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.

1、 Drug name

1. Common name: crizotinib

2. Product Name: XALKORI

3. English name: Crizotinib

2、 Indications

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

2. Recurrent or refractory, systemic ALK positive anaplastic large cell lymphoma in children (1 year and older) and young adults.

3. Adult and pediatric (1 year and older) unresectable, recurrent, or refractory ALK positive inflammatory myofibroblastic tumor.

3、 Specifications and characteristics

Tablets: 250 milligrams.

4、 Main components

Active ingredient: crizotinib.

5、 Usage and dosage

1. Administration route: Oral.

2. Adult non-small cell lung cancer/inflammatory myofibroblastic tumor: The recommended dose is 250 milligrams twice daily.

3. Childhood and young adult anaplastic large cell lymphoma/childhood inflammatory myofibroblastic tumor: The recommended dose is based on body surface area and is 280 milligrams per square meter, twice daily. For specific dosage combinations, please refer to the corresponding table of body surface area in the instruction manual.

4. Course of treatment: Continue treatment until disease progression or unacceptable toxicity occurs.

6、 Dose adjustment

1. Regarding adverse reactions: Depending on the severity of the adverse reactions, medication should be temporarily suspended, the dosage reduced, or permanently discontinued. Adults usually reduce their dosage to 200 milligrams twice a day for the first dose and to 250 milligrams once a day for the second dose. The dosage adjustment for children and young adults is based on body surface area, please refer to the corresponding table in the instruction manual for details.

2. For liver injury: patients with moderate liver injury need to reduce their dosage for the first time, and patients with severe liver injury need to reduce their dosage for the second time.

3. For patients with severe kidney injury who do not require dialysis, a second dose reduction is required.

4. Regarding drug interactions: If it is necessary to use it in combination with potent CYP3A inhibitors, crizotinib should be reduced to the second dose level.

7、 Medication precautions

1. Medication time: can be taken with food or on an empty stomach.

2. Missed dose: If one dose is missed, it should be taken as soon as possible, unless less than 6 hours before the next dose, the missed dose should be skipped and the next dose should be taken according to the original plan.

3. Post vomiting treatment: If vomiting occurs after taking medication, additional doses should not be taken, and the next dose should be taken according to the original plan.

4. It should be swallowed whole and should not be chewed, crushed, or dissolved.

8、 Medication for special populations

1. Pregnant women: May cause harm to the fetus, and pregnant women should be informed of the risks. Women of childbearing age should take effective contraceptive measures during treatment and within 45 days after the last dose.

2. Breastfeeding period: It is recommended not to breastfeed during the treatment period and within 45 days after the last dose.

3. Male patients: Male patients with female partners should use condoms during treatment and within 90 days after the last dose.

4. Children: Safety and efficacy have been established in children aged 1 year and older with anaplastic large cell lymphoma and inflammatory myofibroblastic tumor. The safety and efficacy in children under 1 year old or children with non-small cell lung cancer have not been established.

5. Elderly: No overall safety or efficacy differences were observed in elderly patients with non-small cell lung cancer.

6. Liver/kidney dysfunction: Patients with moderate or severe liver injury or severe kidney injury need to adjust the dosage.

9、 Adverse reactions

1. Common adverse reactions (incidence ≥ 35%):

Adult non-small cell lung cancer: visual impairment, nausea, diarrhea, vomiting, edema, constipation, elevated transaminase levels, fatigue, decreased appetite, upper respiratory tract infection, dizziness, neuropathy.

Patients with anaplastic large cell lymphoma: diarrhea, vomiting, nausea, visual impairment, headache, musculoskeletal pain, stomatitis, fatigue, decreased appetite, fever, abdominal pain, cough, itching.

Inflammatory myofibroblastic tumor in adults: visual impairment, nausea, edema.

Children with inflammatory myofibroblastic tumor: vomiting, nausea, diarrhea, abdominal pain, rash, visual impairment, upper respiratory tract infection, cough, fever, musculoskeletal pain, fatigue, edema, constipation, headache.

2. Serious adverse reactions: including liver toxicity, interstitial lung disease/pneumonia, QT interval prolongation, bradycardia, severe vision loss, gastrointestinal toxicity, etc.

10、 Contraindications

None.

11、 Drug interactions

1. Should be avoided in combination with potent CYP3A inhibitors or inducers.

2. Co administration with CYP3A substrates with narrow therapeutic windows should be avoided.

3. It should be avoided to use drugs that can prolong the QT interval in combination.

4. It should be avoided to use drugs that can cause bradycardia in combination.

5. Avoid consuming grapefruit or drinking grapefruit juice.

12、 Storage method

1. Store at room temperature between 20 ° C and 25 ° C, and allow for short distance transportation between 15 ° C and 30 ° C.

2. Please keep out of reach of children.

Crizotinibinformation