【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, metastatic (ALK-positive): Treatment of metastatic non-small cell lung cancer in adults whose tumors are ALK-positive

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

Absorption: Rapid
Distribution: Vss: 305 L.
Protein binding: 66%; to plasma proteins.
Metabolism: Primarily via CYP3A4 and UGT1A4, with minor contribution from CYP2C8, CYP2C19, CYP3A5, and UGT1A3.
Bioavailability: 81%.
Half-life elimination: 24 hours.
Time to peak: 1.2 hours (range: 0.5 to 4 hours) following a single dose; 2 hours (range: 0.5 to 23 hours) at steady state.
Excretion: Urine: 48% (<1% as unchanged drug); feces: 41% (~9% as unchanged drug).
Clearance (CL/F), mean: 11 L/hour (following a single 100 mg dose) and 18 L/hour at steady state.

Concomitant use of strong CYP3A inducers

Based on the mechanism of action and data from animal reproduction studies, lorlatinib may cause fetal harm if administered during pregnancy.

It is not known if lorlatinib 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 and for 7 days after the last lorlatinib dose.

Cardiovascular: Edema (57%)
Central nervous system: Peripheral neuropathy (47%; grade 3/4: 3%), cognitive dysfunction (27% to 29%), fatigue (26%), mood disorder (23% to 24%), headache (18%), dizziness (16%), speech disturbance (12% to 14%), sleep disorder (10%)
Dermatologic: Skin rash (14%)
Endocrine & metabolic: Hypercholesterolemia (96%), hypertriglyceridemia (90%), hyperglycemia (52%), hypoalbuminemia (33%), weight gain (24%), increased amylase (22%), hyperkalemia (21%), hypomagnesemia (21%), hypophosphatemia (21%)
Gastrointestinal: Increased serum lipase (24%), diarrhea (22%), nausea (18%), constipation (15%), vomiting (12%)
Hematologic & oncologic: Anemia (52%; grade 3/4: 5%), thrombocytopenia (23%; grade 3/4: <1%), lymphocytopenia (22%; grades 3/4: 3%)
Hepatic: Increased serum aspartate aminotransferase (37%), increased serum alanine aminotransferase (28%), increased serum alkaline phosphatase (24%)
Neuromuscular & skeletal: Arthralgia (23%), myalgia (17%), back pain (13%), limb pain (13%)
Ophthalmic: Visual disturbance (15%)
Respiratory: Dyspnea (27%), cough (18%), upper respiratory tract infection (12%)
Miscellaneous: Fever (12%)

Non-small cell lung cancer, metastatic (ALK-positive): Oral: 100 mg once daily until disease progression or unacceptable toxicity
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance.

CrCl 30 to 89 mL/minute: No dosage adjustment necessary.
CrCl 15 to <30 mL/minute: Reduce dose to 75 mg once daily.

Mild impairment (total bilirubin ? ULN with AST > ULN or total bilirubin >1 to 1.5 times ULN with any AST): No dosage adjustment necessary.
Moderate impairment (total bilirubin ?1.5 to 3 times ULN with any AST) or severe impairment (total bilirubin >3 times ULN with any AST): There are no dosage adjustments provided in the manufacturer's labeling (has not been established).