Elunate Fruquintinib Capsules

1. Indications and Usage
Metastatic Colorectal Cancer (mCRC):
Indicated for the treatment of adult patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy; prior anti-VEGF therapy; and prior anti-EGFR therapy (for patients with RAS wild-type tumors).
2. Dosage and Administration
Recommended Dosage:
Dose: 5 mg orally once daily.
Schedule: For 3 consecutive weeks, followed by a 1-week rest period (a 28-day cycle).
Administration: Swallow capsules whole with water. Can be taken with or without food.
Dose Modifications:
With CYP3A Inhibitors: Reduce dose when co-administered with strong CYP3A inhibitors (e.g., reduce to 4 mg or 3 mg).
Toxicity: Interrupt treatment for Grade ≥ 3 toxicities (e.g., hypertension, proteinuria, hand-foot syndrome); resume at reduced dose upon recovery.
3. Mechanism of Action
VEGFR Inhibition:
Fruquintinib is a potent and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3.
Physiological Effect:
It inhibits the phosphorylation of VEGFR and downstream signaling pathways (such as PI3K/AKT and MAPK), thereby inhibiting angiogenesis and tumor growth.
4. Safety and Warnings
Hemorrhage:
Severe hemorrhage, including fatalities, has occurred. Monitor for signs of bleeding. Avoid concomitant use with anticoagulants.
Hypertension:
Hypertension can occur. Monitor blood pressure periodically.
Proteinuria:
Proteinuria has been reported. Monitor urine protein periodically.
Embryo-Fetal Toxicity:
May cause fetal harm. Advise females of reproductive potential to use effective contraception during treatment and for at least 1 month after the final dose.
5. Adverse Reactions
Most Common:
Hypertension, proteinuria, hand-foot skin reaction, dysphonia, fatigue, diarrhea, and increased transaminases.
Serious Adverse Events:
Severe hemorrhage, gastrointestinal perforation, and wound dehiscence.
6. Drug Interactions
Strong CYP3A Inhibitors:
Increase fruquintinib exposure. Reduce fruquintinib dose by one level (e.g., 5 mg → 4 mg).
Strong CYP3A Inducers:
Decrease fruquintinib exposure. Avoid concomitant use with strong CYP3A inducers (e.g., rifampin).
BCRP Substrates:
Fruquintinib is a BCRP inhibitor. Monitor patients for potential toxicity when used with BCRP substrates (e.g., rosuvastatin).
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Fruquintinib.
Storage:
Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F).