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REGULATION OF DRUG TRANSPORTERS: DURING INFECTION AND INFLAMMATION
Table 1.
Clinically Important Substrates of ABC Drug Efflux Transporters
| Transporter | Substrates |
|---|---|
| aSQV, saquinavir; RTV, ritonavir; NFV, nelfinavir; INV, indinavir; APV, amprenavir. | |
| PGP (ABCB1) | Antiretrovirals: Protease inhibitors (RTV, SQV, INV, NFV, APV)a Anticancers: Anthracyclines, vinca alkaloids, taxanes, epipodophyllines, anthracenes Anti-infectives: Erythromycin, levofloxacin, sparfloxacin, ketoconazole Cardiovascular: Digoxin, quinidine, diltiazem, verapamil, β-blockers, statins Immunosuppressants: Cyclosporin A, tacrolimus, Steroids: Dexamethasone, prednisolone, corticosteron, cortisol Opioids: Morphine, loperamide Other: 99mTc-Sestamibi, 99mTc-tetrofosfine |
| MRP1 (ABCC1) | Antiretrovirals: Protease inhibitors (RTV, SQV, INV) Anticancers: Anthracyclines, vinca alkaloids, epipodophyllines, methotrexate, cisplatin, anthracenes, flutamide Steroids: 17-β-Glucoronyl estradiol, S-glutathionyl prostaglandin A2 Toxins: Aflatoxin B1 Other: 99mTc-Sestamibi , 99mTc-tetrofosfine, fluoroscein, indomethacin Notable physiological substrate: LTC4 |
| MRP2 (ABCC2) | Antiretrovirals: Protease inhibitors (RTV, SQV, INV) Antibiotics: Ceftriaxone, grepafloxacin, rifampicin Anticancers: Methotrexate, cisplatin, vinblastine, vincristine, doxorubicin, etoposide Steroids: Estradiol, octreotide Toxins: Heavy metals, arsenite, food carcinogens Other: Temocaprilat, furosemide, sulphinpyrazone, pravastatin, phenytoin, flavonoids, diclofenac, acetaminophen Notable physiological substrate: Bilirubin |
| MRP3 (ABCC3) | Antiretrovirals: None reported Anticancers: Etoposide, teniposide, leucovorin, methotrexate Other: Furosemide, leukotriene C4, acetaminophen Notable physiological substrate: Bile acids |
| BCRP (ABCG2) | Antiretrovirals: AZT, 3TC Anticancers: Topotecan, irinotecan, mitoxantrone, methotrexate, doxorubicin, daunorubicin, adriamycin, etoposide, flavopiridol Food additives: Pheophorbide Other: Prazocin, novobiocin |
