Cabozantinib is a multi-target tyrosine kinase inhibitor (TKI) that selectively inhibits the activity of receptor tyrosine kinases such as MET, VEGFR-1/2/3, AXL, RET, ROS1, etc., blocking tumor angiogenesis, inhibiting tumor cell proliferation and metastasis.

1、 Basic information of drugs

1. Drug name: Cabozantinib (CABOMETYX)

2. Main ingredients: Cabozantinib (S) - Malinate

2、 Indications, usage and dosage

1. Indications: Used for the treatment of advanced renal cell carcinoma (RCC) patients who have previously received anti angiogenic therapy

2. Usage and dosage:

(1) Recommended dosage: 60mg orally, once daily

(2) Medication requirements: Take on an empty stomach (at least 2 hours before taking medication and at least 1 hour after taking medication without eating)

(3) Swallowing method: Swallow the whole piece, do not crush it

3、 Dose Adjustment Guidelines

1. Before and after surgery: Discontinue use at least 28 days before planned surgery (including dental surgery)

2. Adverse reaction management:

Suspend administration when grade ≥ 4 or intolerable grade 3 adverse reactions occur, and reduce dosage according to the following plan after recovery:

Original 60mg → changed to 40mg

Original 40mg → changed to 20mg

Original 20mg → If tolerable, continue with 20mg, otherwise permanently discontinue medication

3. Special combination therapy:

Strong CYP3A4 inhibitors (such as clarithromycin): reduce daily dose by 20mg

Strong CYP3A4 inducers (such as rifampicin): daily dose increase of 20mg (maximum not exceeding 80mg)

4. Liver injury patients: The initial dose for mild or moderate liver injury patients is adjusted to 40mg once daily; Not recommended for severe liver injury

4、 Key precautions

1. Omission treatment: If it is ≥ 12 hours before the next medication, it can be taken immediately, otherwise it will be skipped

2. Dietary taboos: Avoid consuming grapefruit and grapefruit products during medication

3. Indications for permanent discontinuation of medication: uncontrolled fistula/gastrointestinal perforation, severe bleeding, arterial thrombotic events, hypertensive crisis, nephrotic syndrome, reversible posterior leukoencephalopathy syndrome

5、 Safety warnings and adverse reactions

1. Serious adverse reactions:

Bleeding (2.1% experienced ≥ grade 3 bleeding events)

Gastrointestinal perforation/fistula (incidence rates of 0.9% and 1.2%, respectively)

Thrombotic events (venous thrombosis 7.3%, arterial thrombosis 0.9%)

Hypertension (occurring in 37% of patients, with 15% being ≥ grade 3)

Diarrhea (74% occurrence, 11% grade 3)

Hand and foot skin reactions (42% occur, 8.2% are grade 3)

Embryo fetal toxicity (animal experiments show teratogenic risk)

2. Common adverse reactions (incidence ≥ 25%): diarrhea, fatigue, nausea, decreased appetite, skin reactions on hands and feet, hypertension, vomiting, weight loss, constipation

6、 Medication for special populations

1. Pregnant women: prohibited, may cause fetal damage

2. Breastfeeding period: Breastfeeding is prohibited during the medication period and within 4 months after the last administration

3. Population of childbearing age: Effective contraceptive measures should be taken during treatment and 4 months after discontinuation of medication

7、 Drug interactions

1. CYP3A4 strong inhibitors (such as ketoconazole) can increase blood drug concentration and need to be reduced

2. Strong inducers of CYP3A4 (such as rifampicin) can reduce efficacy and require incremental improvement

8、 Storage  information

Storage conditions: Store at room temperature of 20 ℃ -25 ℃, allowing short-term fluctuations of 15 ℃ -30 ℃

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