Crizotinib

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

Drug name

Common name: Crizotinib

Trade name: XALKORI®

Indications

Used for the treatment of:

1. Adult metastatic non-small cell lung cancer NSCLC :Patients who are ALK or ROS1 positive confirmed by FDA-approved testing methods

2. Children ≥1 year old and young adults :Relapsed or refractory systemic ALK-positive anaplastic large cell lymphoma (A LCL)

3. Adults and children ≥1 year old :Unresectable, recurrent or refractory ALK-positive inflammatory myofibroblastic tumor (IMT)

Specifications and properties

Capsule :

250mg: Pink opaque cap/body, imprinted with "Pfizer" and "CRZ250"

Oral granules : < /b>

20mg: light blue opaque cap/white opaque body

50mg: gray opaque cap/light gray opaque body

150mg: light blue opaque cap/body

Main ingredients

Activity Ingredients: crizotinib

Excipients: microcrystalline cellulose, anhydrous lactose, sodium stearyl fumarate, etc.

Coating ingredients: hypromellose, titanium dioxide, polyethylene glycol, etc.

Usage and dosage

Adult NSCLC/IMT : < /b>250mg orally, twice daily

Children ALCL/IMT :280mg/m² based on body surface area, twice daily

Dosage requirements :

Can be taken with food or on an empty stomach

Swallow the capsule whole and do not chew, crush or break it

Oral capsules need to be poured out of the shell and taken directly or used with a spoon/medicine cup

Dose adjustment

1. Hepatotoxicity :Suspend when ALT/AST>5×ULN, and after recovery Reduction

2. ILD/pneumonia : Permanent discontinuation

3. QT prolongation : Pause at QTc>500ms, reduce dose after recovery

4. Renal insufficiency : Severe cases need to reduce the dose

5. Strong CYP3A inhibitors are used in combination with : The dose needs to be reduced

Drug precautions

Diet : Can be taken with food

Missed dose of :< /b>≤12 hours can be retaken, >12 hours skipped

Vomiting : No need to retake, take the next dose as originally planned

Visual monitoring : Report immediately if visual changes occur

Avoid u200 c: Grapefruit and its products

Usage for special groups

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

Children : Safe and effective for ALCL/IMT patients ≥1 year old

Hepatic insufficiency : Moderate to severe dosage reduction is required

Renal insufficiency : Severe cases require dosage reduction

Adverse reactions

Common (≥25%) : p>

Visual disturbance (63%), nausea (55-56%), diarrhea (60-61%), vomiting (46-47%), edema (31-49%)

Severe :

Hepatotoxicity (11% ALT elevation), ILD ( 2.9%), QT prolongation (2.1%)

Contraindications

No absolute contraindications

Drug interactions

Strong CYP3A inhibitor :Avoid combined use (such as ketoconazole)

Strong CYP3A inducer : Avoid combined use (such as rifampin)

CYP3A substrate : May need to be reduced

Storage method

Save at 20-25°C and store in original packaging away from light

Oral granules should be taken immediately after opening