Elunate Fruquintinib Capsules

1. Indications and Usage
Fruquintinib capsules are indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, and anti-VEGF therapy, and anti-EGFR therapy (if RAS wild-type).
2. Dosage and Administration
Recommended Dosage: The recommended dosage is 5 mg administered orally once daily.
Schedule: Patients should take the capsules for 3 weeks, followed by 1 week off (a 4-week cycle).
Administration: Capsules should be swallowed whole and can be taken with or without food.
Missed Dose: If a dose is missed, do not make up for it. Take the next dose at the regular scheduled time on the following day.
Dose Modifications: For intolerable adverse reactions, the dose may be interrupted and reduced to 4 mg once daily, then to 3 mg once daily.
3. Mechanism of Action
Fruquintinib is a potent, selective inhibitor of VEGFR-1, VEGFR-2, and VEGFR-3. By inhibiting these receptors, it blocks angiogenesis, thereby starving the tumor of blood supply and nutrients.
4. Safety and Warnings
Hemorrhage: Increased risk of bleeding, including gastrointestinal bleeding. Discontinue for severe or fatal hemorrhage.
Gastrointestinal Perforation: Monitor for signs of perforation. Discontinue if perforation occurs.
Hypertension: Monitor blood pressure regularly. Manage and discontinue for severe hypertension.
Hepatotoxicity: Monitor liver function tests. Discontinue for severe liver injury.
Hand-Foot Skin Reaction: Monitor for pain and swelling. Reduce dose or discontinue based on severity.
Proteinuria: Monitor urine protein. Discontinue for nephrotic syndrome.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The most common adverse reactions include hypertension, proteinuria, hand-foot skin reaction, fatigue, diarrhea, abdominal pain, dysphonia, bleeding, elevated liver enzymes, and decreased appetite.
Clinical Research: Efficacy was established in the FRESCO trial, demonstrating improved overall survival and progression-free survival compared to placebo in heavily pretreated mCRC patients.
6. Drug Interactions
Fruquintinib is minimally metabolized by CYP3A4, and CYP3A4 inhibitors or inducers have a limited effect on its exposure. However, as it inhibits P-glycoprotein (P-gp) and BCRP, caution is advised when co-administering substrates of these transporters.
7. Pharmaceutical Information
Composition: The active ingredient is fruquintinib.
Appearance: The capsules contain white to off-white powder.
Storage: Store in a tightly closed container below 30°C.