Mechanism | BCR/ABL inhibitor | Drug | Consequences/Recommendations |
Potent CYP3A4 inhibitors | All | Boceprevir, clarithromycin, itraconazole, ketoconazole, lopinavir / ritonavir, nefazodone, nelfinavir, indinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, voriconazole, grape fruit juice. | Increased concentrations of BCR/ABL inhibitor. Avoid. |
Moderate CYP3A4 inhibitors | All | Amprenavir, aprepitant, atazanavir, ciprofloxacin, darunavir / ritonavir, diltiazem, erythromycin, fluconazole, fosamprenavir, crizotinib, imatinib, verapamil, fruit juice. | Increased concentrations of BCR/ABL inhibitor. Avoid high doses. |
Potent CYP3A4 inducers | All | Carbamazepine, oxcarbazepine, phenytoin, phenobarbital, rifampin, rifabutin, St. John's Wort. | Reduced concentrations of BCR/ABL inhibitor. Avoid. |
Moderate CYP3A4 inducers | All | Bosentan, dexamethasone, efavirenz, etravirine, modafinil, nafcillin, nevirapine. | Reduced concentrations of BCR/ABL inhibitor. Consider increasing the dose of the BCR/ABL inhibitor. |
Potent P-glycoprote ininhibitors | Imatinib, nilotinib, ponatinib | Amiodarone, azithromycin, captopril, carvedilol, clarithromycin, cyclosporine, diltiazem, dronedarone, erythromycin, felopdipine, itraconazole, ketoconazole, lopinavir, ritonavir, quercetin, quinidine, verapamil. | Increased concentrations of BCR/ABL inhibitor. Avoid. |
Potent P-glycoprotein inducers | Imatinib, nilotinib, ponatinib | Carbamazepine, phenytoin, St. John's Wort, tipranavir/ritonavir. | Reduced concentrations of BCR/ABL inhibitor. Avoid. |
Potent BCRP inhibitors | Ponatinib | Cyclosporine eltrombopag, gefitinib | Increased concentrations of ponatinib. Exercise caution. |
CYP3A4 substrates | Dasatinib, imatinib, nilotinib, ponatinib | Alfentanil, aprepitant, astemizole, budesonide, buspirone, cisapride, cyclosporine, conivaptan, darifenacin, darunavir, dronedarone, eletriptan, eplerenome, ergotamine, everolimus, felodipine, fentanyl, fluticasone, indinavir, lopinavir, lovastatin, lurasidone, maraviroc, midazolam, nifedipine, nisoldipine, pimozide, quetiapine, saquinavir, sildenafil, somvastatin, sirolimus, tolvaptan, tipranavir, triazolam, vardenafil, triazolam. | Increased concentrations of CYP3A4 substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
CYP2C9 substrates | Dasatinib, imatinib, nilotinib | Acenocoumarol, celecoxib, diclofenac, phenytoin, warfarin, S-warfarin, tolbutamide. | Increased concentrations of CYP2C9 substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
2D6 substrates | Imatinib, nilotinib | Amitriptyline, aripiprazole, atomoxetine, carisoprodol, clomipramine, chlorpromazine, duloxetine, codeine, dextromethorphan, flecainide, haloperidol, imipramine, metoprolol, metoclopramide, mexiletine, mirtazapine, nevibolol, olanzapine, paroxetine, perphenazine, propafenone, R-warfarin, risperidone, tamoxifen, thioridazine, tolterodinetramadol, venlafaxine. | Increased concentrations of 2D6 substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
CYP2C8 substrates | Imatinib, nilotinib | Rosiglitazone, pioglitazone, repaglinide, paclitaxel. | Increased concentrations of CYP2C8 substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
P-glycoprotein substrates | Imatinib, nilotinib, ponatinib | Aliskiren, ambrisentan, cyclosporine, colchicine, dabigatran, digoxin, everolimus, phenoxyphenadine, indinavir, maraviroc, nilotinib, paclitaxel, posaconazole, pravastatin, ritonavir, saxagliptin, sirolimus, sitagliptin, tolvactan, topotecan, verapamil, vincristine. | Increased concentrations of P-glycoprotein substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
BCRP substrates | Dasatinib, imatinib, nilotinib, ponatinib | Daunorubicin, doxorubicin, lapatinib, methotrexate, mitoxantrone, irinotecan, rosuvastatin, sulfasalazine, topotecan. | Increased concentrations of BCRP substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
UGT1A1 substrates | Nilotinib | Atazanavir, dolutegravir, erlotinib, iritotecan, raltegravir. | Increased concentrations of UGT1A1 substrates with an increased risk of toxicity. Avoid drugs with reduced therapeutic index. Exercise caution with the rest. |
UGT1A1 inhibitors | Nilotinib | Atazanavir, dolutegravir, efavirenz, ketoconazole, pazopanib, zafirlukast. | Increased concentrations of nilotinib with an increased potential for toxicity. |