Inhibitors and inducers of P-glycoprotein (P-gp) drug efflux pump (P-gp multidrug resistance transporter)

Inhibitors of P-gp		Inducers of P-gp
Amiodarone Abrocitinib Azithromycin (systemic) Cannabidiol and cannabidiol-containing coformulations Capmatinib Carvedilol Clarithromycin Cobicistat and cobicistat-containing coformulations Cyclosporine (systemic) Daclatasvir Diosmin (a plant flavonoid sold as dietary supplement) Dronedarone Elagolix Elagolix-estradiol-norethindrone Eliglustat Elexacaftor-tezacaftor-ivacaftor Enzalutamide Erythromycin (systemic) Flibanserin Fostamatinib Glecaprevir-pibrentasvir Isavuconazole (isavuconazonium sulfate) Itraconazole Ivacaftor Ketoconazole (systemic)	Lapatinib Ledipasvir Levoketoconazole Neratinib Nirmatrelvir-ritonavir Ombitasvir-paritaprevir-ritonavir (Technivie)* Osimertinib Posaconazole Propafenone Quinidine Quinine Ranolazine Ritonavir and ritonavir-containing coformulations* Rolapitant Selpercatinib Simeprevir Tamoxifen^¶ Tepotinib Tezacaftor-ivacaftor Ticagrelor^¶ Tucatinib Velpatasvir Vemurafenib Verapamil Voclosporin	Apalutamide Carbamazepine Fosphenytoin Green tea (Camellia sinensis) Lorlatinib Phenytoin Rifampin (rifampicin) St. John's wort

Inhibitors of the P-gp drug efflux pump (also known as P-gp multidrug resistance transporter) listed above may increase serum concentrations of drugs that are substrates of P-gp, whereas inducers of P-gp drug efflux may decrease serum concentrations of substrates of P-gp.
Examples of drugs that are substrates of P-gp efflux pump include: Apixaban, colchicine, cyclosporine, dabigatran, digoxin, edoxaban, rivaroxaban, and tacrolimus.
The degree of effect on P-gp substrate serum concentration may be altered by dose and timing of orally administered P-gp inhibitor or inducer.
These classifications are based upon US FDA guidance.^[1,2] Other sources may use a different classification system resulting in some agents being classified differently.
Specific drug interaction effects may be determined by using the Lexicomp drug interactions program included with UpToDate. Refer to UpToDate clinical topics on specific agents and conditions for further details.

P-gp: P-glycoprotein; US FDA: US Food and Drug Administration.

* The combination of ombitasvir-paritaprevir-ritonavir plus dasabuvir (Viekira Pak) is not a significant inhibitor of P-gp efflux pump.^[3]

¶ Minor clinical effect or supportive data are limited to in-vitro effects (ie, clinical effect is unknown).

References:

US Food and Drug Administration. 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 (Accessed on June 5, 2020).
US Food & Drug Administration. Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers. Available at: FDA.gov website.
Menon RM, Badri PS, Wang T, et al. Drug-drug interaction profile of the all-oral anti-hepatitis C virus regimen of paritaprevir/ritonavir, ombitasvir, and dasabuvir. J Hepatol 2015; 63:20.

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