Clinically important substrates of ABC drug efflux transporters
Reviewed in Petrovic et al. (2007).
Transporter | Substrates |
|---|---|
| ABCB1 | Antiretroviral protease inhibitors: (RTV, SQV, INV, NFV, APV) |
| Anticancer drugs: anthracyclines, vinca alkaloids, taxanes, epipodophyllines, anthracenes | |
| Anti-infective drugs: erythromycin, levofloxacin, sparfloxacin, ketoconazole | |
| Cardiovascular: digoxin, quinidine, diltiazem, verapamil, β-blockers, statins | |
| Immunosuppressants: cyclosporin A, tacrolimus | |
| Steroids: dexamethasone, prednisolone, corticosterone, cortisol | |
| Opioids: morphine, loperamide | |
| Other: 33mTc-sestamibi, 33mTc-tetrofosfine | |
| ABCC1 | Antiretroviral protease inhibitors: (RTV, SQV, INV) |
| Anticancer drugs: anthracyclines, vinca alkaloids, epipodophyllines, methotrexate, cisplatin, anthracenes, flutamide | |
| Steroids: 17β-glucoronyl estradiol, S-glutathionyl prostaglandin A2 | |
| Other: 33mTc-sestamibi, 33mTc-tetrofosfine, fluorescein, indomethacin, aflatoxin B1 | |
| ABCC2 | Antiretroviral protease inhibitors: (RTV, SQV, INV) |
| Antibiotics: ceftriaxone, grepafloxacin, rifampicin | |
| Anticancer drugs: methotrexate, cisplatin, vinblastine, vincristine, doxorubicin, etoposide | |
| Steroids: estradiol, octreotide | |
| Other: temocaprilat, furosemide, sulfinpyrazone, pravastatin, phenytoin, flavonoids, diclofenac, acetaminophen, heavy metals, arsenite, food carcinogens | |
| ABCC3 | Anticancer drugs: etoposide, teniposide, leucovorin, methotrexate |
| Other: furosemide, leukotriene C4, acetaminophen | |
| ABCG2 | Antiretroviral drugs: AZT, 3TC |
| Anticancer drugs: topotecan, irinotecan, mitoxantrone, methotrexate, doxorubicin, daunorubicin, Adriamycin, etoposide, flavopiridol | |
|
| Other: prazosin, novobiocin, pheophorbide |
SQV, saquinavir; RTV, ritonavir; NFV, nelfinavir; INV, indinavir; APV, amprenavir; AZT, azidothymidine, zidovudine; 3TC, 2′,3′-dideoxy-3′-thiacytidine, lamivudine.