Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Thu Jul 06 11:42:27 UTC 2023
by
admin
on
Thu Jul 06 11:42:27 UTC 2023
|
Protein Type | ENZYME |
Protein Sub Type | CYTOCHROME P450 |
Sequence Origin | HUMAN |
Sequence Type | COMPLETE |
Record UNII |
PUO0521HZV
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
Code System | Code | Type | Description | ||
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329736-03-0
Created by
admin on Thu Jul 06 11:42:58 UTC 2023 , Edited by admin on Thu Jul 06 11:42:58 UTC 2023
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PRIMARY | |||
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PUO0521HZV
Created by
admin on Thu Jul 06 11:42:58 UTC 2023 , Edited by admin on Thu Jul 06 11:42:58 UTC 2023
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PRIMARY | |||
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SUB182775
Created by
admin on Thu Jul 06 11:42:58 UTC 2023 , Edited by admin on Thu Jul 06 11:42:58 UTC 2023
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PRIMARY | |||
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EC 1.14.13.67
Created by
admin on Thu Jul 06 11:42:58 UTC 2023 , Edited by admin on Thu Jul 06 11:42:58 UTC 2023
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PRIMARY | |||
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P08684
Created by
admin on Thu Jul 06 11:42:58 UTC 2023 , Edited by admin on Thu Jul 06 11:42:58 UTC 2023
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PRIMARY |
Related Record | Type | Details | ||
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
Midazolam is the substrate.
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INHIBITOR -> METABOLIC ENZYME |
Measured by midazolam 1′-hydroxylation; 42% inhibition at 10 micromolar.
IC50
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> TARGET |
PHARMAKINETIC ENHANCER
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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 |
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
WEAK
TIME-DEPENDENT INHIBITION
Ki
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
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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.
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SUBSTRATE -> METABOLIC ENZYME | |||
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NON-INHIBITOR -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
IN VITRO
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
IRREVERSIBLE INHIBITOR
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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 |
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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 | |||
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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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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 |
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.
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INHIBITOR -> METABOLIC ENZYME |
IC50
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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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NON-SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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NON-INHIBITOR -> METABOLIC ENZYME |
DID NOT INHIBIT ANY OTHER CYP ENZYMES
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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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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
Unit K inact(min-1)
IRREVERSIBLE INHIBITOR
k(inactivation)
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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INHIBITOR -> METABOLIC ENZYME |
The following dose modifications are recommended: Strong CYP3A inhibitors: Reduce dose to 250 mg QD
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NON-SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INDUCER -> METABOLIC ENZYME |
The induction of CYP3A4 enzyme (3.9 times) was lower than the mRNA increase (65 times), indicating possible time-dependent inhibition.
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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 |
IC50
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SUBSTRATE -> 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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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 |
MAJOR
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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
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INHIBITOR -> METABOLIC ENZYME |
In an in-vitro study, eluxadoline appears to show time-dependent inhibition of CYP3A4 at 50 μM, a concentration that can be achieved in the gut (Igut is estimated to be 700 μM).
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
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INHIBITOR -> METABOLIC ENZYME |
Lomitapide is a weak in vivo CYP3A inhibitor.
WEAK
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
CYP3A4 in the total clearance of erdafitinib is estimated to be 20%.
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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
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NON-SUBSTRATE -> METABOLIC ENZYME |
high stability to human CYP4503A4 (85% remaining)
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
The following dose modifications are recommended: Sensitive CYP3A substrates: Avoid concomitant use.
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
moderate and strong inducers of CYP3A4 should not be co-administered due to the potential for loss of efficacy.
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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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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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 | |||
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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 |
IN VITRO
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SUBSTRATE -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME |
sensitive substrates of CYP3A4 with a narrow therapeutic index should not be coadministered.
STRONG
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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INDUCER -> METABOLIC ENZYME |
Tafamidis induced CYP3A4 in vitro with an EC50 of 28 μM.
EC50
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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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 |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
POTENT
|
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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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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME |
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INHIBITOR -> METABOLIC ENZYME | |||
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INDUCER -> 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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INDUCER -> METABOLIC ENZYME |
POTENT
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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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
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INHIBITOR -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
RESPONSIBLE FOR 90 PERCENT OF METABOLISM
MAJOR
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INHIBITOR -> METABOLIC ENZYME |
Lonafarnib is a potent CYP3A time-dependent and mechanism-based inhibitor.
TIME-DEPENDENT INHIBITION
POTENCY
|
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SUBSTRATE -> METABOLIC ENZYME |
CYP3A4 showed no preference between the two enantiomers
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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 |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
Low systematic exposure
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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-SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
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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 |
6β-hydroxylation of testosterone
IC50
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SUBSTRATE -> METABOLIC ENZYME | |||
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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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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INDUCER -> METABOLIC ENZYME |
strong CYP3A4 induction in a concentration-dependent manner
MAY BE CLINICALLY SIGNIFICANT
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
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NON-INHIBITOR -> METABOLIC ENZYME |
NO INHIBITION AT 160 TIMES CMAX
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SUBSTRATE -> METABOLIC ENZYME | |||
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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 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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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> TARGET | |||
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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 |
MAJOR
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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 |
WEAK INHIBITION
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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TISSUE EXPRESSION -> PARENT | |||
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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.
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INHIBITOR -> METABOLIC ENZYME |
Time-dependent inhibition. significant effect with other drugs which are substrate of CYP3A4 at clinical dose of Lenvatinib
MAJOR
PLASMA
|
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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 | |||
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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 |
MAJOR
|
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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 | |||
|
INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
|
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|
SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
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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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
|
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
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
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
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SUBSTRATE -> METABOLIC ENZYME | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
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.
|
||
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INHIBITOR -> METABOLIC ENZYME |
SELECTIVE
|
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INDUCER -> METABOLIC ENZYME | |||
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SUBSTRATE -> 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 | |||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
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SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
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SUBSTRATE -> METABOLIC ENZYME |
|
||
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INHIBITOR -> METABOLIC ENZYME |
TIME-DEPENDENT INHIBITION
|
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INDUCER -> 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
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
IN-VITRO
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
In vitro, avapritinib is a time-dependent inhibitor as well as an inducer of CYP3A.
TIME-DEPENDENT INHIBITION
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
Zanubrutinib is a weak inducer of CYP3A4 and CYP2C19 in vivo.
WEAK
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
NON-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 |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
Eribulin inhibited CYP3A4 activity with an apparent inhibition constant (Ki) value ranging from 3 μM to 30 μM (2190 ng/mL to 21,900 ng/mL), and the inhibition was demonstrated to be reversible and competitive.
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A.
MAJOR
|
||
|
ANIMAL ORTHOLOG->HUMAN ORTHOLOG | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
TIME-DEPENDENT INHIBITION
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME |
WEAK
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
WEAK
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
Does not induce CYP3A4 activity.
|
||
|
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 | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
Moderate inhibitor
MINOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
POTENT
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
TIME-DEPENDENT INHIBITION
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
|
||
|
NON-INHIBITOR -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
Possible deadly drug interaction with CYP3A4 inhibitors
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
The fraction metabolized through CYP3A accounts for approximately 40% of the total hepatic panobinostat elimination.
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
NON-INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
In vitro, avapritinib is a time-dependent inhibitor as well as an inducer of CYP3A.
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
10% conversion to M1
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
APICAL
|
||
|
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
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
MODERATE INDUCER THROUGH MEDIATED BY THE PREGNANE X RECEPTOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
the presence of strong CYP 3A4 inhibition by itraconazole can lead to an AUC increase of 400%.
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
POTENT
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
Predicted no effect with other CYP2C8 substrates at clinical dose of Lenvatinib
|
||
|
INDUCER -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
ANIMAL ORTHOLOG->HUMAN ORTHOLOG |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
TIME-DEPENDENT INHIBITION
Ki
|
||
|
INHIBITOR -> METABOLIC ENZYME |
COMPETITIVE INHIBITOR
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
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 |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME |
Lumacaftor is a strong inducers of CYP3A4
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
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 |
MAJOR
|
||
|
NON-INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
Ki
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
REVERSIBLE
|
||
|
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 | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
CYP3A4-mediated (oxidative) metabolism of canagliflozin is minimal (approximately 7%) in humans.
MINOR
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
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 | |||
|
INHIBITOR -> METABOLIC ENZYME |
E-Norendoxifen inhibited CYP3A4 3.7-fold more potently than Z-norendoxifen.
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
NON-SUBSTRATE -> METABOLIC ENZYME |
|
||
|
NON-INDUCER -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0‐20%), and FMO3 (0‐33%) in vitro.
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
NON-SUBSTRATE -> METABOLIC ENZYME |
WAS NOT A SUBSTRATE FOR ANY OTHER CYP ENZYME
|
||
|
INDUCER -> METABOLIC ENZYME |
Delafloxacin was a mild inducer (less than 2 fold) of CYP3A4 at a clinically relevant concentration.
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INDUCER -> METABOLIC ENZYME |
Strong Inducer
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
|
||
|
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
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
In human liver microsomes, dasatinib was a weak time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> TARGET |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INDUCER -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
|
||
|
INDUCER -> METABOLIC ENZYME |
Both ACT-064992 and ACT-132577 can induce CYP3A4 enzymes in vitro.
|
||
|
INHIBITOR -> METABOLIC ENZYME |
IC50
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME |
E-Norendoxifen inhibited CYP3A4 3.7-fold more potently than Z-norendoxifen.
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
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 | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
INHIBITOR -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
IN VITRO
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
MODERATE
|
||
|
INHIBITOR -> METABOLIC ENZYME |
MODERATE
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
NON-INHIBITOR -> METABOLIC ENZYME |
|
||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INDUCER -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
INHIBITOR -> METABOLIC ENZYME |
In vitro, alpelisib is a strong time-dependent inhibitor of CYP3A4.
TIME-DEPENDENT INHIBITION
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MINOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
|
||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
SUBSTRATE -> METABOLIC ENZYME | |||
|
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 |
COMPETITIVE INHIBITOR
Ki
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
MAJOR
|
||
|
SUBSTRATE -> METABOLIC ENZYME |
Metabolism of entrectinib is primary mediated by CYP3A4 (> 90%)
MAJOR
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SUBSTRATE -> METABOLIC ENZYME | |||
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INHIBITOR -> METABOLIC ENZYME |
WEAK
IC50
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