. 2003 Nov 11;89(10):1855–1859. doi: 10.1038/sj.bjc.6601152

Table 4. Substrates of cytochrome P450 enzymes CYP3A3/4.

Substrates: imatinib may increase the potency of these drugs
Acetaminophen, Alfentanil, Alosetron, Alprazolam, Amiodarone, Amitriptyline (minor), Amlodipine, Anastrozole, Androsterone, Antipyrine, Astemizole, Atorvastatin, Benzphetamine, Bepridil, Bexarotene, Bromazepam, Bromocriptine, Budesonide, Bupropion (minor), Buspirone, Busulphan, Caffeine, Cannabinoids, Carbamazepine, Cerivastatin, Cevimeline, Chlorpromazine, Cimetidine, Cisapride, Citalopram, Clarithromycin, Clindamycin, Clomipramine, Clonazepam, Clozapine, Cocaine, Codeine (demethylation), Cortisol, Cortisone, Cyclobenzaprine (demethylation), Cyclophosphamide, Cyclosporine, Dapsone, Dehydroepiandrostendione, Delavirdine, Desmethyldiazepam, Dexamethasone, Dextromethorphan (minor, N-demethylation), Diazepam (minor;hydroxylation, N-demethylation), Digitoxin, Diltiazem, Disopyramide, Docetaxel, Dofetilide (minor), Dolasetron, Donepezil, Doxorubicin, Doxycycline, Dronabinol, Enalapril, Erythromycin, Estradiol, Ethinyl Estradiol, Ethosuximide, Etoposide, Exemestene, Felodipine, Fentanyl, Fexotenadine, Finasteride, Fluoxetine, Flutamide, Glyburide, Granisetron, Halofantrine, Hydrocortisone, Hydroxyarginine, Ifosfamide, Imipramine, Indinavir, Isradipine, Itraconazole, Ketoconazole, Lansoprazole (minor), Letrozole, Levobupivicaine, Lidocaine, Loratadine, Losartan, Lovastatin, Methadone, Mibefradil, Miconazole, Midazolam, Mifepristone, Mirtazapine (N-demethylation), Montelukast, Navelbine, Nefazodone, Nelfinavir, Nevirapine, Nicardipine, Nifedipine, Niludipine, Nimodipine, Nisoldipine, Nitrendipine, Omeprazole (sulfonation), Ondansetron, Oral contraceptives, Orphenadrine, Paclitaxel, Pantoprazole, Pimozide, Pioglitazone, Pravastatin, Prednisone, Progesterone, Proguanil, Propafenone, Quercetin, Quetiapine, Quinidine, Quinine, Repaglinide, Retinoic acid, Rifampin, Risperidone, Ritonavir, Salmeterol, Saquinavir, Sertindole, Sertraline, Sibutramine, Sildenalfil citrate, Simvastatin, Sirolimus, Sufentanil, Tacrolimus, Tamoxifen, Temazepam, Teniposide, Terfenadine, Testosterone, Tetrahydrocannabinol, Theophylline, Tiagabine, Tolterodine, Toremifene, Trazodone, Tretinoin, Triazolam, Troglitazone, Troleandomycin, Venlafaxine (N-demethylation), Verapamil, Vinblastine, Vincristine, Warfarin (R-warfarin), Yohimbine, Zaleplon (minor pathway), Zatoestron, Zileuton, Ziprasidone, Zolpidem, Zonisamide.

Substrates: imatinib may increase the potency of these drugs

Acetaminophen, Alfentanil, Alosetron, Alprazolam, Amiodarone, Amitriptyline (minor), Amlodipine, Anastrozole, Androsterone, Antipyrine, Astemizole, Atorvastatin, Benzphetamine, Bepridil, Bexarotene, Bromazepam, Bromocriptine, Budesonide, Bupropion (minor), Buspirone, Busulphan, Caffeine, Cannabinoids, Carbamazepine, Cerivastatin, Cevimeline, Chlorpromazine, Cimetidine, Cisapride, Citalopram, Clarithromycin, Clindamycin, Clomipramine, Clonazepam, Clozapine, Cocaine, Codeine (demethylation), Cortisol, Cortisone, Cyclobenzaprine (demethylation), Cyclophosphamide, Cyclosporine, Dapsone, Dehydroepiandrostendione, Delavirdine, Desmethyldiazepam, Dexamethasone, Dextromethorphan (minor, N-demethylation), Diazepam (minor;hydroxylation, N-demethylation), Digitoxin, Diltiazem, Disopyramide, Docetaxel, Dofetilide (minor), Dolasetron, Donepezil, Doxorubicin, Doxycycline, Dronabinol, Enalapril, Erythromycin, Estradiol, Ethinyl Estradiol, Ethosuximide, Etoposide, Exemestene, Felodipine, Fentanyl, Fexotenadine, Finasteride, Fluoxetine, Flutamide, Glyburide, Granisetron, Halofantrine, Hydrocortisone, Hydroxyarginine, Ifosfamide, Imipramine, Indinavir, Isradipine, Itraconazole, Ketoconazole, Lansoprazole (minor), Letrozole, Levobupivicaine, Lidocaine, Loratadine, Losartan, Lovastatin, Methadone, Mibefradil, Miconazole, Midazolam, Mifepristone, Mirtazapine (N-demethylation), Montelukast, Navelbine, Nefazodone, Nelfinavir, Nevirapine, Nicardipine, Nifedipine, Niludipine, Nimodipine, Nisoldipine, Nitrendipine, Omeprazole (sulfonation), Ondansetron, Oral contraceptives, Orphenadrine, Paclitaxel, Pantoprazole, Pimozide, Pioglitazone, Pravastatin, Prednisone, Progesterone, Proguanil, Propafenone, Quercetin, Quetiapine, Quinidine, Quinine, Repaglinide, Retinoic acid, Rifampin, Risperidone, Ritonavir, Salmeterol, Saquinavir, Sertindole, Sertraline, Sibutramine, Sildenalfil citrate, Simvastatin, Sirolimus, Sufentanil, Tacrolimus, Tamoxifen, Temazepam, Teniposide, Terfenadine, Testosterone, Tetrahydrocannabinol, Theophylline, Tiagabine, Tolterodine, Toremifene, Trazodone, Tretinoin, Triazolam, Troglitazone, Troleandomycin, Venlafaxine (N-demethylation), Verapamil, Vinblastine, Vincristine, Warfarin (R-warfarin), Yohimbine, Zaleplon (minor pathway), Zatoestron, Zileuton, Ziprasidone, Zolpidem, Zonisamide.

Simvastatin in bold is a substrate for CYP3A4 and in this study, coadministration with imatinib resulted in significantly increased mean maximum concentration and area under concentration–time curve values for simvastatin. One might expect coadministration with imatinib to increase the potency of these drugs. Caution is also required with drugs which induce or inhibit CPY3A4. Adapted from Cytochrome P-450 Enzymes and Drug metabolism. (In: Lacy CF, Armstrong LL, Goldman MP, Lance LL (eds) Drug Information Handbook, 8th edn. Hudson, OH: LexiComp Inc. 2000: pp 1364–1371).