FRUZAQLA (Fruquintinib)

What Is FRUZAQLA and What Is It Used For?

FRUZAQLA contains the active substance fruquintinib, a targeted anticancer agent classified as a tyrosine kinase inhibitor. Specifically, fruquintinib is a highly selective inhibitor of vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), which are proteins on cells that play a central role in the formation of new blood vessels, a process known as angiogenesis.

Colorectal cancer is the third most common cancer worldwide, and when it spreads (metastasizes) to other organs such as the liver or lungs, treatment becomes significantly more complex. FRUZAQLA is approved for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have already been treated with available standard therapies, including fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF agents, and anti-EGFR agents (if eligible). It provides a treatment option for patients who have progressed through or are intolerant to these earlier lines of therapy.

How Does FRUZAQLA Work?

Solid tumors, including colorectal cancers, require a blood supply to grow beyond a few millimeters in size. Tumors achieve this by releasing signals, primarily through the vascular endothelial growth factor (VEGF) pathway, that stimulate the surrounding tissue to form new blood vessels. These new vessels deliver oxygen and nutrients that enable the tumor to grow and eventually spread to distant sites in the body.

Fruquintinib works by binding to and blocking the kinase activity of VEGFR-1, VEGFR-2, and VEGFR-3. By inhibiting all three receptors, the drug prevents the signaling cascade that would otherwise trigger the growth of new blood vessels around the tumor. Without an adequate blood supply, tumor growth is slowed and the cancer's ability to spread is reduced.

The selectivity of fruquintinib for VEGF receptors is an important distinguishing feature. Unlike some broader multi-kinase inhibitors used in cancer treatment, fruquintinib has minimal activity against other kinase targets. This selectivity means that many of the off-target side effects associated with less selective agents may be reduced, although fruquintinib still has its own characteristic side-effect profile that requires careful monitoring.

Clinical Evidence

The approval of FRUZAQLA was based primarily on the FRESCO-2 trial, a large randomized, double-blind, placebo-controlled Phase III clinical study conducted across sites in the United States, Europe, Japan, and Australia. The trial enrolled 691 patients with previously treated metastatic colorectal cancer. Results showed that patients receiving fruquintinib plus best supportive care had a statistically significant improvement in overall survival compared to placebo plus best supportive care, with a median overall survival of 7.4 months versus 4.8 months, representing a 34% reduction in the risk of death (hazard ratio 0.66, p < 0.001).

What Should You Know Before Taking FRUZAQLA?

Contraindications

FRUZAQLA must not be used if you have a known hypersensitivity (allergy) to fruquintinib or any of the other ingredients in the capsules. The 1 mg capsules contain tartrazine (E102) and sunset yellow FCF (E110), while the 5 mg capsules contain allura red AC (E129), all of which are colorants that may cause allergic reactions in susceptible individuals. If you have experienced allergic reactions to any food colorings in the past, inform your healthcare provider before starting this medication.

Warnings and Precautions

Before starting FRUZAQLA and throughout the course of treatment, your healthcare provider should be aware of several important conditions and risk factors. The following warnings apply:

Hypertension (high blood pressure): FRUZAQLA commonly causes elevated blood pressure. Your doctor should ensure that your blood pressure is adequately controlled before initiating treatment and will monitor it regularly throughout therapy. If blood pressure becomes significantly elevated, your doctor may prescribe additional antihypertensive medication, reduce the dose of FRUZAQLA, or temporarily or permanently discontinue treatment.

Bleeding: There is an increased risk of bleeding events with FRUZAQLA, including serious gastrointestinal bleeding. Inform your doctor if you have a history of bleeding disorders or if you are taking blood-thinning medications such as warfarin or acenocoumarol. Seek immediate medical attention if you notice blood in your stool, black stools, blood in your urine, or experience significant abdominal pain.

Gastrointestinal perforation: In rare cases, treatment with FRUZAQLA can lead to a hole forming in the wall of the stomach or intestine (perforation), which is a serious and potentially life-threatening complication. Seek emergency medical care immediately if you develop severe abdominal pain, vomiting blood, or pass red or black stools.

Proteinuria (protein in the urine): FRUZAQLA can cause protein to leak into the urine, which may indicate kidney stress. Your doctor will regularly check your urine for protein during treatment and may adjust your dosage accordingly.

Posterior reversible encephalopathy syndrome (PRES): In uncommon cases, FRUZAQLA may cause a condition involving swelling of the brain that leads to severe headache, confusion, seizures, or vision changes. Seek emergency medical attention immediately if you experience any of these symptoms.

Wound healing: FRUZAQLA may impair wound healing. If you are planning surgery, your doctor will likely advise you to stop taking FRUZAQLA before the procedure and not restart it until the wound has adequately healed. Tell your doctor if you have any unhealed wounds.

Thromboembolic events: Patients who have recently experienced blood clots in veins or arteries, such as stroke, heart attack, or pulmonary embolism, should discuss the risks and benefits of treatment with their doctor before starting FRUZAQLA.

Hand-foot syndrome: This common side effect involves redness, pain, swelling, or blistering of the palms and soles. While usually manageable, it can affect daily activities. Your doctor can recommend supportive measures or dose adjustments if it becomes severe.

Children and Adolescents

FRUZAQLA has not been studied in children or adolescents and is not intended for use in patients under 18 years of age for the treatment of colorectal cancer.

Pregnancy and Breastfeeding

FRUZAQLA has not been studied in pregnant women. Based on its mechanism of action (blocking blood vessel formation), fruquintinib is expected to cause harm to a developing fetus if used during pregnancy. FRUZAQLA should not be used during pregnancy unless clearly necessary and no alternative treatment is available. A pregnancy test should be performed before starting treatment.

Contraception: Women of childbearing potential must use a highly effective method of contraception during treatment with FRUZAQLA and for at least 2 weeks after the last dose. Discuss appropriate contraceptive options with your healthcare provider.

Breastfeeding: It is not known whether fruquintinib passes into breast milk, and a risk to the nursing infant cannot be excluded. Breastfeeding should be discontinued during treatment and for at least 2 weeks after the last dose of FRUZAQLA. Consult your doctor about the best way to feed your child during this period.

Driving and Using Machines

FRUZAQLA may have a minor effect on the ability to drive and use machines. Fatigue is a common side effect. Do not drive or operate machinery if you experience symptoms that affect your concentration or reaction time.

How Does FRUZAQLA Interact with Other Drugs?

Drug interactions can affect how well FRUZAQLA works or increase the risk of side effects. Always inform your healthcare provider about all medications you are taking, have recently taken, or plan to take, including prescription drugs, over-the-counter medicines, and herbal supplements.

Major Interactions

Fruquintinib is metabolized in the liver, and certain medications that affect liver enzymes can alter its blood levels. The most clinically significant interaction involves strong CYP3A4 inducers:

Other Considerations

While the primary identified interaction is with strong CYP3A4 inducers, as with any cancer medication, it is essential to maintain an open dialogue with your oncologist about all substances you consume. Herbal supplements such as St. John's wort (Hypericum perforatum) are also known to be potent CYP3A4 inducers and should be avoided during FRUZAQLA treatment. Additionally, grapefruit and grapefruit juice can inhibit CYP3A4 and may affect drug levels, though the clinical significance with fruquintinib has not been fully established.

Nonsteroidal anti-inflammatory drugs (NSAIDs) and aspirin may increase the risk of gastrointestinal bleeding when taken concurrently with FRUZAQLA. Discuss the use of these pain relievers with your healthcare provider and consider safer alternatives for pain management during treatment.

What Is the Correct Dosage of FRUZAQLA?

Always take FRUZAQLA exactly as your doctor has prescribed. Do not change the dose or stop taking the medicine without consulting your healthcare provider. The dose may be adjusted based on your response to treatment and any side effects you experience.

Adults

Children

FRUZAQLA is not approved for use in children or adolescents (under 18 years of age). There are no pediatric dosing recommendations, as the safety and efficacy in this population have not been established.

Elderly

No dose adjustment is required for elderly patients based on age alone. However, older adults may be more susceptible to certain side effects, particularly hypertension and fatigue. Your doctor will monitor you closely and adjust treatment as needed based on your individual tolerance.

Missed Dose

Overdose

If you have taken more FRUZAQLA than prescribed, contact your doctor immediately. There is no specific antidote for fruquintinib overdose. Treatment is supportive, and your doctor may advise you to stop taking the medication temporarily or permanently. You may need to be monitored in a healthcare setting for potential complications, particularly hypertension and bleeding.

Duration of Treatment

Your doctor will assess your condition regularly to determine whether FRUZAQLA continues to be beneficial. Treatment is typically continued for as long as the medication is providing clinical benefit and the side effects remain manageable. Do not stop taking FRUZAQLA unless your doctor advises you to do so, as premature discontinuation may reduce the effectiveness of your cancer treatment.

What Are the Side Effects of FRUZAQLA?

Like all medicines, FRUZAQLA can cause side effects, although not everybody gets them. Some side effects can be serious and require immediate medical attention, while others are more common and can often be managed with supportive care and dose adjustments. Your healthcare team will monitor you closely throughout treatment and can help manage any side effects that occur.

Managing Common Side Effects

Many of the common side effects of FRUZAQLA can be managed effectively with appropriate supportive care. Hypertension is typically controlled with antihypertensive medications prescribed by your doctor. Hand-foot syndrome may be alleviated with moisturizing creams, avoiding prolonged heat exposure to hands and feet, and wearing comfortable footwear. For diarrhea, your doctor may recommend antidiarrheal medications and adequate fluid intake. Mouth sores can be managed with gentle oral hygiene and medicated mouthwashes.

Your healthcare team may adjust your FRUZAQLA dose (either reducing it or temporarily interrupting treatment) to help manage side effects while maintaining treatment efficacy. It is important to report all side effects to your doctor, even those that seem minor, so that they can provide the best possible supportive care.

Reporting Side Effects

Reporting suspected side effects after a medicine has been authorized is important, as it allows continuous monitoring of the medicine's benefit-risk balance. Healthcare professionals and patients can report suspected adverse reactions to their national regulatory authority, such as the EMA in Europe or the FDA in the United States.

How Should You Store FRUZAQLA?

Proper storage of FRUZAQLA is essential to maintain the effectiveness and safety of the medication. Follow these storage guidelines:

• Temperature: No special temperature storage requirements. Store at room temperature.
• Container: Keep FRUZAQLA in its original packaging to protect from moisture. Keep the bottle tightly closed at all times.
• Desiccant: Each bottle contains a desiccant packet (small moisture-absorbing sachet). Leave this packet inside the bottle. Do not swallow the desiccant packet.
• Expiry date: Do not use FRUZAQLA after the expiry date printed on the carton and bottle (EXP). The expiry date refers to the last day of that month.
• Children: Keep this medicine out of the sight and reach of children.
• Disposal: Do not dispose of medications in wastewater or household waste. Return unused medicine to your pharmacy for proper disposal to protect the environment.

Each bottle of FRUZAQLA contains 21 hard capsules, which is exactly the number needed for the 21-day active treatment phase of one cycle. The 1 mg capsules are approximately 16 mm in length, white with a yellow cap, and marked with "HM013" and "1mg." The 5 mg capsules are approximately 19 mm in length, white with a red cap, and marked with "HM013" and "5mg."

What Does FRUZAQLA Contain?

FRUZAQLA 1 mg Hard Capsules

Each capsule contains 1 mg of fruquintinib as the active substance. The other ingredients include:

• Capsule contents: Corn starch, microcrystalline cellulose (E460), talc (E553b)
• Capsule shell: Gelatin, titanium dioxide (E171), tartrazine (E102), sunset yellow FCF (E110)
• Printing ink: Shellac (E904), propylene glycol (E1520), potassium hydroxide, black iron oxide (E172)

FRUZAQLA 5 mg Hard Capsules

Each capsule contains 5 mg of fruquintinib as the active substance. The other ingredients include:

• Capsule contents: Corn starch, microcrystalline cellulose (E460), talc (E553b)
• Capsule shell: Gelatin, titanium dioxide (E171), allura red AC (E129), brilliant blue FCF (E133)
• Printing ink: Shellac (E904), propylene glycol (E1520), potassium hydroxide, black iron oxide (E172)

Marketing Authorization Holder

FRUZAQLA is marketed by Takeda Pharmaceuticals International AG. The medicine is manufactured by Takeda Ireland Limited. For further information about this medicine, consult the European Medicines Agency (EMA) website or contact your local Takeda representative.

References

This article is based on the following peer-reviewed sources and regulatory documents:

1. European Medicines Agency (EMA). FRUZAQLA (fruquintinib) — Summary of Product Characteristics. European Public Assessment Report (EPAR). 2024.
2. U.S. Food and Drug Administration (FDA). FRUZAQLA Prescribing Information. Approved November 2023.
3. Dasari A, Lonardi S, Garcia-Carbonero R, et al. Fruquintinib versus placebo in patients with refractory metastatic colorectal cancer (FRESCO-2): an international, multicentre, randomised, double-blind, phase 3 study. The Lancet. 2023;402(10395):41-53.
4. National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Colon Cancer. Version 1.2024.
5. European Society for Medical Oncology (ESMO). Metastatic Colorectal Cancer: ESMO Clinical Practice Guidelines. Annals of Oncology. 2023.
6. World Health Organization (WHO). WHO Model List of Essential Medicines. 23rd List, 2023.
7. British National Formulary (BNF). Fruquintinib. National Institute for Health and Care Excellence (NICE). 2024.

Medical Editorial Team

Evidence Standard: All medical information follows the GRADE evidence framework and is reviewed according to WHO, EMA, FDA, and ESMO guidelines. Evidence Level 1A where applicable. No commercial funding or pharmaceutical sponsorship.

Last reviewed: February 3, 2026 | Published: August 25, 2025