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

Approval Year

Unknown
149124
Substance Class Protein
Created
by admin
on Mon Mar 31 23:00:09 GMT 2025
Edited
by admin
on Mon Mar 31 23:00:09 GMT 2025
Protein Type ENZYME
Protein Sub Type CYTOCHROME P450
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
L0423Z5LDW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CYP-2C8
Preferred Name English
CYTOCHROME P450 2C8
Common Name English
HUMAN CYTOCHROME P450 2C8
Common Name English
CYTOCHROME P 450 2C8
Common Name English
CYP2C8
Common Name English
CYP2C8 (HUMAN)
Common Name English
Code System Code Type Description
UNIPROT
P10632
Created by admin on Mon Mar 31 23:00:09 GMT 2025 , Edited by admin on Mon Mar 31 23:00:09 GMT 2025
PRIMARY
CAS
330207-13-1
Created by admin on Mon Mar 31 23:00:09 GMT 2025 , Edited by admin on Mon Mar 31 23:00:09 GMT 2025
PRIMARY
FDA UNII
L0423Z5LDW
Created by admin on Mon Mar 31 23:00:09 GMT 2025 , Edited by admin on Mon Mar 31 23:00:09 GMT 2025
PRIMARY
Related Record Type Details
Structure of MALATHION
INHIBITOR -> METABOLIC ENZYME
Human hepatic CYP2C8 activities after incubation with different pesticides showed that CYP2C8 activities were inhibited extensively by malathion (100,90%).
Structure of TOZASERTIB
SUBSTRATE -> METABOLIC ENZYME
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of GRAZOPREVIR ANHYDROUS
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of VANOXERINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of VOXILAPREVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of DASABUVIR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of Selexipag
SUBSTRATE -> METABOLIC ENZYME
Structure of Resmetirom
INHIBITOR -> METABOLIC ENZYME
Structure of IMATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ROSIGLITAZONE
SUBSTRATE -> METABOLIC ENZYME
Structure of IPTACOPAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ZOPICLONE
SUBSTRATE -> METABOLIC ENZYME
Structure of SIPOGLITAZAR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of Resmetirom
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIFAMPIN
INDUCER -> METABOLIC ENZYME
Structure of TECOVIRIMAT
INHIBITOR -> METABOLIC ENZYME
MINOR
Structure of Dronedarone
INHIBITOR -> METABOLIC ENZYME
LOW
Ki
Structure of APOMORPHINE
SUBSTRATE -> METABOLIC ENZYME
Structure of Desloratadine
SUBSTRATE -> METABOLIC ENZYME
Structure of DUVELISIB
INHIBITOR -> METABOLIC ENZYME
Structure of OLACAFTOR
INHIBITOR -> METABOLIC ENZYME
Structure of SERATRODAST
SUBSTRATE -> METABOLIC ENZYME
Structure of VELPATASVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of LEVOMETHADONE
SUBSTRATE -> METABOLIC ENZYME
CYP2C8 contribution to the metabolism was smaller than that of CYP3A4.
Structure of ETRASIMOD
SUBSTRATE -> METABOLIC ENZYME
MAJOR
EXTENT PERCENTAGE
Structure of CERLAPIRDINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ENASIDENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of DOSIMERTINIB
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of SILIBININ A
SUBSTRATE -> METABOLIC ENZYME
Structure of Desloratadine
NON-INHIBITOR -> METABOLIC ENZYME
Structure of GLECAPREVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of REPAGLINIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of CLOPIDOGREL ACYL-.BETA.-D-GLUCURONIDE
INHIBITOR -> METABOLIC ENZYME
Structure of VECABRUTINIB
INHIBITOR -> METABOLIC ENZYME
Structure of JD-5037
INHIBITOR -> METABOLIC ENZYME
Structure of PHENOBARBITAL
INDUCER -> METABOLIC ENZYME
Structure of LONAFARNIB
SUBSTRATE -> METABOLIC ENZYME
Structure of AMIODARONE
SUBSTRATE -> METABOLIC ENZYME
Structure of EVATANEPAG
SUBSTRATE -> METABOLIC ENZYME
Structure of Taragarestrant
INHIBITOR -> METABOLIC ENZYME
Structure of AZD-1656
SUBSTRATE -> METABOLIC ENZYME
Structure of Isavuconazole
INDUCER -> METABOLIC ENZYME
Structure of ALVESPIMYCIN
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of Lurasidone
INHIBITOR -> METABOLIC ENZYME
MODERATE
Structure of Pralsetinib
INDUCER -> METABOLIC ENZYME
Structure of TAZAROTENIC ACID
SUBSTRATE -> METABOLIC ENZYME
Structure of PHENTHOATE
INHIBITOR -> METABOLIC ENZYME
Human hepatic CYP2C8 activities after incubation with different pesticides showed that CYP2C8 activities were inhibited extensively by phenthoate (100,90%).
Structure of JTE-151
INHIBITOR -> METABOLIC ENZYME
Structure of CENOBAMATE
INDUCER -> METABOLIC ENZYME
Structure of METHADONE
SUBSTRATE -> METABOLIC ENZYME
Involved in the metabolism of methadone, but its contribution to the metabolism of (R)-methadone was smaller than that of CYP3A4. For the metabolism of (S)-methadone, the roles of CYP2C8 and CYP3A4 appeared equal.
Structure of SEBETRALSTAT
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of Selexipag
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ORANTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of Teriflunomide
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of COBICISTAT
NON-INHIBITOR -> METABOLIC ENZYME
Structure of IROSUSTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of REGORAFENIB ANHYDROUS
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of SIMEPREVIR
INHIBITOR -> METABOLIC ENZYME
CYP2C8
IC50
Structure of BRANEBRUTINIB
INHIBITOR -> METABOLIC ENZYME
Structure of ELISMETREP
INHIBITOR -> METABOLIC ENZYME
Structure of ETHINYL ESTRADIOL
SUBSTRATE -> METABOLIC ENZYME
Structure of TRIMETHOPRIM
INHIBITOR -> METABOLIC ENZYME
MAJOR
Ki
Structure of Febuxostat
SUBSTRATE -> METABOLIC ENZYME
Structure of Isavuconazole
INHIBITOR -> METABOLIC ENZYME
Structure of Laselipag
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of METHOXYCHLOR
SUBSTRATE -> METABOLIC ENZYME
Structure of GLASDEGIB
SUBSTRATE -> METABOLIC ENZYME
Glasdegib is metabolized primarily by the CYP3A4 pathway, with minor contributions by CYP2C8 and UGT1A9
MINOR
Structure of TRICLABENDAZOLE SULFOXIDE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of CERIVASTATIN
SUBSTRATE -> METABOLIC ENZYME
Structure of ENCORAFENIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of Clascoterone
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
Structure of Carbamazepine
SUBSTRATE -> METABOLIC ENZYME
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
INHIBITOR -> METABOLIC ENZYME
Structure of CABAZITAXEL
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of RIOCIGUAT
SUBSTRATE -> METABOLIC ENZYME
Structure of Buprenorphine
SUBSTRATE -> METABOLIC ENZYME
Structure of Pralsetinib
INHIBITOR -> METABOLIC ENZYME
Structure of FLIBANSERIN
SUBSTRATE -> METABOLIC ENZYME
Structure of CHLOROQUINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIPRETINIB
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of LUSUTROMBOPAG
INHIBITOR -> TARGET
MINOR
Structure of DEFERASIROX
INHIBITOR -> METABOLIC ENZYME
WEAK
IC50
Structure of TUCATINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LOMITAPIDE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of ELAGOLIX
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of TEPOTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of AMODIAQUINE
SUBSTRATE -> METABOLIC ENZYME
Structure of BREXPIPRAZOLE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of ISTRADEFYLLINE
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of Ozanimod
SUBSTRATE -> METABOLIC ENZYME
Structure of LORLATINIB
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of PACLITAXEL
SUBSTRATE -> METABOLIC ENZYME
Structure of Eltrombopag
SUBSTRATE -> METABOLIC ENZYME
Structure of LICOFELONE
SUBSTRATE -> METABOLIC ENZYME
Structure of UMBRALISIB
INHIBITOR -> METABOLIC ENZYME
Structure of Miridesap
NON-INHIBITOR -> METABOLIC ENZYME
Structure of FINERENONE
SUBSTRATE -> METABOLIC ENZYME
Structure of Tuspetinib
INHIBITOR -> METABOLIC ENZYME
Structure of OTESECONAZOLE
INDUCER -> METABOLIC ENZYME
mRNA levels in at least 2 hepatocyte cultures. Up 10 micromolar OTESECONAZOLE
Structure of SARIZOTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of ABIRATERONE
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.
Structure of Relugolix
SUBSTRATE -> METABOLIC ENZYME
Structure of SILIBININ A
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of SIMEPREVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of PF-06835919
NON-INHIBITOR -> METABOLIC ENZYME
Structure of Lumateperone
SUBSTRATE -> METABOLIC ENZYME
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
SUBSTRATE -> METABOLIC ENZYME
Structure of TRIFAROTENE
SUBSTRATE -> METABOLIC ENZYME
HUMAN LIVER
TISSUE EXPRESSION -> PARENT
Structure of RETAPAMULIN
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of ENZALUTAMIDE
INHIBITOR -> METABOLIC ENZYME
Structure of IDELALISIB
INHIBITOR -> METABOLIC ENZYME
IN VITRO
Structure of ALDUMASTAT
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of TUCATINIB
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
Structure of IXAZOMIB
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%).
Structure of RIVOGLITAZONE
SUBSTRATE -> METABOLIC ENZYME
Structure of TAFENOQUINE
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of APIXABAN
NON-INHIBITOR -> METABOLIC ENZYME
Structure of MONTELUKAST
SUBSTRATE -> METABOLIC ENZYME
Structure of DABRAFENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of GS-563117
INHIBITOR -> METABOLIC ENZYME
Structure of BRIGATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ALECTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CHLORAMPHENICOL
NON-INHIBITOR -> METABOLIC ENZYME
Structure of Rifamycin
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.
Structure of OLODATEROL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of OXYMETAZOLINE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of TRICLABENDAZOLE SULFONE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of MOMELOTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ENZALUTAMIDE
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.
Structure of UAB-30
SUBSTRATE -> METABOLIC ENZYME
Structure of GEMFIBROZIL
INHIBITOR -> METABOLIC ENZYME
Structure of Migoprotafib
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
IC50
Structure of TRICLABENDAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of Tirbanibulin
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of MITAPIVAT
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.
Structure of LONAFARNIB
INHIBITOR -> METABOLIC ENZYME
Structure of AVATROMBOPAG
INDUCER -> METABOLIC ENZYME
In vitro data suggests that avatrombopag weakly induces CYP2C8 and CYP2C9
WEAK
Structure of LENVATINIB
INHIBITOR -> METABOLIC ENZYME
INHIBITOR
PLASMA
Structure of PROFENOFOS
INHIBITOR -> METABOLIC ENZYME
inhibitions between 59 and 84% were observed with profenofos
Structure of TAMATINIB
INDUCER -> METABOLIC ENZYME
Structure of MAVOGLURANT
SUBSTRATE -> METABOLIC ENZYME
Structure of Apalutamide
SUBSTRATE -> METABOLIC ENZYME
Structure of OTESECONAZOLE
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
IC50
Structure of AZILSARTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of CERALASERTIB
SUBSTRATE -> METABOLIC ENZYME
Structure of PRETOMANID
INHIBITOR -> METABOLIC ENZYME
Pretomanid is a weak time-dependent inhibitor of CYP2C8 and CYP2C19.
TIME-DEPENDENT INHIBITION
Structure of ELAGOLIX
INDUCER -> TARGET
Structure of RHINACANTHIN C
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of PEXIDARTINIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of VERINURAD
SUBSTRATE -> METABOLIC ENZYME
Structure of Belumosudil
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
Structure of ZIMLOVISERTIB
NON-INHIBITOR -> METABOLIC ENZYME
Structure of FENITROTHION
INHIBITOR -> METABOLIC ENZYME
inhibitions between 59 and 84% were observed with fenitrothion
Structure of ELAGOLIX
INHIBITOR -> TARGET
Ki

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
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) CHEMICAL
NIH
NCATS
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