What Is Fruquintinib (Fruzaqla)? FDA Approval, Licensing and Reimbursement in Turkey

• Active Ingredient: Fruquintinib
• Brand Name: Fruzaqla
• Route of Administration: Oral
• Class: Tyrosine kinase inhibitors
• Category: VEGFR inhibitors (vascular endothelial growth factor receptor inhibitors)
• Manufacturer: Takeda Pharma
• Distribution in Turkey: Takeda Pharma
• Approved Cancers: Metastatic colorectal cancer (mCRC)

What Is Fruzaqla and How Does It Work?

Fruzaqla, used in metastatic (stage 4) colorectal cancer (mCRC), is an oral tyrosine kinase inhibitor.

It targets vascular endothelial growth factor (VEGF) receptors, which play an important role in cancer cell growth and spread. VEGF enables tumors to form new blood vessels through a process called angiogenesis . By blocking VEGF's role in this process, fruquintinib limits tumor growth and reduces metastatic potential.

It is highly selective for VEGFR-1, VEGFR-2 and VEGFR-3 receptors, providing a more targeted treatment.

Fruquintinib's mechanism of action is illustrated below.

FDA Approval History

• November 8, 2023: Approved by the FDA for metastatic colorectal cancer previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, anti-VEGF therapy and, in appropriate patients, anti-EGFR therapy.

Fruquintinib is the first selective VEGFR inhibitor to receive FDA approval for metastatic colorectal cancer.

The main findings that led to FDA approval of fruquintinib in the FRESCO-2 trial are as follows:

Licensing in Turkey

Official licensing information for Fruzaqla, containing fruquintinib, has not yet been announced in Turkey. Because it is FDA-approved, it may enter the Turkish licensing process in the near future.

Is It Reimbursed in Turkey?

It has not yet been included in reimbursement coverage by Turkey's Social Security Institution (SGK).

Mechanisms of Resistance

Resistance may arise when cancer cells activate VEGF-independent pathways. Tumors finding alternative routes to support themselves despite VEGF inhibition may develop treatment resistance.

Pharmacokinetic Properties

• Absorption: Fruquintinib is well absorbed after oral administration.
• Distribution: It is highly bound to plasma proteins and distributes well into body tissues.
• Metabolism: Metabolized in the liver through the CYP3A4 enzyme system.

Dose Range

Fruzaqla is taken at 5 mg once daily for the first 21 days of each 28-day cycle.

Drug Interactions

Use with CYP3A4 inhibitors and inducers requires caution. Concomitant anticoagulants (blood thinners) may increase bleeding risk.

Precautions

• High Blood Pressure: Blood pressure should be checked regularly during treatment.
• Bleeding Risk: Serious bleeding may occur, particularly with anticoagulant use.
• Infection Risk: Fruquintinib may weaken the immune system and increase infection risk.
• Liver and Kidney Problems: The drug may increase liver enzymes and affect kidney function.

Side Effects

The most commonly reported effects are:

• Hypertension (high blood pressure)
• Palmar-plantar erythrodysesthesia (hand-foot syndrome)
• Proteinuria (protein in the urine)
• Dysphonia (hoarseness)
• Diarrhea
• Abdominal pain
• Asthenia (weakness)