【藥品庫存】 本藥品為臨時採購藥品，經院長核可後，限定特定科別、病人使用。

Non-small cell lung cancer (NSCLC), metastatic (ALK-positive)

Antineoplastic Agent, Anaplastic Lymphoma Kinase Inhibitor; Antineoplastic Agent, Tyrosine Kinase Inhibitor

Absorption: A high-fat, high-calorie meal increased the combined exposure of alectinib plus its active metabolite M4 by 3.1-fold
Distribution: Parent drug: 4,016 L; M4 (active metabolite): 10,093 L; distributes in the CSF at approximately the free concentrations in plasma
Protein binding: >99% to plasma proteins
Metabolism: Hepatic via CYP3A4 to major active metabolite M4; M4 is also metabolized by CYP3A4
Bioavailability: 37% (under fed conditions)
Half-life elimination: Parent drug: 33 hours; M4: 31 hours
Time to peak: 4 hours
Excretion: Feces (98%; 84% as unchanged parent drug and 6% as M4); urine (<0.5%)

There are no contraindications listed in the manufacturer’s US labeling.
Canadian labeling: Known hypersensitivity to alectinib or any component of the formulation.

Based on data from animal reproduction studies and its mechanism of action, alectinib may be expected to cause fetal harm if administered during pregnancy.

It is not known if alectinib is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, the manufacturer does not recommend breastfeeding during therapy or for 1 week after the final dose.

>10%:
Cardiovascular: Edema (30%), bradycardia (8% to 18%)
Central nervous system: Fatigue (?41%), headache (17%)
Dermatologic: Skin rash (18%)
Endocrine & metabolic: Hyperglycemia (36%), hypocalcemia (32%), hypokalemia (29%), hypophosphatemia (21%), hyponatremia (20%), weight gain (11%)
Gastrointestinal: Constipation (34%), nausea (18%), diarrhea (16%), vomiting (12%)
Hematologic & oncologic: Anemia (56%, grades 3/4: 2%), lymphocytopenia (22%, grades 3/4: 5%)
Hepatic: Increased serum AST (51%), increased serum alkaline phosphatase (47%), hyperbilirubinemia (39%), increased serum ALT (34%)
Neuromuscular & skeletal: Increased creatine phosphokinase (43%), weakness (?41%), musculoskeletal pain (?29%), myalgia (?29%), back pain (12%)
Renal: Increased serum creatinine (28%)
Respiratory: Cough (19%), dyspnea (16%)
1% to 10%:Cardiovascular: Pulmonary embolism (1%)
Dermatologic: Skin photosensitivity (10%)
Ophthalmic: Visual disturbances (10%)
Renal: Renal insufficiency (8%)

Oral: 600 mg twice daily; continue until disease progression or unacceptable toxicity (Ou 2016; Peters 2017)

Missed doses: If a dose is missed or if vomiting occurs, take the next dose at the regularly scheduled time.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Recommended alectinib dosage reductions for toxicity:
Initial starting dose: 600 mg twice daily
First dose reduction: 450 mg twice daily
Second dose reduction: 300 mg twice daily
If unable to tolerate 300 mg twice daily, discontinue alectinib

CrCl ?30 mL/minute: No dosage adjustment is necessary.
CrCl <30 mL/minute or ESRD: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
Renal toxicity during treatment:Grade 3 renal impairment: Withhold alectinib until serum creatinine recovers to ?1.5 times ULN, then resume at reduced dose (see Dosage Adjustment for Toxicity for recommended alectinib dosage reduction levels).
Grade 4 renal impairment: Permanently discontinue.

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment is necessary.
Severe impairment (Child-Pugh class C): 450 mg twice daily
Hepatotoxicity during treatment:
ALT or AST >5 times ULN and total bilirubin ?2 times ULN: Withhold alectinib; upon recovery to baseline or to ALT/AST ?3 times ULN, may resume at a reduced dose (see Dosage Adjustment for Toxicity for recommended alectinib dosage reduction levels).
ALT or AST >3 times ULN and total bilirubin >2 times ULN (in the absence of cholestasis or hemolysis): Permanently discontinue.
Total bilirubin >3 times ULN: Withhold alectinib; upon recovery to baseline or to total bilirubin ?1.5 times ULN, may resume at a reduced dose (see Dosage Adjustment for Toxicity for recommended alectinib dosage reduction levels).

仿單:請勿存放於超過30度環境，避光避熱