Crizotinib is an oral multi-target tyrosine kinase inhibitor that selectively inhibits the activity of kinases such as anaplastic lymphoma kinase (ALK), ROS1 oncogene (ROS1), and hepatocyte growth factor receptor (c-Met), blocking tumor cell proliferation and survival signaling pathways.

Drug name

Common name: Crizotinib

Product Name: XALKORI ®

indication

Used for treatment:

Adult metastatic non-small cell lung cancer (NSCLC): patients confirmed as ALK or ROS1 positive by FDA approved testing methods

Children aged ≥ 1 and young adults: relapsed or refractory systemic ALK positive anaplastic large cell lymphoma (ALCL)

Adults and children aged ≥ 1 year: unresectable, recurrent, or refractory ALK positive inflammatory myofibroblastic tumor (IMT)

Specifications and characteristics

Capsules:

200mg: Pink opaque cap/white opaque body, printed with "Pfizer" and "CRZ200"

250mg: Pink opaque cap/body with "Pfizer" and "CRZ250" printed on it

Oral granules:

20mg: Light blue opaque cap/white opaque body

50mg: gray opaque cap/light gray opaque body

150mg: Light blue opaque cap/body

main ingredients

Active ingredient: crizotinib

Accessories: Microcrystalline cellulose, anhydrous lactose, sodium stearate fumarate, etc

Coating ingredients: Hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol, etc

Usage and Dosage

Adult NSCLC/IMT: 250mg orally, twice daily

ALCL/IMT for children: 280mg/m ², based on body surface area, twice a day

Medication requirements:

Can be taken with food or on an empty stomach

Swallow the capsule in its entirety, do not chew, crush, or pry open

Oral granules should be poured out of the shell and taken directly or together with a spoon/medicine cup

Dose adjustment

Hepatotoxicity: Pause when ALT/AST>5 × ULN, reduce after recovery

ILD/pneumonia: permanent discontinuation of medication

QT prolongation: Pause when QTc>500ms, reduce after recovery

Renal insufficiency: severe cases require reduction in dosage

Combination use of strong CYP3A inhibitors: Need to reduce dosage

Medication precautions

Diet: Can be taken with food

Missed service: can be replenished within ≤ 12 hours, skipped after>12 hours

Vomiting: No need to supplement, take the next dose according to the original plan

Visual monitoring: Report any visual changes immediately

Avoid: Grapefruits and their products

Medication for special populations

Pregnancy/lactation: contraindicated, contraception is required during treatment and after discontinuation of medication

Children: ALCL/IMT patients aged ≥ 1 year are safe and effective

Liver dysfunction: moderate to severe requiring reduction in dosage

Renal insufficiency: severe cases require reduction in dosage

adverse reaction

Common (≥ 25%):

Visual impairment (63%)

Disgusting (55-56%)

Diarrhea (60-61%)

Vomiting (46-47%)

Edema (31-49%)

Serious:

Hepatotoxicity (11% elevated ALT)

ILD(2.9%)

QT prolongation (2.1%)

contraindication

No absolute contraindications

Drug interactions

Strong CYP3A inhibitors: avoid combination therapy (such as ketoconazole)

Strong CYP3A inducer: Avoid combination therapy (such as rifampicin)

CYP3A substrate: may need to be reduced

Storage method

Store at 20-25 ° C and keep away from light in its original packaging

Oral granules should be taken immediately after opening

Crizotinibinformation