Fruquintinib is a targeted therapy used for metastatic colorectal cancer, and its administration requires strict attention to contraindications. Although there is no official list of “three strictest prohibitions”, three types of situations demand special caution based on the drug’s properties: interactions with certain medications, consumption of grapefruit-related foods, and contraindications in specific health conditions. Patients must strictly follow medical advice and undergo regular monitoring during treatment.
I. Avoid Concomitant Use with Certain Drugs
CYP3A4 inhibitors or inducers
Strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole) or inducers (e.g., rifampicin, phenytoin) may significantly alter the plasma concentration of fruquintinib, resulting in reduced efficacy or increased side effects.
Anticoagulant / antiplatelet agents
Drugs such as warfarin and aspirin may raise the risk of bleeding and require cautious co-administration.
Before treatment, inform your doctor of all medications you are taking (including traditional Chinese medicines and dietary supplements) for appropriate regimen adjustment.
II. Avoid Grapefruit and Related Products
Grapefruit, pomelo and their juices contain strong inhibitors of the CYP3A4 enzyme that metabolizes fruquintinib. They can cause drug accumulation in the body and worsen adverse reactions including diarrhea, hypertension and proteinuria.
It is recommended to avoid these foods during treatment and for 1–2 weeks after stopping fruquintinib.
III. Contraindications in Specific Health Conditions
Severe hepatic or renal impairment: May impair drug metabolism; dose adjustment or contraindication may be required after medical evaluation.
Active bleeding or coagulation disorders: Fruquintinib inhibits angiogenesis and may increase bleeding risk.
Uncontrolled hypertension or cardiovascular disease: Blood pressure must be closely monitored during treatment; temporary treatment interruption may be necessary.
General Precautions
Strictly follow medical orders: Dosage and treatment duration are individualized; do not adjust the dose or stop treatment without medical approval.
Regular monitoring
Routine tests include complete blood count, liver and kidney function, blood pressure and urine protein, to detect abnormalities at an early stage.
Seek immediate medical help
Emergency care is required for severe diarrhea, dyspnea, chest pain or bleeding.
Fruquintinib is a prescription medication. Its indications and contraindications must be evaluated by a specialist before use, and the treatment plan should be dynamically adjusted according to clinical responses during therapy.



