Fruquintinib (brand name Fruzaqla®) is an oral kinase inhibitor medication used to treat adults with advanced metastatic colorectal cancer (mCRC).
It works by blocking the action of abnormal proteins-vascular endothelial growth factor receptors, or VEGFR-1, -2, and -3 that signal cancer cells to multiply and inhibit the growth of new blood vessels that feed tumors.
It belongs to a class of drugs known as kinase inhibitors, specifically designed to block angiogenesis.
By blocking these proteins, the drug helps cut off the blood supply that tumors need to grow and spread.
It restricts tumor growth and progression by inhibiting all 3VEGFR‘s and has the potential to inhibit lymphangiogenesis.
Fruquintinib is approved for patients with mCRC who have been previously treated with standard chemotherapies and other targeted therapies.
This includes prior treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if appropriate, an anti-EGFR therapy.
It is available as capsules and is typically taken once daily for 21 consecutive days, followed by a 7-day rest period (a 28-day cycle). It can be taken with or without food.
Form: Oral capsule (available in 1 mg and 5 mg strengths).
Cycle: The standard recommended dose is 5 mg once daily for 21 consecutive days, followed by a 7-day rest period (a 28-day cycle).
Clinical trials (FRESCO and FRESCO-2) showed that fruquintinib significantly improved overall survival and progression-free survival in heavily pretreated mCRC patients compared to a placebo.
Fruquintinib plus trifluridine-tipracil demonstrated acceptable tolerability in clinical activity with a partial response rate of 10.9% and a median free progression survival of 6.4 months.
Side Effects: Common side effects include hypertension, hand-foot skin reactions (palmar-plantar erythrodysesthesia), protein in the urine (proteinuria), voice changes (dysphonia), abdominal pain, diarrhea, and fatigue.
Common side effects (occurring in >20% of patients) include:
Hypertension
Infections
Palmar-plantar erythrodysesthesia (hand-foot syndrome)
Proteinuria
Dysphonia (voice changes or hoarseness)
Gastrointestinal issues such as diarrhea and abdominal pain
Asthenia/Fatigue
Voice changes
Serious risks include gastrointestinal perforation, severe hemorrhage and liver toxicity.
Fruquintinib can cause serious side effects, including severe bleeding, infections, heart problems, and slow wound healing.
Women of childbearing potential and males with female partners of childbearing potential should use effective contraception during treatment and for 2 weeks after the last dose.