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

Inhibitors of P-gp		Inducers of P-gp
Abrocitinib Adagrasib Amiodarone Azithromycin (systemic) Belumosudil Cannabidiol and cannabidiol-containing coformulations Capmatinib Carvedilol Clarithromycin Cobicistat and cobicistat-containing coformulations Cyclosporine (systemic) Daclatasvir Daridorexant 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 Mavorixafor Mifepristone^* Neratinib Nirmatrelvir-ritonavir Ombitasvir-paritaprevir-ritonavir (Technivie)^¶ Osimertinib Pirtobrutinib Posaconazole Propafenone Quinidine Quinine Ranolazine Ritonavir and ritonavir-containing coformulations^¶ Rolapitant Selpercatinib Simeprevir Sotagliflozin Sotorasib^Δ Tamoxifen^Δ Tepotinib Tezacaftor-ivacaftor Ticagrelor^Δ Tucatinib Vanzacaftor-tezacaftor-deutivacaftor 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 drug interactions program included within 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.

* Mifepristone is a significant inhibitor of P-gp when used chronically (eg, for hyperglycemia in patients with Cushing syndrome), not in single-dose use.

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

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

Data from: UpToDate Lexidrug. More information available at https://online.lexi.com/.

References:

Clinical drug interaction studies — Cytochrome P450 enzyme- and transporter-mediated drug interactions: Final guidance for industry. US Food & Drug Administration. https://www.fda.gov/media/135586/download (Accessed on June 5, 2020).
Drug development and drug interactions: Table of substrates, inhibitors and inducers. US Food & Drug Administration. https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers (Accessed on March 29, 2018).
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.

Graphic 73326 Version 90.0

خرید پکیج

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