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

Approval Year

Unknown
127998
Substance Class Protein
Created
by admin
on Sat Dec 17 19:14:13 UTC 2022
Edited
by admin
on Sat Dec 17 19:14:13 UTC 2022
Protein Type ENZYME
Protein Sub Type CYTOCHROME P450
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
PUO0521HZV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CYTOCHROME P450 3A4
Common Name English
ALBENDAZOLE MONOOXYGENASE
Common Name English
CHOLESTEROL 25-HYDROXYLASE
Common Name English
CYP3A4
Common Name English
CYTOCHROME P 450 3A4
Common Name English
HUMAN CYTOCHROME P450 3A4
Common Name English
NIFEDIPINE OXIDASE
Common Name English
Code System Code Type Description
CAS
329736-03-0
Created by admin on Sat Dec 17 19:15:02 UTC 2022 , Edited by admin on Sat Dec 17 19:15:02 UTC 2022
PRIMARY
FDA UNII
PUO0521HZV
Created by admin on Sat Dec 17 19:15:02 UTC 2022 , Edited by admin on Sat Dec 17 19:15:02 UTC 2022
PRIMARY
EVMPD
SUB182775
Created by admin on Sat Dec 17 19:15:02 UTC 2022 , Edited by admin on Sat Dec 17 19:15:02 UTC 2022
PRIMARY
EC (ENZYME CLASS)
EC 1.14.13.67
Created by admin on Sat Dec 17 19:15:02 UTC 2022 , Edited by admin on Sat Dec 17 19:15:02 UTC 2022
PRIMARY
UNIPROT
P08684
Created by admin on Sat Dec 17 19:15:02 UTC 2022 , Edited by admin on Sat Dec 17 19:15:02 UTC 2022
PRIMARY
Related Record Type Details
Structure of TRAZODONE
SUBSTRATE -> METABOLIC ENZYME
Structure of VELIPARIB
SUBSTRATE -> METABOLIC ENZYME
Structure of OTESECONAZOLE
INHIBITOR -> METABOLIC ENZYME
Measured by midazolam 1?-hydroxylation; 42% inhibition at 10 micromolar.
IC50
Structure of VIBEGRON
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VERAPAMIL
SUBSTRATE -> METABOLIC ENZYME
Structure of TADALAFIL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of AVAPRITINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of LONAFARNIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TMC-558445
INHIBITOR -> TARGET
PHARMAKINETIC ENHANCER
Structure of SEGESTERONE ACETATE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CARBAMAZEPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of DILTIAZEM
INHIBITOR -> METABOLIC ENZYME
CYTOCHROME P450 3A12 (CANINE)
ANIMAL ORTHOLOG->HUMAN ORTHOLOG
Structure of LEFAMULIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IRINOTECAN
SUBSTRATE -> METABOLIC ENZYME
Structure of SIROLIMUS
SUBSTRATE -> METABOLIC ENZYME
Structure of APALUTAMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of TIRBANIBULIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LEMBOREXANT
INHIBITOR -> METABOLIC ENZYME
WEAK
TIME-DEPENDENT INHIBITION
Ki
Structure of EXEMESTANE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TENAPANOR
SUBSTRATE -> METABOLIC ENZYME
Tenapanor is a substrate of CYP3A4 and CYP3A5; however, none of the CYP enzymes was found to be responsible for ?25% of its overall elimination.
Structure of ALDUMASTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of IDELALISIB
INHIBITOR -> METABOLIC ENZYME
IN VITRO
Structure of EBASTINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PALONOSETRON
SUBSTRATE -> METABOLIC ENZYME
Structure of BOSENTAN ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FINERENONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of INDACATEROL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of AZD-7268
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ROLAPITANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIFAXIMIN
SUBSTRATE -> METABOLIC ENZYME
Structure of ALPELISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ALVESPIMYCIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ERIBULIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BORTEZOMIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ERAVACYCLINE
SUBSTRATE -> METABOLIC ENZYME
Structure of AMG-487
INHIBITOR -> METABOLIC ENZYME
Structure of BUPRENORPHINE
SUBSTRATE -> METABOLIC ENZYME
Structure of APIXABAN
SUBSTRATE -> METABOLIC ENZYME
Structure of TRIMETHOPRIM
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of REMIBRUTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FLUNITRAZEPAM
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of MACIMORELIN
SUBSTRATE -> METABOLIC ENZYME
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.
Structure of TEMSIROLIMUS
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of OZANIMOD
SUBSTRATE -> METABOLIC ENZYME
Structure of LOPERAMIDE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CIRTUVIVINT
SUBSTRATE -> METABOLIC ENZYME
Structure of WARFARIN, (R)-
SUBSTRATE -> METABOLIC ENZYME
Structure of ABIRATERONE ACETATE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of PRETOMANID
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TEMSAVIR
SUBSTRATE -> METABOLIC ENZYME
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
Structure of TAZEMETOSTAT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FLUTICASONE PROPIONATE
SUBSTRATE -> METABOLIC ENZYME
Structure of ANIDULAFUNGIN
NON-INHIBITOR -> METABOLIC ENZYME
Structure of ARTEMOTIL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of MEPERIDINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ORANTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ETRAVIRINE
INDUCER -> METABOLIC ENZYME
Structure of RETAPAMULIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CERITINIB
INHIBITOR -> METABOLIC ENZYME
Midazolam is the substrate.
Structure of BEXAROTENE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BERGAMOTTIN
INHIBITOR -> METABOLIC ENZYME
Unit K inact(min-1)
IRREVERSIBLE INHIBITOR
k(inactivation)
Structure of HYDROCORTISONE
SUBSTRATE -> METABOLIC ENZYME
Structure of GLECAPREVIR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of Tuspetinib
INHIBITOR -> METABOLIC ENZYME
Structure of LORCASERIN
SUBSTRATE -> METABOLIC ENZYME
Structure of MDE
MDE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IVOSIDENIB
INHIBITOR -> METABOLIC ENZYME
The following dose modifications are recommended: Strong CYP3A inhibitors: Reduce dose to 250 mg QD
Structure of RIPRETINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PEXIDARTINIB
INDUCER -> METABOLIC ENZYME
The induction of CYP3A4 enzyme (3.9 times) was lower than the mRNA increase (65 times), indicating possible time-dependent inhibition.
Structure of LOMITAPIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of ELIGLUSTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of APOMORPHINE
SUBSTRATE -> METABOLIC ENZYME
Structure of CARFILZOMIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of NELFINAVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of VOCLOSPORIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of AZELASTINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PF-00807925
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PRALSETINIB
INDUCER -> METABOLIC ENZYME
Structure of ALECTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of AXITINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ZOLPIDEM
SUBSTRATE -> METABOLIC ENZYME
Structure of ETHINYL ESTRADIOL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of GILTERITINIB
INHIBITOR -> METABOLIC ENZYME
Strong CYP3A inhibitor: co-administration of itraconazole, a strong CYP3A and P-gp inhibitor, increased gilteritinib systemic exposure by approximately 2.2- fold. Moderate CYP3A inhibitor: coadministration of fluconazole, a moderate CYP3A inhibitor, increased gilteritinib systemic exposure by approximately 1.4-fold.
IC50
Structure of ELUXADOLINE
INHIBITOR -> METABOLIC ENZYME
In an in-vitro study, eluxadoline appears to show time-dependent inhibition of CYP3A4 at 50 ?M, a concentration that can be achieved in the gut (Igut is estimated to be 700 ?M).
Structure of MEPHOBARBITAL
SUBSTRATE -> METABOLIC ENZYME
Structure of CLARITHROMYCIN
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of LOMITAPIDE
INHIBITOR -> METABOLIC ENZYME
Lomitapide is a weak in vivo CYP3A inhibitor.
WEAK
Structure of RIFAXIMIN
INDUCER -> METABOLIC ENZYME
Structure of IXABEPILONE
SUBSTRATE -> METABOLIC ENZYME
Structure of TINIDAZOLE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ERDAFITINIB
SUBSTRATE -> METABOLIC ENZYME
CYP3A4 in the total clearance of erdafitinib is estimated to be 20%.
Structure of RELUGOLIX
SUBSTRATE -> METABOLIC ENZYME
Co-administration with rifampin (P-gp and strong CYP3A inducer) decreased the AUC and Cmax of relugolix by 55% and 23%, respectively.
MAJOR
Structure of MILCICLIB
NON-SUBSTRATE -> METABOLIC ENZYME
high stability to human CYP4503A4 (85% remaining)
Structure of OTENABANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LITHOCHOLIC ACID
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IVOSIDENIB
SUBSTRATE -> METABOLIC ENZYME
The following dose modifications are recommended: Sensitive CYP3A substrates: Avoid concomitant use.
MAJOR
Structure of IDELALISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of BOCEPREVIR
SUBSTRATE -> METABOLIC ENZYME
moderate and strong inducers of CYP3A4 should not be co-administered due to the potential for loss of efficacy.
Structure of OLANZAPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of TEPOTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PHENYTOIN
INDUCER -> METABOLIC ENZYME
Structure of VINORELBINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CARVEDILOL
SUBSTRATE -> METABOLIC ENZYME
Structure of REMIBRUTINIB
INHIBITOR -> METABOLIC ENZYME
Structure of ISTRADEFYLLINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DACLATASVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of EBRACTEOLATA COMPOUND B
SUBSTRATE -> METABOLIC ENZYME
Structure of EAPB-0203
SUBSTRATE -> METABOLIC ENZYME
Structure of CYCLOBENZAPRINE
SUBSTRATE -> METABOLIC ENZYME
Structure of MIDAZOLAM
SUBSTRATE -> METABOLIC ENZYME
Structure of COBICISTAT
INHIBITOR -> METABOLIC ENZYME
Structure of VORAPAXAR
SUBSTRATE -> METABOLIC ENZYME
Structure of VORICONAZOLE
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
Structure of TEGILERIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of BOCEPREVIR
INHIBITOR -> METABOLIC ENZYME
sensitive substrates of CYP3A4 with a narrow therapeutic index should not be coadministered.
STRONG
Structure of TEMSIROLIMUS
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TAFAMIDIS
INDUCER -> METABOLIC ENZYME
Tafamidis induced CYP3A4 in vitro with an EC50 of 28 ?M.
EC50
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 TESTOSTERONE
SUBSTRATE -> METABOLIC ENZYME
Structure of RELUGOLIX
INDUCER -> METABOLIC ENZYME
Structure of DELAVIRDINE
INHIBITOR -> METABOLIC ENZYME
Structure of VERINURAD
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CLOPIDOGREL
METABOLIC ENZYME -> SUBSTRATE
Structure of GALANTAMINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of NALOXEGOL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CHLORPYRIFOS
SUBSTRATE -> METABOLIC ENZYME
Structure of NEFAZODONE
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of TELITHROMYCIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIVOGLITAZONE
SUBSTRATE -> METABOLIC ENZYME
Structure of TERFENADINE
SUBSTRATE -> METABOLIC ENZYME
Structure of CYCLOSPORINE
SUBSTRATE -> METABOLIC ENZYME
Structure of DABRAFENIB
INDUCER -> METABOLIC ENZYME
Structure of MIDAZOLAM
INHIBITOR -> METABOLIC ENZYME
Structure of ENCORAFENIB
INDUCER -> METABOLIC ENZYME
IC50
Structure of ETORICOXIB
SUBSTRATE -> METABOLIC ENZYME
Structure of TICAGRELOR
SUBSTRATE -> METABOLIC ENZYME
Structure of AVATROMBOPAG
SUBSTRATE -> METABOLIC ENZYME
Structure of Erythromycin
SUBSTRATE -> METABOLIC ENZYME
Structure of TELITHROMYCIN
INDUCER -> METABOLIC ENZYME
POTENT
Structure of ZONISAMIDE
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.
MAJOR
Structure of VOXELOTOR
INHIBITOR -> METABOLIC ENZYME
Structure of DASATINIB ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LONAFARNIB
INHIBITOR -> METABOLIC ENZYME
Lonafarnib is a potent CYP3A time-dependent and mechanism-based inhibitor.
TIME-DEPENDENT INHIBITION
POTENCY
Structure of METHADONE
SUBSTRATE -> METABOLIC ENZYME
CYP3A4 showed no preference between the two enantiomers
Structure of ISAVUCONAZOLE
INHIBITOR -> METABOLIC ENZYME
Structure of ULIPRISTAL ACETATE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BUFOGENIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ANTIPYRINE
SUBSTRATE -> METABOLIC ENZYME
Structure of LETERMOVIR
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of DESMETHYL DABRAFENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of EPLERENONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TAPINAROF
SUBSTRATE -> METABOLIC ENZYME
Low systematic exposure
Structure of TAMATINIB
INHIBITOR -> METABOLIC ENZYME
Structure of OPROZOMIB
SUBSTRATE -> METABOLIC ENZYME
Structure of MECLIZINE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of DECERNOTINIB
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
Structure of LAQUINIMOD
SUBSTRATE -> METABOLIC ENZYME
Structure of IMIDAFENACIN
SUBSTRATE -> METABOLIC ENZYME
Structure of SELPERCATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of RESVERATROL
INHIBITOR -> METABOLIC ENZYME
6?-hydroxylation of testosterone
IC50
Structure of ALOGLIPTIN
SUBSTRATE -> METABOLIC ENZYME
Structure of GNE-0877
INDUCER -> METABOLIC ENZYME
Structure of AVANAFIL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of OZENOXACIN
INHIBITOR -> METABOLIC ENZYME
In vitro, ozenoxacin caused mild inhibition of CYP3A4 and CYP2C9 at high concentrations (?100 ?M).
Structure of MORPHOTHIADINE
INDUCER -> METABOLIC ENZYME
strong CYP3A4 induction in a concentration-dependent manner
MAY BE CLINICALLY SIGNIFICANT
Structure of ALMOTRIPTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of SONIDEGIB
NON-INDUCER -> METABOLIC ENZYME
compared to positive controls
Structure of NOMIFENSINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DEXTROMETHORPHAN
SUBSTRATE -> METABOLIC ENZYME
Structure of SOTORASIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ZIMLOVISERTIB
NON-INHIBITOR -> METABOLIC ENZYME
Structure of GDC-0425
SUBSTRATE -> METABOLIC ENZYME
Structure of ZAFIRLUKAST
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.
Structure of LIQUIRITIGENIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ESOMEPRAZOLE
SUBSTRATE -> TARGET
Structure of NORTILIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of NALMEFENE
SUBSTRATE -> METABOLIC ENZYME
Structure of Hepenofovir
SUBSTRATE -> METABOLIC ENZYME
Structure of BUDESONIDE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of EVATANEPAG
SUBSTRATE -> METABOLIC ENZYME
Structure of COPANLISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of DIAZEPAM
SUBSTRATE -> METABOLIC ENZYME
Structure of ISAVUCONAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of OSILODROSTAT
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITION
Structure of ILAPRAZOLE
SUBSTRATE -> METABOLIC ENZYME
HUMAN LIVER
TISSUE EXPRESSION -> PARENT
Structure of LAROTRECTINIB
INHIBITOR -> METABOLIC ENZYME
Coadministration of multiple doses of larotrectinib with a sensitive CYP3A4 substrate (midazolam) increased the AUCinf and Cmax of midazolam by 1.7-fold as compared to midazolam administered alone.
Structure of LENVATINIB
INHIBITOR -> METABOLIC ENZYME
Time-dependent inhibition. significant effect with other drugs which are substrate of CYP3A4 at clinical dose of Lenvatinib
MAJOR
PLASMA
Structure of RIMEGEPANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DPA-714
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of SEMAGACESTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of IFOSFAMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of POMALIDOMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of DIETHYLTOLUAMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of SERATRODAST
SUBSTRATE -> METABOLIC ENZYME
Structure of MIFEPRISTONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of GILTERITINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of DIENOGEST
SUBSTRATE -> METABOLIC ENZYME
Structure of Tamnorzatinib
SUBSTRATE -> METABOLIC ENZYME
Structure of ENDOSULFAN I
SUBSTRATE -> METABOLIC ENZYME
Structure of CERLAPIRDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of CHLORAMPHENICOL
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
Structure of ESKETAMINE
SUBSTRATE -> METABOLIC ENZYME
Structure of NEVIRAPINE
INHIBITOR -> METABOLIC ENZYME
Structure of ALOSETRON
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
Structure of SELEGILINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of MIDOMAFETAMINE
SUBSTRATE -> METABOLIC ENZYME
Structure of RGH-618
INDUCER -> METABOLIC ENZYME
Structure of CLOBAZAM
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ELAGOLIX
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CENOBAMATE
SUBSTRATE -> METABOLIC ENZYME
Structure of ENASIDENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CONIVAPTAN
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of SARIZOTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of LICOFELONE
SUBSTRATE -> METABOLIC ENZYME
Structure of MOMELOTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of 2-AMINOTHIAZOLOBENZAZEPINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ILOPERIDONE
SUBSTRATE -> METABOLIC ENZYME
Structure of BICTEGRAVIR
SUBSTRATE -> METABOLIC ENZYME
Coadministration of BIC (given without F/TAF) with rifampin decreased the mean BIC Cmax and AUC by 28% and 75%, respectively.
Structure of PROADIFEN
INHIBITOR -> METABOLIC ENZYME
SELECTIVE
Structure of MOTESANIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DOMPERIDONE
SUBSTRATE -> METABOLIC ENZYME
TROGLITAZONE
INDUCER -> METABOLIC ENZYME
Structure of DPC-963
SUBSTRATE -> METABOLIC ENZYME
Structure of PRALSETINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TELAPREVIR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ESTRADIOL
SUBSTRATE -> METABOLIC ENZYME
Structure of 20(S)-GINSENOSIDE RH2
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DESFESOTERODINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BIIB021
SUBSTRATE -> METABOLIC ENZYME
Structure of PEXIDARTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of SITAGLIPTIN
SUBSTRATE -> METABOLIC ENZYME
Structure of PANOBINOSTAT
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Structure of PACLITAXEL
INDUCER -> METABOLIC ENZYME
Structure of VORICONAZOLE
INHIBITOR -> METABOLIC ENZYME
Structure of FIDAXOMICIN
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
Structure of FLINDOKALNER
SUBSTRATE -> METABOLIC ENZYME
Structure of FLUCONAZOLE
INHIBITOR -> METABOLIC ENZYME
Structure of AVAPRITINIB
INHIBITOR -> METABOLIC ENZYME
In vitro, avapritinib is a time-dependent inhibitor as well as an inducer of CYP3A.
TIME-DEPENDENT INHIBITION
Ki
Structure of (2-(4-METHOXY-3-PHENETHYLOXY-PHENYL)-ETHYL)-DIPROPYL-AMINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DUVELISIB
INHIBITOR -> METABOLIC ENZYME
Structure of ZANUBRUTINIB
INDUCER -> METABOLIC ENZYME
Zanubrutinib is a weak inducer of CYP3A4 and CYP2C19 in vivo.
WEAK
Structure of KRO-105714
SUBSTRATE -> METABOLIC ENZYME
Structure of PACLITAXEL
SUBSTRATE -> METABOLIC ENZYME
Structure of Desloratadine
INHIBITOR -> METABOLIC ENZYME
WEAK
Structure of Desloratadine
SUBSTRATE -> METABOLIC ENZYME
Structure of CERIVASTATIN
SUBSTRATE -> METABOLIC ENZYME
Structure of LUMEFANTRINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ODANACATIB
SUBSTRATE -> METABOLIC ENZYME
Structure of PEXIDARTINIB
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of Roflumilast
SUBSTRATE -> METABOLIC ENZYME
Structure of CJ-13610
SUBSTRATE -> METABOLIC ENZYME
Structure of TERIFLUNOMIDE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of OSU-6162
SUBSTRATE -> METABOLIC ENZYME
Structure of LY-2623091
SUBSTRATE -> METABOLIC ENZYME
Structure of SELICICLIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CYCLOHEXANAMINE, N-(3-ETHOXYPROPYL)-1-PHENYL-
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of Orbitazine
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FERROQUINE
SUBSTRATE -> METABOLIC ENZYME
Structure of CP-199331
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TEZACAFTOR
SUBSTRATE -> METABOLIC ENZYME
Structure of FLORBETABEN F-18
SUBSTRATE -> METABOLIC ENZYME
Structure of ALFUZOSIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIBOCICLIB
SUBSTRATE -> METABOLIC ENZYME
IVERMECTIN
SUBSTRATE -> METABOLIC ENZYME
Structure of ERIBULIN
INHIBITOR -> METABOLIC ENZYME
Eribulin inhibited CYP3A4 activity with an apparent inhibition constant (Ki) value ranging from 3 ?M to 30 ?M (2190 ng/mL to 21,900 ng/mL), and the inhibition was demonstrated to be reversible and competitive.
Ki
Structure of BRIGATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of DARUNAVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of MICONAZOLE
INHIBITOR -> METABOLIC ENZYME
Structure of RIVOCERANIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FELODIPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of DOCETAXEL ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
Structure of Nirmatrelvir
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Structure of NIMETAZEPAM
SUBSTRATE -> METABOLIC ENZYME
Structure of LETROZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of RUFINAMIDE
INDUCER -> METABOLIC ENZYME
WEAK
Structure of PIMECROLIMUS
SUBSTRATE -> METABOLIC ENZYME
Structure of ABT-384
SUBSTRATE -> METABOLIC ENZYME
Structure of ZILEUTON
SUBSTRATE -> METABOLIC ENZYME
Structure of AMBRISENTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of NINTEDANIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CINOBUFAGIN
SUBSTRATE -> METABOLIC ENZYME
Structure of PRIMIDONE
INDUCER -> METABOLIC ENZYME
Structure of PONESIMOD
SUBSTRATE -> METABOLIC ENZYME
Structure of TICAGRELOR
INHIBITOR -> METABOLIC ENZYME
WEAK
Structure of Linvencorvir
SUBSTRATE -> METABOLIC ENZYME
Structure of SUFENTANIL
SUBSTRATE -> METABOLIC ENZYME
Structure of SILDENAFIL
SUBSTRATE -> METABOLIC ENZYME
Structure of ARTEMETHER
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IXAZOMIB
SUBSTRATE -> METABOLIC ENZYME
CYP 3A CONTRIBUTES FOR 42% OF IXAZOMIB METABOLISM
MAJOR
Structure of LESINURAD
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of VORTIOXETINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PITOLISANT
SUBSTRATE -> METABOLIC ENZYME
Structure of PALIPERIDONE
SUBSTRATE -> METABOLIC ENZYME
Structure of DPA-714 F-18
SUBSTRATE -> METABOLIC ENZYME
Structure of COBIMETINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CANNABIDIOL
SUBSTRATE -> METABOLIC ENZYME
Structure of TG-100435
SUBSTRATE -> METABOLIC ENZYME
Structure of VINCRISTINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PAROXETINE
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of VILANTEROL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of NETUPITANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ENCORAFENIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TOLTERODINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ESZOPICLONE
SUBSTRATE -> METABOLIC ENZYME
Structure of ENZALUTAMIDE
INHIBITOR -> METABOLIC ENZYME
Structure of RIFAPENTINE
INDUCER -> METABOLIC ENZYME
Structure of RIFABUTIN
INDUCER -> METABOLIC ENZYME
Structure of NALDEMEDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of TASIMELTEON
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ENCEQUIDAR
SUBSTRATE -> METABOLIC ENZYME
Structure of CINACALCET
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TZB-30878
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VOXILAPREVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of EVIFACOTREP
SUBSTRATE -> METABOLIC ENZYME
Structure of MITAPIVAT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIMONABANT
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Structure of BPR-1K871
SUBSTRATE -> METABOLIC ENZYME
Structure of DUTASTERIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of METHOXYCHLOR
SUBSTRATE -> METABOLIC ENZYME
Structure of RUCAPARIB
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
Structure of ROKITAMYCIN
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of FENTANYL
SUBSTRATE -> METABOLIC ENZYME
Structure of NEBIVOLOL
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of UMBRALISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of EPINASTINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PANOBINOSTAT
SUBSTRATE -> METABOLIC ENZYME
The fraction metabolized through CYP3A accounts for approximately 40% of the total hepatic panobinostat elimination.
Structure of CRISABOROLE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of QUETIAPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of ESAXERENONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VARDENAFIL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IRUPLINALKIB
SUBSTRATE -> METABOLIC ENZYME
Structure of BENIDIPINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BUTYLPHTHALIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of ENCEQUIDAR
NON-INHIBITOR -> METABOLIC ENZYME
Structure of AMG-487
SUBSTRATE -> METABOLIC ENZYME
Structure of CEVIMELINE
SUBSTRATE -> METABOLIC ENZYME
Structure of ALDUMASTAT
INDUCER -> METABOLIC ENZYME
Structure of GRAZOPREVIR ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
Structure of CLINDAMYCIN
SUBSTRATE -> METABOLIC ENZYME
Structure of Plogosertib
SUBSTRATE -> METABOLIC ENZYME
Structure of IBRUTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of TOFACITINIB
NON-INHIBITOR -> METABOLIC ENZYME
NO INHIBITION AT 160 TIMES CMAX
Structure of CENOBAMATE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ETRAVIRINE
SUBSTRATE -> METABOLIC ENZYME
Structure of DUVELISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of AVAPRITINIB
INDUCER -> METABOLIC ENZYME
In vitro, avapritinib is a time-dependent inhibitor as well as an inducer of CYP3A.
Structure of Maraviroc
SUBSTRATE -> METABOLIC ENZYME
Structure of NIFEDIPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of OLACAFTOR
INDUCER -> METABOLIC ENZYME
Structure of SULFINPYRAZONE
INDUCER -> METABOLIC ENZYME
Structure of NELONICLINE
SUBSTRATE -> METABOLIC ENZYME
10% conversion to M1
Structure of ELEXACAFTOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of BELINOSTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of VECABRUTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ESOMEPRAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of CICLESONIDE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PALBOCICLIB
SUBSTRATE -> METABOLIC ENZYME
Structure of (+)-?-Dihydrotetrabenazine
SUBSTRATE -> METABOLIC ENZYME
Structure of Colchicine
SUBSTRATE -> METABOLIC ENZYME
APICAL
Structure of LAPATINIB
INHIBITOR -> METABOLIC ENZYME
Lapatinib is a mechanism-based inactivator of CYP3A4, most likely via the formation and further oxidation of its O-dealkylated metabolite to a quinoneimine that covalently modifies the CYP3A4 apoprotein and/or heme moiety.
TIME-DEPENDENT INHIBITION
Structure of TILDACERFONT
SUBSTRATE -> METABOLIC ENZYME
Structure of PF-06282999
INDUCER -> METABOLIC ENZYME
MODERATE INDUCER THROUGH MEDIATED BY THE PREGNANE X RECEPTOR
Structure of RITONAVIR
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of SKF-8742
INHIBITOR -> METABOLIC ENZYME
Structure of PHENOBARBITAL
INDUCER -> METABOLIC ENZYME
Structure of LENVATINIB
SUBSTRATE -> METABOLIC ENZYME
Predicted no effect with other CYP2C8 substrates at clinical dose of Lenvatinib
Structure of LORLATINIB
INDUCER -> METABOLIC ENZYME
Structure of PRACINOSTAT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIOCIGUAT
SUBSTRATE -> METABOLIC ENZYME
Structure of MKC-963
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RIFAMPIN
INDUCER -> METABOLIC ENZYME
Structure of NIROGACESTAT
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of EZLOPITANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of SONIDEGIB
SUBSTRATE -> METABOLIC ENZYME
metabolism by CYP3A4 (at least 29% of its overall metabolism); Ketoconazole(CYP 3A4 inhibition) increased sonidegib exposure 2.2-fold;Rifampin (CYP 3A4 induction) reduced exposure by 72%
Structure of ZOPICLONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PIMAVANSERIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PRUCALOPRIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of CAPMATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of LAROTRECTINIB
INDUCER -> METABOLIC ENZYME
Structure of EDOXABAN
SUBSTRATE -> METABOLIC ENZYME
CYTOCHROME P450 1A2 (CANINE)
ANIMAL ORTHOLOG->HUMAN ORTHOLOG
Structure of L-738372
SUBSTRATE -> METABOLIC ENZYME
Structure of IMRECOXIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LEUCOMYCIN A7
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of BUPIVACAINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of REBOXETINE
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of SIPONIMOD
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of LORLATINIB
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Ki
Structure of ATAZANAVIR
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
Structure of CHLOROQUINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IVOSIDENIB
INDUCER -> METABOLIC ENZYME
The following dose modifications are recommended: Strong CYP3A inducers: Avoid concomitant use.
Structure of DESVENLAFAXINE
SUBSTRATE -> METABOLIC ENZYME
Structure of BALOXAVIR
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of ANACETRAPIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of EVEROLIMUS
SUBSTRATE -> METABOLIC ENZYME
Structure of TRIFAROTENE
SUBSTRATE -> METABOLIC ENZYME
Structure of PEXACERFONT
SUBSTRATE -> METABOLIC ENZYME
Structure of OMEPRAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of LUMACAFTOR
INDUCER -> METABOLIC ENZYME
Lumacaftor is a strong inducers of CYP3A4
Structure of VISMODEGIB
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of OSILODROSTAT
SUBSTRATE -> METABOLIC ENZYME
Structure of LUMATEPERONE
SUBSTRATE -> METABOLIC ENZYME
Structure of U-48800
SUBSTRATE -> METABOLIC ENZYME
Structure of BREXPIPRAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of CASOPITANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CYCLOPHOSPHAMIDE ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
Structure of GOSOGLIPTIN
SUBSTRATE -> METABOLIC ENZYME
Structure of CYCLOHEXANAMINE, N-(2-ETHOXYETHYL)-1-PHENYL-
SUBSTRATE -> METABOLIC ENZYME
Structure of LURBINECTEDIN
SUBSTRATE -> METABOLIC ENZYME
Structure of AMIODARONE
SUBSTRATE -> METABOLIC ENZYME
Structure of ELBASVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of VALDECOXIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of NERATINIB
NON-INHIBITOR -> METABOLIC ENZYME
Structure of TIPRANAVIR
SUBSTRATE -> METABOLIC ENZYME
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
Structure of IVACAFTOR
SUBSTRATE -> METABOLIC ENZYME
In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A.
MAJOR
Structure of GRAZOPREVIR ANHYDROUS
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of CAPRAVIRINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VONOPRAZAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DARUNAVIR
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of DELAVIRDINE
INDUCER -> METABOLIC ENZYME
Structure of OLICERIDINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ABIRATERONE
SUBSTRATE -> METABOLIC ENZYME
Structure of TIVOZANIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of TUCATINIB
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
Structure of BARICITINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of LINAGLIPTIN
SUBSTRATE -> METABOLIC ENZYME
Linagliptin co-administration with P-gp and CYP 3A4 inducers may reduce its efficacy because of lower linagliptin exposures; therefore, it is strongly recommended to use the alternative treatments when it is to be co- administered with P-gp or CYP 3A4 inducers.
Structure of BUSPIRONE
SUBSTRATE -> METABOLIC ENZYME
Structure of ARGATROBAN ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
Structure of TRIAZOLAM
SUBSTRATE -> METABOLIC ENZYME
Structure of CANAGLIFLOZIN ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
CYP3A4-mediated (oxidative) metabolism of canagliflozin is minimal (approximately 7%) in humans.
MINOR
Structure of REMIBRUTINIB
INDUCER -> METABOLIC ENZYME
Structure of TILIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of VALSPODAR
SUBSTRATE -> METABOLIC ENZYME
Structure of E-NORENDOXIFEN
INHIBITOR -> METABOLIC ENZYME
E-Norendoxifen inhibited CYP3A4 3.7-fold more potently than Z-norendoxifen.
Structure of PRASTERONE
SUBSTRATE -> METABOLIC ENZYME
Structure of LEMBOREXANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of UBROGEPANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of OPK-88004
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DAROLUTAMIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of GABAPENTIN ENACARBIL
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of DACOMITINIB ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
IN-VITRO
Structure of NERATINIB
NON-INDUCER -> METABOLIC ENZYME
Structure of ANANDAMIDE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LERSIVIRINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of FEDRATINIB
SUBSTRATE -> METABOLIC ENZYME
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0?20%), and FMO3 (0?33%) in vitro.
Structure of BENZAMIDE, N-CYCLOPROPYL-3-(5-((2-FLUORO-4-IODOPHENYL)AMINO)-3,4,6,7-TETRAHYDRO-6,8-DIMETHYL-2,4,7-TRIOXOPYRIDO(4,3-D)PYRIMIDIN-1(2H)-YL)-
SUBSTRATE -> METABOLIC ENZYME
Structure of ANIDULAFUNGIN
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of DELAFLOXACIN
INDUCER -> METABOLIC ENZYME
Delafloxacin was a mild inducer (less than 2 fold) of CYP3A4 at a clinically relevant concentration.
Structure of VILAZODONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of IVACAFTOR CARBOXYLATE
INDUCER -> METABOLIC ENZYME
Strong Inducer
Structure of INAVOLISIB
SUBSTRATE -> METABOLIC ENZYME
Structure of OLAPARIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LETERMOVIR
INHIBITOR -> METABOLIC ENZYME
Structure of O-DEALKYLATED LAPATINIB
INHIBITOR -> METABOLIC ENZYME
Lapatinib is a mechanism-based inactivator of CYP3A4, most likely via the formation and further oxidation of its O-dealkylated metabolite to a quinoneimine that covalently modifies the CYP3A4 apoprotein and/or heme moiety
Structure of Nirmatrelvir
SUBSTRATE -> METABOLIC ENZYME
Structure of DIHYDROXYBERGAMOTTIN
INHIBITOR -> METABOLIC ENZYME
IRREVERSIBLE INHIBITOR
Structure of CENOBAMATE
INDUCER -> METABOLIC ENZYME
Structure of CLOBAZAM
INDUCER -> METABOLIC ENZYME
Structure of OLAPARIB
INHIBITOR -> METABOLIC ENZYME
Inhibitor at higher concentrations than are clinically achieved.
MINOR
Structure of CLARITHROMYCIN
INDUCER -> METABOLIC ENZYME
Structure of ATORVASTATIN
SUBSTRATE -> METABOLIC ENZYME
Structure of RABEPRAZOLE SODIUM
SUBSTRATE -> METABOLIC ENZYME
Structure of DASATINIB ANHYDROUS
INHIBITOR -> METABOLIC ENZYME
In human liver microsomes, dasatinib was a weak time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
Structure of ABEMACICLIB
SUBSTRATE -> METABOLIC ENZYME
Structure of SELINEXOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ALISKIREN
SUBSTRATE -> METABOLIC ENZYME
Structure of TRAMADOL
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of 21-DESACETYLDEFLAZACORT
SUBSTRATE -> METABOLIC ENZYME
Structure of DOSIMERTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of LUSUTROMBOPAG
INHIBITOR -> TARGET
MINOR
Structure of VANDETANIB
SUBSTRATE -> METABOLIC ENZYME
Structure of NERATINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ISAVUCONAZOLE
INDUCER -> METABOLIC ENZYME
Structure of SIMVASTATIN
SUBSTRATE -> METABOLIC ENZYME
Structure of HYDROXYPROGESTERONE CAPROATE
SUBSTRATE -> METABOLIC ENZYME
Structure of PERAMPANEL
SUBSTRATE -> METABOLIC ENZYME
Structure of CITALOPRAM
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
Structure of APROCITENTAN
INDUCER -> METABOLIC ENZYME
Both ACT-064992 and ACT-132577 can induce CYP3A4 enzymes in vitro.
Structure of SILIBININ A
INHIBITOR -> METABOLIC ENZYME
IC50
Structure of ACALABRUTINIB
SUBSTRATE -> METABOLIC ENZYME
Structure of NORENDOXIFEN
INHIBITOR -> METABOLIC ENZYME
E-Norendoxifen inhibited CYP3A4 3.7-fold more potently than Z-norendoxifen.
Structure of IMATINIB
SUBSTRATE -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
Structure of CERALASERTIB
SUBSTRATE -> METABOLIC ENZYME
Structure of ATAZANAVIR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VECABRUTINIB
INHIBITOR -> METABOLIC ENZYME
Structure of TOLVAPTAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VERAPAMIL
INHIBITOR -> METABOLIC ENZYME
Structure of QUINIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of CLOTRIMAZOLE
INDUCER -> METABOLIC ENZYME
Structure of TICLOPIDINE
SUBSTRATE -> METABOLIC ENZYME
Structure of ZANUBRUTINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VERUBECESTAT
NON-INHIBITOR -> METABOLIC ENZYME
Structure of SAQUINAVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of OLACAFTOR
SUBSTRATE -> METABOLIC ENZYME
Structure of ENZALUTAMIDE
INDUCER -> METABOLIC ENZYME
Therefore, co-administration of enzalutamide with CYP3A4, 2C9, and 2C19 substrates with a narrow therapeutic index should be avoided
STRONG
Structure of VERUBECESTAT
NON-INDUCER -> METABOLIC ENZYME
Structure of PEMIGATINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ELIGLUSTAT
INHIBITOR -> METABOLIC ENZYME
Ki
Structure of CJ-12458
SUBSTRATE -> METABOLIC ENZYME
Structure of Valbenazine
SUBSTRATE -> METABOLIC ENZYME
Structure of BRILAROXAZINE
SUBSTRATE -> METABOLIC ENZYME
Structure of NORQUETIAPINE
SUBSTRATE -> METABOLIC ENZYME
Structure of INDINAVIR ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VK-2809
SUBSTRATE -> METABOLIC ENZYME
Structure of SKF-26754A
INHIBITOR -> METABOLIC ENZYME
Structure of MIVEBRESIB
SUBSTRATE -> METABOLIC ENZYME
Structure of CHOLIC ACID
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RANOLAZINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ALPRAZOLAM
SUBSTRATE -> METABOLIC ENZYME
Structure of DELAVIRDINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of UMBRALISIB
INHIBITOR -> METABOLIC ENZYME
Structure of ALFENTANIL
SUBSTRATE -> METABOLIC ENZYME
IN VITRO
Structure of CISAPRIDE
SUBSTRATE -> METABOLIC ENZYME
Structure of LURASIDONE
INHIBITOR -> METABOLIC ENZYME
MODERATE
Structure of OXYMETAZOLINE
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of BEROTRALSTAT
INHIBITOR -> METABOLIC ENZYME
MODERATE
Structure of LOVASTATIN
SUBSTRATE -> METABOLIC ENZYME
Structure of ROPIVACAINE
SUBSTRATE -> METABOLIC ENZYME
Structure of VEMURAFENIB
SUBSTRATE -> METABOLIC ENZYME
Structure of EAPB-0503
SUBSTRATE -> METABOLIC ENZYME
Structure of ELISMETREP
INHIBITOR -> METABOLIC ENZYME
Structure of ELIMUSERTIB
INHIBITOR -> METABOLIC ENZYME
Structure of NAPHTHALENE
SUBSTRATE -> METABOLIC ENZYME
Structure of LASOFOXIFENE
SUBSTRATE -> METABOLIC ENZYME
Structure of TECOVIRIMAT
INDUCER -> METABOLIC ENZYME
MINOR
Structure of VENETOCLAX
SUBSTRATE -> METABOLIC ENZYME
Structure of REMDESIVIR
INHIBITOR -> METABOLIC ENZYME
Structure of ALVAMELINE
SUBSTRATE -> METABOLIC ENZYME
Structure of ALPELISIB
INHIBITOR -> METABOLIC ENZYME
In vitro, alpelisib is a strong time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
Ki
Structure of PIMOBENDAN
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of Banoxantrone
SUBSTRATE -> METABOLIC ENZYME
Structure of CIFENLINE
SUBSTRATE -> METABOLIC ENZYME
Structure of Tuspetinib
SUBSTRATE -> METABOLIC ENZYME
Structure of SIMEPREVIR
SUBSTRATE -> METABOLIC ENZYME
Plasma concentration will significantly increase if taken with medications that are strong CYP3A4 inhibitors (i.e. erythromycin, ritonavir) and will significantly decrease if taken with strong CYP3A4 inducers (i.e. efavirenz, rifampin, Saint John's wort).
Structure of FASIGLIFAM
SUBSTRATE -> METABOLIC ENZYME
Structure of TOFACITINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of VOXELOTOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ENTRECTINIB
SUBSTRATE -> METABOLIC ENZYME
Metabolism of entrectinib is primary mediated by CYP3A4 (> 90%)
MAJOR
Structure of CHOLESTEROL
SUBSTRATE -> METABOLIC ENZYME
Structure of SIMEPREVIR
INHIBITOR -> METABOLIC ENZYME
WEAK
IC50
Structure of TOZASERTIB
SUBSTRATE -> METABOLIC ENZYME
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
SUBSTRATE -> METABOLIC ENZYME
Structure of AMPRENAVIR
INHIBITOR -> METABOLIC ENZYME
Structure of DRONEDARONE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of DRONABINOL
SUBSTRATE -> METABOLIC ENZYME
Structure of DELAMANID
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of STIRIPENTOL
INHIBITOR -> METABOLIC ENZYME
Structure of BETRIXABAN
SUBSTRATE -> METABOLIC ENZYME
Structure of MACITENTAN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of RISDIPLAM METABOLITE M1
INHIBITOR -> METABOLIC ENZYME
Inactivation rate 0.063 minute
TIME-DEPENDENT INHIBITION
Ki
Structure of RUCAPARIB
SUBSTRATE -> METABOLIC ENZYME
In vitro, rucaparib was metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4.
Structure of OXCARBAZEPINE
INDUCER -> METABOLIC ENZYME
Ki
Structure of C-1311
INHIBITOR -> METABOLIC ENZYME
Structure of SB-773812
SUBSTRATE -> METABOLIC ENZYME
Structure of VANOXERINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ALBENDAZOLE
SUBSTRATE -> METABOLIC ENZYME
Structure of VELPATASVIR
SUBSTRATE -> METABOLIC ENZYME
Structure of LETERMOVIR
INDUCER -> METABOLIC ENZYME
Structure of RIFAMYCIN
INDUCER -> METABOLIC ENZYME
Rifamycin is an inducer of CYP3A4 and CYP2B6 but not CYP1A2 in vitro, however, based on systemic concentrations of rifamycin observed after administration of the recommended dose, clinically relevant induction of these enzymes in vivo is unlikely.
Structure of TORCETRAPIB
SUBSTRATE -> METABOLIC ENZYME
Structure of SAXAGLIPTIN ANHYDROUS
SUBSTRATE -> METABOLIC ENZYME
Structure of ALPELISIB
INDUCER -> METABOLIC ENZYME
STRONG
Structure of LEMBOREXANT
INDUCER -> METABOLIC ENZYME
Structure of DES(1H-PYRROLO(2,3-B)PYRIDINE)-2-HYDROXY-1H-PYRROLO(2,3-B)PYRIDINE-DECERNOTINIB
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Structure of RIFAMYCIN
NON-SUBSTRATE -> METABOLIC ENZYME
Structure of OTESECONAZOLE
INDUCER -> METABOLIC ENZYME
mRNA levels in at least 2 hepatocyte cultures. Up 10 micromolar OTESECONAZOLE
Structure of BILR-355
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of ANIDULAFUNGIN
NON-INDUCER -> METABOLIC ENZYME
Structure of ITRACONAZOLE
INHIBITOR -> METABOLIC ENZYME
POTENT
Structure of Binimetinib
SUBSTRATE -> METABOLIC ENZYME
Structure of FLUVOXAMINE
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITOR
Structure of ALISERTIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of GEMFIBROZIL
NON-INHIBITOR -> METABOLIC ENZYME
Structure of SELUMETINIB
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of CLINDAMYCIN
INHIBITOR -> METABOLIC ENZYME
Structure of CONIVAPTAN
SUBSTRATE -> METABOLIC ENZYME
Structure of ESCITALOPRAM
SUBSTRATE -> METABOLIC ENZYME
Structure of APREPITANT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of GEMIGLIPTIN
SUBSTRATE -> METABOLIC ENZYME
MAJOR
Structure of PERHEXILINE
SUBSTRATE -> METABOLIC ENZYME
Structure of PHENCYCLIDINE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
HYPERICUM PERFORATUM WHOLE
INDUCER -> METABOLIC ENZYME
Structure of ANETHOLTRITHION
SUBSTRATE -> METABOLIC ENZYME
MINOR
Structure of RISDIPLAM