Erlotinib - Overall Recommendations
Erlotinib CAN be Co-Administered with the Following Agents
Erlotinib CAN be Co-Administered with the Following Agents, IF Administered with Caution
- Ciprofloxacin (inhibits both CYP3A4 and CYP1A2)1,2
- Potent CYP1A2 inhibitors (e.g. fluvoxamine)1
- P-glycoprotein inhibitors (e.g. cyclosporine, verapamil)1
Erlotinib CANNOT be Co-Administered with the Following Agents
- Potent CYP3A4 inhibitors (e.g. ketoconazole)1,2
- Potent CYP3A4 inducers (e.g. rifampicin)1,2
- Proton pump inhibitors (other drugs that alter gastric pH should also be avoided)1,2
- Platinum-based chemotherapy2
Additional Important Information when Prescribing Erlotinib
If co-administration of erlotinib and strong CYP3A4 inhibitors is necessary and toxicity occurs, use with caution and reduce the erlotinib dose in 50-mg decrements.2-4
If co-administration of a CYP3A4 inducer is necessary, increase the erlotinib dose in 50-mg increments at 2-week intervals as tolerated, to a maximum of 450 mg.2
In smokers, increase the erlotinib dose by 50-mg increments at 2-week intervals to a maximum of 300 mg; immediately reduce to the recommended dose upon cessation of smoking.2
Co-administration of erlotinib and medicines that alter gastric pH:1,2
- avoid concomitant use of proton pump inhibitors, as separation of doses may not eliminate the interaction
- if an H2-Receptor antagonist (e.g. ranitidine) is required, erlotinib must be taken ≥2 hours before or 10 hours after the H2-receptor antagonist
- if needed, antacids should be taken ≥4 hours before or 2 hours after erlotinib.
Prothrombin time and INR should be regularly monitored in patients taking warfarin or other coumarin-derived anticoagulants.1,2
Erlotinib is not recommended in combination with platinum-based chemotherapy.2 Erlotinib increases platinum concentrations; although the magnitude of this increase is not considered clinically relevant, in clinical practice factors such as renal impairment may lead to increased exposure to carboplatin.1
- European Medicines Agency. Erlotinib (TARCEVA). Summary of Product Characteristics. 2015.
- Food and Drug Administration. Erlotinib (TARCEVA) Prescribing information. 2015.
- van Leeuwen RW, van Gelder T, Mathijssen RH, Jansman FG. Drug-drug interactions with tyrosine-kinase inhibitors: a clinical perspective. Lancet Oncol 2014; 15: e315-326.
- Teo YL, Ho HK, Chan A. Metabolism-related pharmacokinetic drug-drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations. Br J Clin Pharmacol 2015; 79: 241-253.