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

Source

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