Example substrates and inhibitors for the MDR1 and BCRP transporters
| MDR1 Substrates | BCRP Substrates |
|---|---|
| Doxorubicin, vinblastine, tyrosine kinase inhibitors, HIV protease inhibitors (ritonavir, indinavir), phenytoin, prazosin, digoxin, diltiazem, tetracycline, morphine, polycyclic compounds (steroid aldosterone), fluorescent dyes (Rhodamine 123), amyloid- β, phospholipids, and lipid-derived signaling molecules | Doxorubicin, methotrexate, tyrosine kinase inhibitors, mitoxantrone, antiviral drugs (abacavir, zidovudine), fluoroquinolone antibiotics, prazosin, glyburide, etoposide, topotecan, zearalenone, aflatoxin B, fluorescent dyes (Hoechst 33342, Rhodamine 123), Genistein, protoporphyrin IX, amyloid-β, cholate |
| MDR1 Inhibitors | BCRP Inhibitors |
| Verapamil, cyclic peptides (cyclosporin A, PSC833), tamoxifen, sildanefil, curcuminoids, flavonoids, LY335979 (zosuquidar), GF120918 (elacridar) | Ko143, omeprazole, fumitremorgin C, GF120918 (elacridar), tyrosine kinase inhibitors, tacrolimus, tamoxifen, cyclosporin A |