Table 1.

Substrates of MDR1 classified according to their use and chemical origins. Family and mode of action is specified for anti-tumor drugs substrates of MDR1. The substrates known to act as MDR1 inhibitors are in bold, substrates shared with BCRP-1 are mentioned with (*) and substrates shared with MRP-1 are designated with (°).

Antitumor drugs
Molecules			Family			Mode of action
daunorubicin*°, epirubicin°, doxorubicin (Adriamycin)*° docetaxel°, paclitaxel° vincristine°, vinblastine° etoposide°, teniposide irinotecan*°, topotecan mitoxantrone, bisantrene melphalan° mitomycin C actinomycin D tamoxifen			Anthracycline Taxane Vinca-alkaloïd Podophyllotoxin Camptothecin Anthracenedione Nitrogen mustard Antibiotic Antibiotic Anti-oestrogen			DNA and RNA synthesis, topoisomerase II inhibition and chromatin damages induction Microtubules depolymerisation inhibition Microtubules polymerisation inhibition Topoisomerase II inhibition Topoisomerase I inhibition DNA Alkylation DNA Alkylation Topoisomerase II inhibition, DNA Alkylation Transcription Inhibition Oestrogen secretion reduction
HIV Protease inhibitors		Antimicrobial agents			Steroids			Cardiac drugs
amprenavir indinavir° nelfinavir ritonavir*° saquinavir° lopenavir		amoxicillin azithromycin erythromycin ciprofloxacin° clarythromycin doxycyclin ketoconazole itraconazole levofloxacin puromycin rifampicin tetracycline sparfloxacin			aldosterone estradiol° progesterone glucocorticoids: cortisol cortisone dexamethasone methylprednisolone prednisone			AHC-93 bunitrolol carvedilol celiprolol digitoxin digoxin diltiazem mibefradil nicardipine quinidine prazosin reserpine talinolol verapamil
Anti-histamines	Fluorescent dye			Opioids			Immuno-suppressants	Others
cimetidine fexo fenadine phenothiazine terfenadine	calcein° hoechst 33342* rhodamine 123°			asimadoline domperidone fentanyl metadone morphine loperamide pentazocine			cyclosporin A* sirolimus tacrolimus	carbazepine clomipramine omeprazole* ondansetron Ranitidin atorvastatin* amyloid β PAF