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Cabozantinib is a multi-target tyrosine kinase inhibitor (TKI) that blocks tumor angiogenesis and inhibits tumor cell proliferation and metastasis by selectively inhibiting the activity of MET, VEGFR-1/2/3, AXL, RET, ROS1 and other receptor tyrosine kinases.
Cabozantinib is a multi-target tyrosine kinase inhibitor, suitable for the following conditions:
1. Renal cell carcinoma (RCC) : Monotherapy for patients with advanced renal cell carcinoma, combined with nivolumab as first-line treatment for advanced RCC
2. Hepatocellular carcinoma (HCC) : Treatment of patients with hepatocellular carcinoma who have received sorafenib
3. Differentiated thyroid cancer (DTC) : Treatment of locally advanced patients aged 12 years and above who are refractory to radioactive iodine or are not suitable for radioactive iodine therapy Or patients with metastatic DTC who have previously received VEGFR-targeted therapy after progression
4. Neuroendocrine tumors (NETs) :Treatment of previously treated unresectable locally advanced or metastatic pancreatic (pNET) or extrapancreatic (epNET) high score 12 years and older Neuroendocrine tumors
Adults and adolescents weighing ≥40kg: 60 mg orally once a day (monotherapy)
Combined with nivolumab: 40 mg once a day< /p>
Adolescents weighing <40kg: 40mg once a day
Dosage requirements : Take on an empty stomach (1 hour before a meal or 2 hours after a meal), swallow the whole tablet without crushing/chewing
Gradually reduce the dose according to the severity of adverse reactions to 40 mg or 20 mg once a day
Serious adverse reactions require permanent discontinuation
Surgical management : Stop the drug 3 weeks before surgery, resume medication at least 2 weeks after the surgery and after the wound has healed
Handling of missed doses : If the dose is missed for more than 12 hours, skip the dose and take the medication normally the next day< /p>
Monotherapy : Diarrhea, fatigue, hand-foot skin reaction, decreased appetite, hypertension, nausea, vomiting, weight loss
Combined treatment : Diarrhea, fatigue, hepatotoxicity, stomatitis, rash, hypertension, hypothyroidism, musculoskeletal pain
Bleeding risk : Fatal bleeding may occur, and it is contraindicated in patients with a recent history of bleeding.
Perforation/Fistula : Monitor for gastrointestinal symptoms and seek immediate medical attention if abdominal pain occurs.
Thrombus events : such as myocardial infarction, pulmonary embolism, etc., the drug needs to be stopped immediately.
Hypertensive crisis : Monitor blood pressure regularly during treatment. If control is not good, dose adjustment is required.
Hepatotoxicity : More common when combined with nivolumab, liver function needs to be monitored regularly.
Wound healing disorder : Medication needs to be suspended before and after elective surgery.
Osteonecrosis of the jaw : An oral examination is required before treatment. Treatment must be interrupted if there is jaw pain.
Embryotoxicity : Contraindicated for pregnant women. Patients of childbearing age need to take effective contraceptive measures.
Pregnant women: : may cause fetal damage. Contraception is required during medication and within 4 months of stopping the medication.
Lactation period : Breastfeeding is prohibited during treatment and within 4 weeks of drug withdrawal.
Children : Adolescents over 12 years old need to monitor bone growth.
Liver damage : Moderate liver damage requires dose reduction, severe liver damage avoid use.
Avoid combined use of : Strong CYP3A4 inhibitors (such as ketoconazole), strong/moderate CYP3A4 inducers (such as rifampicin).
Antacid : An interval of 4 hours (before) or 10 hours (after) should be used in combination with proton pump inhibitors.
Renal cell carcinoma : The median progression-free survival (PFS) was 8.6 months with single drug and 16.6 months with nivolumab.
Hepatocellular carcinoma : Median overall survival (OS) 10.2 months (vs placebo 8.0 months).
Thyroid cancer : Median PFS 11.0 months (vs placebo 1.9 months).
Neuroendocrine tumor : Median PFSpNET13.8 months, epNET8.5 months.