Tyrosine Kinase Inhibitors Flashcards
Imatinib
- First generation TKI
- Recommended initial dose = 400 mg once daily for CP-CML
- Recommended initial dose = 600 mg once daily for AP-CML and BP- CML
Imatinib DDI w/ Antidepressants
Minor increase in exposure; Monitor QTc monitoring
Imatinib DDI w/ Cardiovascular Meds
Increase in exposure; strongly consider alternative cardiac medication or TKI dose adjustment
Imatinib DDI w/ Anti-infectives
Increase in exposure
Imatinib Side Effects
~ fluid retention
~ GI upset
~ Muscle cramps
~ rash
Nilotinib Dosing : newly diagnosed CP-CML
300 mg twice daily
Nilotinib Dosing: resistant or intolerant CP-CML and AP-CML
400 mg twice daily
Nilotinib Dosing: BP-CML
400 mg twice daily
Nilotinib prolongs the…
QT interval
ECGs should be obtained at baseline, 7 days after initiation, and periodically thereafter, as well as following any dose adjustments
Nilotinib DDI w/ PPIs
decrease in exposure
Nilotinib DDI w/ H2RAs
decrease in exposure; AVOID; if absolutely necessary consider once daily H2RA greater than or equal to 2 hours after or greater than 10 hours before taking nilotinib
Nilotinib DDI w/ Antacids
decrease in exposure if concomitant; use antacids at least 2 hours before or at least 2 hours after taking
Nilotinib DDI w/ antidepressants
AVOID d/t cumulative QTc prolongation risk
Nilotinib DDI w/ CV Medications
increase in exposure and arrhythmia risk; AVOID
Nilotinib DDI w/ anti-infectives (azole antifungals, clarithromycin, telithromycin, ritonavir)
increase in exposure
Nilotinib Dosing Considerations
avoid food 2 hours before and 1 hour after taking