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 Mon Oct 21 19:44:04 UTC 2019
Edited
by admin
on Mon Oct 21 19:44:04 UTC 2019
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 Mon Oct 21 19:44:04 UTC 2019 , Edited by admin on Mon Oct 21 19:44:04 UTC 2019
PRIMARY
EVMPD
SUB182775
Created by admin on Mon Oct 21 19:44:04 UTC 2019 , Edited by admin on Mon Oct 21 19:44:04 UTC 2019
PRIMARY
EC (ENZYME CLASS)
EC 1.14.13.67
Created by admin on Mon Oct 21 19:44:04 UTC 2019 , Edited by admin on Mon Oct 21 19:44:04 UTC 2019
PRIMARY
PUBCHEM
121225712
Created by admin on Mon Oct 21 19:44:04 UTC 2019 , Edited by admin on Mon Oct 21 19:44:04 UTC 2019
PRIMARY
UNIPROT
P08684
Created by admin on Mon Oct 21 19:44:04 UTC 2019 , Edited by admin on Mon Oct 21 19:44:04 UTC 2019
PRIMARY
Related Record Type Details
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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.
INHIBITOR -> METABOLIC ENZYME
IC50
NON-SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
Unit K inact(min-1)
IRREVERSIBLE INHIBITOR
k(inactivation)
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
NON-INDUCER -> METABOLIC ENZYME
compared to positive controls
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
The following dose modifications are recommended: Strong CYP3A inhibitors: Reduce dose to 250 mg QD
INDUCER -> METABOLIC ENZYME
The induction of CYP3A4 enzyme (3.9 times) was lower than the mRNA increase (65 times), indicating possible time-dependent inhibition.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
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
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).
INHIBITOR -> METABOLIC ENZYME
POTENT
INHIBITOR -> METABOLIC ENZYME
Lomitapide is a weak in vivo CYP3A inhibitor.
WEAK
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
CYP3A4 in the total clearance of erdafitinib is estimated to be 20%.
NON-SUBSTRATE -> METABOLIC ENZYME
high stability to human CYP4503A4 (85% remaining)
SUBSTRATE -> METABOLIC ENZYME
The following dose modifications are recommended: Sensitive CYP3A substrates: Avoid concomitant use.
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
moderate and strong inducers of CYP3A4 should not be co-administered due to the potential for loss of efficacy.
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
sensitive substrates of CYP3A4 with a narrow therapeutic index should not be coadministered.
STRONG
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INDUCER -> METABOLIC ENZYME
Tafamidis induced CYP3A4 in vitro with an EC50 of 28 ?M.
EC50
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.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
METABOLIC ENZYME -> SUBSTRATE
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
NO INHIBITION AT 160 TIMES CMAX
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
CYP3A4 showed no preference between the two enantiomers
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
INHIBITOR -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
In vitro, ozenoxacin caused mild inhibition of CYP3A4 and CYP2C9 at high concentrations (‰100 ?M).
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> TARGET
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
TISSUE EXPRESSION -> PARENT
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.
METABOLIC ENZYME -> INHIBITOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
COMPETITIVE INHIBITOR
Ki
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
RESPONSIBLE FOR 90 PERCENT OF METABOLISM
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Coadministration of BIC (given without F/TAF) with rifampin decreased the mean BIC Cmax and AUC by 28% and 75%, respectively.
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
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
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
IN-VITRO
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
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
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
WEAK
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
CYP 3A CONTRIBUTES FOR 42% OF IXAZOMIB METABOLISM
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
INHIBITOR -> METABOLIC ENZYME
IRREVERSIBLE INHIBITOR
INHIBITOR -> METABOLIC ENZYME
REVERSIBLE
SUBSTRATE -> METABOLIC ENZYME
MINOR
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%
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
TIME-DEPENDENT INHIBITION
Ki
INDUCER -> METABOLIC ENZYME
The following dose modifications are recommended: Strong CYP3A inducers: Avoid concomitant use.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Inhibitor at higher concentrations than are clinically achieved.
MINOR
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A.
MAJOR
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
IC50
SUBSTRATE -> METABOLIC ENZYME
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
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.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
NON-INDUCER -> METABOLIC ENZYME
NON-SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
Delafloxacin was a mild inducer (less than 2 fold) of CYP3A4 at a clinically relevant concentration.
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> TARGET
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
Both ACT-064992 and ACT-132577 can induce CYP3A4 enzymes in vitro.
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> 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
STRONG
NON-INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
MODERATE
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
In vitro, alpelisib is a strong time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
Ki
SUBSTRATE -> METABOLIC ENZYME
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).
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK
IC50
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
In vitro, rucaparib was metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
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.
SUBSTRATE -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
STRONG
SUBSTRATE -> METABOLIC ENZYME
MAJOR
NON-SUBSTRATE -> METABOLIC ENZYME
NON-INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
WEAK INHIBITOR
NON-SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MINOR
SUBSTRATE -> METABOLIC ENZYME
NON-INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
WEAK
INHIBITOR -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
WEAK
INDUCER -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
Midazolam is the substrate.
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
Concomitant administration of CYP3A4 inhibitors may inhibit the metabolism of ulipristal acetate and cause increased plasma concentration of ulipristal acetate. In addition, concomitant administration of CYP3A4 inducers may reduce plasma concentrations of ulipristal acetate and may result in decrease in efficacy.
MAJOR
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INHIBITOR -> METABOLIC ENZYME
POTENT
INDUCER -> TARGET
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
Glasdegib is metabolized primarily by the CYP3A4 pathway.
MAJOR
NON-SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
- Co-administration of deflazacort with clarithromycin, a strong CYP3A4 inhibitor, increased total exposure to 21-desDFZ by about 3-fold. - Co-administration of deflazacort with rifampin, a strong CYP3A4 inducer, significantly decreased the exposure of 21-desDFZ.
INHIBITOR -> METABOLIC ENZYME
Ki
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
POTENT
SUBSTRATE -> METABOLIC ENZYME
MAJOR
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
NON-SUBSTRATE -> METABOLIC ENZYME
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
As cabazitaxel is mainly metabolized by CYP3A in vitro, strong CYP3A inducers or inhibitors are expected to affect the pharmacokinetics of cabazitaxel.
MAJOR
INDUCER -> METABOLIC ENZYME
INDUCER -> METABOLIC ENZYME
CYP3A4 expression was also induced by rifampin by a mean value of approximately 43-fold compared to vehicle control values
INHIBITOR -> METABOLIC ENZYME
WEAK
INHIBITOR -> METABOLIC ENZYME
Cobimetinib is a time-dependent inhibitor of CYP3A4 in vitro.
TIME-DEPENDENT INHIBITION
SUBSTRATE -> METABOLIC ENZYME
SUBSTRATE -> METABOLIC ENZYME
MAJOR
INDUCER -> METABOLIC ENZYME
INHIBITOR -> TARGET
Ki
INHIBITOR -> METABOLIC ENZYME
IC50
INHIBITOR -> METABOLIC ENZYME
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
Related Record Type Details
PARENT -> METABOLITE INACTIVE
The benzoic acid metabolite of lorlatinib (PF-06895751) is pharmacologically inactive.
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL