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Cytochrome P450 3A (including 3A4) inhibitors and inducers

Cytochrome P450 3A (including 3A4) inhibitors and inducers
Strong inhibitors
Atazanavir
Ceritinib
Clarithromycin
Cobicistat and cobicistat-containing coformulations
Darunavir
Idelalisib
Indinavir
Itraconazole
Ketoconazole
Levoketoconazole
Lonafarnib
Lopinavir
Mifepristone
Nefazodone
Nelfinavir
Ombitasvir-paritaprevir-ritonavir
Ombitasvir-paritaprevir-ritonavir plus dasabuvir
Posaconazole
Ritonavir and ritonavir-containing coformulations
Saquinavir
Telithromycin
Tucatinib
Voriconazole
Moderate inhibitors
Amiodarone*
Aprepitant
Berotralstat
Cimetidine*
Conivaptan
Crizotinib
Cyclosporine*
Diltiazem
Duvelisib
Dronedarone
Erythromycin
Fedratinib
Fluconazole
Fosamprenavir
Fosaprepitant*
Fosnetupitant-palonosetron
Grapefruit juice
Imatinib
Isavuconazole (isavuconazonium sulfate)
Lefamulin
Letermovir
Netupitant
Nilotinib
Ribociclib
Schisandra
Verapamil
Strong inducers
Apalutamide
Carbamazepine
Enzalutamide
Fosphenytoin
Lumacaftor
Lumacaftor-ivacaftor
Mitotane
Phenobarbital
Phenytoin
Primidone
Rifampin (rifampicin)
Moderate inducers
Bexarotene
Bosentan
Cenobamate
Dabrafenib
Dexamethasone
Dipyrone
Efavirenz
Elagolix, estradiol, and norethindrone therapy packΔ
Eslicarbazepine
Etravirine
Lorlatinib
Modafinil
Nafcillin
Pexidartinib
Rifabutin
Rifapentine
Sotorasib
St. John's wort
  • For drug interaction purposes, the inhibitors and inducers of CYP3A metabolism listed above can alter serum concentrations of drugs that are dependent upon the CYP3A subfamily of liver enzymes, including CYP3A4, for elimination or activation.
  • These classifications are based upon US Food and Drug Administration (FDA) guidance.[1,2] Other sources may use a different classification system resulting in some agents being classified differently.
  • Data are for systemic drug forms. Degree of inhibition or induction may be altered by dose, method, and timing of administration.
  • Weak inhibitors and inducers are not listed in this table with exception of a few examples. Clinically significant interactions can occasionally occur due to weak inhibitors and inducers (eg, target drug is highly dependent on CYP3A4 metabolism and has a narrow therapeutic index). Accordingly, specific interactions should be checked using a drug interaction program such as the Lexicomp drug interactions program included within UpToDate.
  • Refer to UpToDate topics on specific agents and indications for further details.
* Classified as a weak inhibitor of CYP3A4 according to FDA system.[1]
¶ Classified as a weak inducer of CYP3A4 according to FDA system.[1]
Δ The fixed-dose combination therapy pack taken in the approved regimen has moderate CYP3A4 induction effects. When elagolix is used as a single agent, it is a weak CYP3A4 inducer. Norethindrone and estradiol are not CYP3A4 inducers.
Data from: Lexicomp Online (Lexi-Interact). Copyright © 1978-2022 Lexicomp, Inc. All Rights Reserved.
References:
  1. Clinical Drug Interaction Studies — Cytochrome P450 Enzyme- and Transporter-Mediated Drug Interactions Guidance for Industry (January 2020) available at: https://www.fda.gov/regulatory-information/search-fda-guidance-documents/clinical-drug-interaction-studies-cytochrome-p450-enzyme-and-transporter-mediated-drug-interactions.
  2. US Food & Drug Administration. Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers. Available at: FDA.gov website.
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