Crizotinib
Generic Details
Generic Name
Crizotinib
Other Names
- Xalkori
Drug Class
- Kinase inhibitor
Chemical Formula
C21H22Cl2FN5O
Molecular Weight
450.343 g/mol
Mechanism of Action
- Inhibits receptor tyrosine kinases including ALK and MET proteins
Indications
- Non-small cell lung cancer (NSCLC) with ALK rearrangement
- ROS1-positive metastatic NSCLC
- Advanced or metastatic ALK-positive or ROS1-positive solid tumors
Common Dosage Forms
- Capsule
Typical Dosage
- 250 mg orally twice daily
- With or without food
Pediatric Dosage
- Safety and efficacy not established in children
Geriatric Dosage
- No specific dosage adjustments
Side Effects
- Nausea
- Vomiting
- Diarrhea
- Edema
- Liver function test abnormalities
- Visual disturbances
- Interstitial lung disease
- QT interval prolongation
Contraindications
- Hypersensitivity to crizotinib
Pregnancy Category
- D (US)
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Strong CYP3A inhibitors/inducers
- Strong CYP2B6 inhibitors
- P-gp substrates
Overdose Symptoms
- Bradycardia
- Hypotension
- Vomiting
- Visual disturbances
Antidote for Overdose
- No specific antidote
Storage Conditions
- Store at 20°C to 25°C (68°F to 77°F)
- Excursions permitted between 15°C and 30°C (59°F and 86°F)
Pharmacokinetics
- Absorption: Rapid and extensive
- Distribution: Widely distributed, crosses the blood-brain barrier
- Metabolism: Primarily hepatic via CYP3A4
- Excretion: Mainly feces (63%) and urine (22%)
Precautions
- Hepatotoxicity
- Interstitial lung disease/pneumonitis
- QTc prolongation
- Bradycardia
- Visual disturbances
- Renal impairment
Warnings
- Hepatotoxicity
- Interstitial lung disease/pneumonitis
- QTc prolongation
- Bradycardia
- Embryo-fetal toxicity