CYP3A4-inhibitors and inducers
This is a list composed of substances that induce or inhibit CYP3A4. The substances are in alphabetical order and classified as strong, moderate or weak inducers or inhibitors according to guidelines from the European Medicines Agency. The classifications are supported by references. The list is adapted to substances used in Sweden and limited to substances which could be classified based on data retrieved from literature search. The list is produced and maintained by Clinical Pharmacology at Karolinska University Hospital.
| Substance | Inhibitor/inducer | References |
| amiodarone | weak inhibitor | Bequemont et al., 2007 |
| apalutamide | strong inducer | Duran et al., 2020 |
| aprepitant | moderate inhibitor/ weak inducer | Majumdar et al., 2003 Shadle et al., 2004 |
| asciminib | weak inhibitor | Hoch et al., 2022 |
| atazanavir | strong inhibitor | EPAR Reyataz |
| berotralstat | moderate inhibitor | SPC Orladeyo 2021 EPAR Orladeyo 2021 FDA. Orladeyo |
| bicalutamide | weak inhibitor | SPC Casodex |
| bosentan | moderate inducer | Sandqvist et al., 2013 |
| brigatinib | weak inducer | Hanley et al., 2022 |
| carbamazepine | strong inducer | Ucar et al., 2004 |
| cenobamate | strong inducer | EPAR Ontozry |
| ceritinib | strong inhibitor | Hurtado et al., 2021 |
| cilostazol | weak inhibitor | Jung-Ruyl et al., 2019 |
| cimetidin | weak inhibitor | Salonen et al., 1986 |
| ciprofloxacin | moderate inhibitor | Hedaya et al., 2006 |
| clarithromycin | strong inhibitor | Yeates et al., 1996 Gorski et al., 1998 Quinney et al., 2008 |
| clobazam | weak inducer | Walzer et al., 2012 |
| cobicistat | strong inhibitor | Mathias et al., 2019 EPAR Tybost |
| crizotinib | moderate inhibitor | EPAR Xalcori |
| cyclosporine | weak inhibitor | Jonge et al., 2011 |
| dabrafenib | moderate inducer | EPAR Tafinlar Falchook et al., 2014 |
| dalfopristin | weak inhibitor | FDA Synercid |
| darolutamid | weak inducer | Zurth et al., 2019 |
| darunavir | *Not studied by itself, only in combination with ritonavir which inhibits CYP3A4. Always given in combination with ritonavir | EPAR Prezista |
| dexametason | weak inducer | SPC Neofordex Villikka et al., 1998 |
| dicloxacillin | weak inducer | Stage TB et al., 2018 |
| diltiazem | moderate inhibitor | Backman et al., 1994 |
| dronedarone | moderate inhibitor | EPAR Multaq |
| duvelisib | moderate inhibitor | EPAR Copiktra |
| efavirenz | moderate inducer | Gerber et al., 2005 Fellay et al., 2005 SPC Efavirenz |
| encorafenib | strong inducer | SPC Braftovi 2024 ClinicalTrials.gov NCT03864042 |
| entrectinib | weak inhibitor | Meneses-Lorente et al., 2021 |
| enzalutamide | strong inducer | Gibbons et al., 2015 |
| erlotinib | weak inducer | Calvert et al., 2014 |
| erythromycin | moderate inhibitor | Olkkola et al., 1993 Okudaira et al., 2007 |
| eslicarbazepine | weak inducer | SPC Zebinix |
| etravirine | weak inducer | SPC Intelence Kakuda et al., 2014 |
| everolimus | weak inhibitor | Urva et al., 2013 |
| fedratinib | moderate inhibitor | Ogasawara et al., 2020 |
| fluconazole | moderate inhibitor | Ahonen et al., 1997 Olkkola et al., 1996 |
| fluvoxamine | weak inhibitor | Lam et al., 2003 Kashuba et al., 1998 |
| fosamprenavir | *Not studied by itself, only in combination with ritonavir which inhibits CYP3A4. Always given in combination with ritonavir | EPAR Telzir |
| fosaprepitant | weak inhibitor/weak inducer | Shadle et al., 2004 |
| givosiran | weak inhibitor | SPC Givlaari |
| glycerol phenylbuturate | weak inducer | EPAR Ravicti |
| grape fruit juice | moderate inhibitor when given p.o. Does not affect when given as i.v. | Veronese et al., 2003 |
| grazoprevir | weak inhibitor | EPAR Zepatier |
| idelalisib | strong inhibitor | Jin et al., 2015 EPAR Zydelig |
| imatinib | moderate inhibitor | O’Brien et al., 2003 |
| isavuconazole | moderate inhibitor | SPC Cresemba Townsend et al., 2017 |
| itraconazole | strong inhibitor | Olkkola et al., 1994 Ahonen et al., 1995 Olkkola et al., 1996 |
| ivacaftor | weak inhibitor | Robertson et al., 2015 |
| ivosidenib | strong inducer | FDA (Multidisciplinary Review) Fan et al., 2020 Lachowiez et al., 2023 |
| ketoconazole | strong inhibitor | Olkkola et al., 1994 Lam et al., 2003 |
| lapitinib | weak inhibitor | Koch et al., 2017 |
| larotrectinib | weak inhibitor | EPAR Vitrakvi |
| lefamulin | moderate inhibitor | EPAR Xenleta |
| lenacapavir | moderate inhibitor | EPAR Sunlenca |
| letermovir | moderate inhibitor | EPAR Prevymis |
| lomitapide | weak inhibitor | Tuteja et al., 2014 |
| lonafarnib | strong inhibitor | EPAR Zokinvy 2022 FDA Zokinvy 2020 |
| lopinavir | *Not studied by itself, only in combination with ritonavir which inhibits CYP3A4. Always given in combination with ritonavir | SPC Kaletra |
| lorlatinib | moderate inducer | EPAR Lorviqua |
| miconazole | weak inhibitor | Ishiwata et al., 2016 |
| mithotane | strong inducer | van Erp et al., 2011 |
| modafinil | moderate inducer | Rowland et al., 2018 Robertson Jr et al., 2002 |
| nefazodone | moderate inhibitor | Lam et al., 2003 |
| nelfinavir | strong inhibitor | Hsyu et al., 2001 Fellay et al., 2005 |
| netupitant | moderate inhibitor | Lanzarotti et al., 2013 |
| nevirapine | weak inducer | SPC Viramune EPAR Viramune |
| nilotinib | moderate inhibitor | Zhang et al., 2015 |
| osilodostat | weak inhibitor | EPAR Isturisa Armani et al., 2017 |
| oxacarbapezine | weak inducer | Zaccara et al., 1993 |
| palbociclib | weak inhibitor | EPAR Ibrance |
| paritaprevir | *Not studied by itself, only in combination with ritonavir which inhibits CYP3A4. Always given in combination with ritonavir | SPC Viekirax |
| pazopanib | weak inhibitor | Goh et al., 2010 |
| phenobarbital | strong inducer | Rutledge et al., 1988 |
| phenytoin | strong inducer | Michelucci et al., 1996 |
| phosphenytoin | strong inducer | Michelucci et al., 1996 |
| posaconazole | strong inhibitor | Krishna et al., 2009 |
| primidone | strong inducer | Rutledge et al., 1988 |
| quinupristin | weak inhibitor | Synercid (quinupristin/dalfopristin). Monarch Pharmaceuticals Ireland Limited. SPC. 2005 |
| rifabutin | weak inducer | SPC Ansatipin |
| rifampicin | strong inducer | Rutledge et al., 1988 |
| rifamycin | strong inducer | Rutledge et al., 1988 |
| ribociclib | moderate inhibitor | EPAR Kisqali |
| rimegepant | weak inhibitor | EPAR Vydura Vydura FDA 2020 |
| ritlecitinib | moderate inhibitor | EPAR Litfulo |
| ritonavir | strong inhibitor | Fichtenbaum et al., 2002 Greenblatt et al., 2009 |
| roxitromycin | weak inhibitor | Zaccara et al., 1993 |
| rucaparib | weak inhibitor | EPAR Rubraca Xiao et al., 2019 |
| rufinamide | weak inducer | EPAR Inovelon |
| saquinavir | strong inhibitor | Palkama et al., 1999 Schmitt et al., 2009 |
| selpercatinib | weak inhibitor | SPC Retsevmo EPAR Retsevmo FDA Retsevmo |
| simeprevir | weak inhibitor | EPAR Olysio |
| St John’s wort | moderate inducer | Dresser et al., 2003 |
| tecovirimat | weak inducer | EPAR Tecovirimat SIGA |
| telithromycin | strong inhibitor | EPAR Ketek |
| telotristat ethyl | moderate inducer | EPAR Xermelo |
| ticagrelor | weak inducer | Teng et al., 2013 |
| tipranavir | *Not studied by itself, only in combination with ritonavir which inhibits CYP3A4. Always given in combination with ritonavir | SPC Aptivus |
| troleandomycin | moderate inhibitor | Warot et al., 1987 |
| tucatinib | strong inhibitor | EPAR Tukysa |
| upadacitinib | weak inducer | EPAR Rinvoq |
| vemurafenib | weak inducer | SPC Zelboraf |
| verapamil | moderate inhibitor | Backman et al., 1994 |
| voriconazole | strong inhibitor | Saari et al., 2006 |
| voxelotor | weak inhibitor | EPAR Oxbryta FDA Oxbryta |
| zanubrutinib | weak inducer | Ou et al., 2021 |