ALECENSA® (alectinib) capsule
|Mechanism of Action||Tyrosine kinase inhibitor targeting anaplastic lymphoma kinase & rearranged during transfection|
|Dosage||600 mg twice daily|
|Pharmacodynamics (PD)||QT interval prologation assessed at 600 243 mg twice daily|
|Pharmacokinetics (PK)||Major active metabolite M4 by CYP3A4
Dose-proportional increases over the dose range of 460 mg to 900 mg (daily
Mean accumulation ~6-fold for both at steady-state
Tmax 4 hour
T1/2 33 hr (alectinib), 31 hr ( M4)
Absolute bioavailability 37%
High-fat, high-calorie meal increased the combined exposure by 3.1-fold
Plasma protein binding 99% for both
Excretion in feces 84% as alectinib, 6% as M4.
|PK-PD Analysis||Have not been reported|
|Population PK||Have not been reported.
|Special Populations||No dose adjustment mild and moderate renal impairment, mild hepatic impairment.
Age, body weight, mild hepatic impairment, mild to moderate renal impairment, race, and sex no clinically meaningful effect on systemic exposures of alectinib and M4.
|Drug Interactions||Strong CYP3A inhibitor or a strong CYP3A inducer or an acid-reducing agent (esomeprazole) no clinically meaningful effect|