Drugs that may alter Gleevec plasma concentrations (Long List)

also see: CYTOCHROME P450 DRUG INTERACTION TABLE

Note: CYP3A4 is the main enzyme that metabolizes Gleevec and therefore effects may be more pronounced that those related to CYP2D6


Drugs that Induce CYP3A4
Reduce Gleevec levels
  • May result in sub-therapeutic levels of Gleevec

  • May be more of a concern for lower doses of Gleevec

  • CYP3A4 inducers
• Carbamazepine
• Dexamethasone
• Ethosuximide
• Glucocorticoids
• Griseofulvin
• Phenytoin
• Primidone
• Progesterone
• Rifabutin
• Rifampin
• Nafcillin
• Nelfinavir
• Nevirapine
• Oxcarbazepine
• Phenobarbital
• Phenylbutazone
• Rofecoxib (mild)
• St John’s wort
• Sulfadimidine
• Sulfinpyrazone
• Troglitazone
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

 
 
 
 
 
Drugs that Inhibit CYP3A4
Increase Gleevec levels
  • May result in above normal levels of Gleevec

  • May be more of a concern for higher doses of Gleevec

  • CYP3A4 inhibitors
• Amiodarone
• Anastrozole
• Azithromzcin
• Cannabinoids
• Cimetidine
• Clarithromycin
• Clotrimazole
• Cyclosporine
• Danazol
• Delavirdine
• Dexamethasone
• Diethyldithiocarbamate
• Diltiazem
• Dirithyromycin
• Disulfiram
• Entacapone (high dose)
• Erythromycin
• Ethinyl estradiol
• Fluconazole
• Fluoxetine
• Fluvoxamine
• Gestodene
• Grapefruit juice
• Indinavir
• Isoniazid
• Ketoconazole
• Metronidazole
• Mibefradil
• Miconazole
• Nefazodone
• Nelfinavir
• Nevirapine
• Norfloxacin
• Norfluoxetine
• Omeprazole
• Oxiconazole
• Paroxetine (weak)
• Propoxyphene
• Quinidine
• Quinine
• Quinupristine and dalfopristin
• Ranitidine
• Ritonavir
• Saquinavir
• Sertindole
• Sertraline
• Troglitazone
• Troleandomycin
• Valproic acid

Drugs that Induce CYP2D6
May Reduce Gleevec levels
  • May result in sub-therapeutic levels of Gleevec

  • May be more of a concern for lower doses of Gleevec

  • CYP2D6 inducers
• Dexamethasone
• Rifampin
 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
Drugs that Inhibit CYP2D6
May Increase Gleevec levels
  • May result in above normal levels of Gleevec

  • May be more of a concern for higher doses of Gleevec

  • CYP2D6 inhibitors
• Amiodarone
• Celecoxib
• Chloroquine
• Chlorpromazine
• Cimetidine
• Citalopram
• Clomipramine
• Codeine
• Delavirdine
• Desipramine
• Dextropropoxyphene
• Diltiazem
• Doxorubicin
• Entacapone (high dose)
• Fluoxetine
• Fluphenazine
• Fluvaxamine
• Haloperidol
• Labetalol
• Lobeline
• Lomustine
• Methadone
• Mibefradil
• Moclobemide
• Nortuloxeline
• Paroxetine
• Perphenazine
• Propafenone
• Quinacrine
• Quinidine
• Ranitidine  (ranitidine, Zantac)
• Risperidone (weak)
• Ritonavir
• Serindole
• Sertraline (weak)
• Thioridazine
• Valproic acid
• Venlafaxine (weak)
• Vinblastine
• Vincristine
• Vinorelbine
• Yohimbine

Note: This page is for educational use and thus is not intended to provide medical advice; please inform your physician or pharmacist of any prescription or over-the-counter medications or supplements you may be taking, and ask them if you have any questions regarding any possible interactions. While we do make an effort to keep this list updated, it may not be complete. Please refer to a site like CYTOCHROME P450 DRUG INTERACTION TABLE and/or your medication’s prescribing information for more definitive information.

For more information about Gleevec see Full Prescribing Information.
For more information about Sutent see Full Prescribing Information.
For more information about Stivarga see Full Prescribing Information.

Reference

Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007) Accessed 6/29/16.

Core Values