Drug reference

Lorlatinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

RifampinSevereTextbookG&G 14e · p1388
ApalutamideSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
AvapritinibSevereDatabaseDDInter

Mechanism

Lorlatinib is a tyrosine kinase inhibitor, specifically acting as an anaplastic lymphoma kinase (ALK) inhibitor. It also demonstrates significant clinical activity in ROS1-positive non-small cell lung cancer (NSCLC). This agent is noted for its impressive intracranial activity, leading to significant and durable intracranial responses.

Indications

Anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (specialist use only)ROS1-positive non-small cell lung cancermetastatic, ALK-positive NSCLC who failed 1 or 2 prior ALK inhibitorsfirst-line treatment for metastatic, ALK-positive NSCLC

Dosing

Adult: By mouth: 100 mg daily. For dose adjustments due to side-effects, consult product literature. If concomitant use with potent CYP3A4 inhibitors is unavoidable, reduce starting dose to 75 mg once daily.

Pharmacokinetics

Half-life

24 h

Metabolism

CYP3A4

Contraindications

Patients with cardiac risk factors or conditions which may affect left ventricular ejection fraction (requires cardiac monitoring)
Lactose intolerance (consider formulation)
Worsening respiratory symptoms indicative of interstitial lung disease or pneumonitis (requires withholding or permanent discontinuation)

Side effects

Common

AnaemiaAnxietyArthralgiaAstheniaBehaviour abnormalCognitive disorderConcentration impairedConfusionConstipationDeliriumDementiaDepressionDiarrhoeaDyslipidaemiaGait abnormalHallucinationsHeadacheInflammationLearning disabilityMemory lossMental impairment (thought disturbance)Mood alteredMuscle weaknessMyalgiaNauseaNerve disorders

Serious