (more than 90% inhibition) by organophosphorus insecticides malathion
SUBSTRATE -> METABOLIC ENZYME
CYP1A2, CYP2C9, and CYP2C19 are involved in the metabolism of diphenhydramine as low-affinity P450 isozymes.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
NON-SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
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
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
INHIBITOR -> TARGET
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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.
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
WEAK
NON-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%).
SUBSTRATE -> METABOLIC ENZYME
TISSUE EXPRESSION -> PARENT
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL