Fruquintinib

12.1. Mechanism of Action Fruquintinib is a small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 with IC 50 values of 33, 35, and 0.5 nM, respectively.

• 1. INDICATIONS AND USAGE FRUZAQLA is indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine‑, oxaliplatin‑, and irinotecan‑based chemotherapy, an anti‑VEGF therapy, and, if RAS wild‑type and medically appropriate, an anti-EGFR therapy.ICD-10: C18.9

• 4. CONTRAINDICATIONS None.contraindicated

2. DOSAGE AND ADMINISTRATION The recommended dose of FRUZAQLA is 5 mg orally once daily, with or without food for the first 21 days of each 28-day cycle. ( 2.1 ) 2.1. Recommended Dosage The recommended dose of FRUZAQLA is 5 mg orally once daily for the first 21 days of each 28-day cycle until disease progression or unacceptable toxicity. Take FRUZAQLA with or without food [see Clinical Pharmacology (12.3) ] at approximately the same time each day. Swallow the FRUZAQLA capsule whole. Take a missed dose if less than 12 hours have passed since the missed scheduled dose. Do not take two doses on the same day to make up for a missed dose. Do not take an additional dose if vomiting occurs after taking FRUZAQLA but continue with the next scheduled dose. 2.2. Dosage Modifications for Adverse Reactions The recommended dose reductions for adverse reactions are provided in Table 1. Table 1: Recommended Dose Reductions for FRUZAQLA Dose Level FRUZAQLA Dosage First dose reduction 4 mg orally once daily Second dose reduction 3 mg orally once daily Permanently discontinue FRUZAQLA in patients unable to tolerate 3 mg orally once daily. The recommended dosage modifications for adverse reactions are provided in Table 2. Table 2: Recommended Dosage Modifications for FRUZAQLA Adverse Reaction Severity Severity as defined by National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 5.0.

5. WARNINGS AND PRECAUTIONS Hypertension: Control blood pressure prior to treatment and monitor during treatment. Manage with anti-hypertensive medications and adjustment of the dose of FRUZAQLA, if necessary. Withhold, dose reduce, or permanently discontinue based on severity of hypertension. ( 2.2 , 5.1 ) Hemorrhagic Events: Closely monitor patients who are at risk for bleeding. Withhold, reduce dose, or permanently discontinue FRUZAQLA based on severity and persistence of hemorrhage. ( 2.2 , 5.2 ) Infections: Monitor for infection during treatment and withhold FRUZAQLA during active infections. Do not start FRUZAQLA in patients with active infections. ( 5.3 ) Gastrointestinal (GI) Perforation: Periodically monitor for GI perforation. Permanently discontinue FRUZAQLA in patients who develop GI perforation or fistula. ( 5.4 ) Hepatotoxicity: Monitor liver laboratory tests prior to the start of FRUZAQLA and periodically during treatment. Withhold, reduce the dose, or permanently discontinue based on severity. ( 2.2 , 5.5 ) Proteinuria: Monitor urine protein. Discontinue FRUZAQLA for nephrotic syndrome ( 2.2 , 5.6 ) Palmar-Plantar Erythrodysesthesia: Withhold FRUZAQLA based on severity. ( 2.2 , 5.7 ) Posterior Reversible Encephalopathy Syndrome (PRES): Immediately discontinue FRUZAQLA if PRES is suspected and confirmed via Magnetic Resonance Imaging (MRI). ( 5.8 ) Impaired Wound Healing: Withhold FRUZAQLA for 2 weeks before major surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing.

6. ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Hypertension [see Warnings and Precautions (5.1) ] . Hemorrhagic Events [see Warnings and Precautions (5.2) ] . Infections [see Warnings and Precautions (5.3) ] . Gastrointestinal Perforation [see Warnings and Precautions (5.4) ] . Hepatotoxicity [see Warnings and Precautions (5.5) ]. Proteinuria [see Warnings and Precautions (5.6) ] . Palmar-Plantar Erythrodysesthesia (PPE) [see Warnings and Precautions (5.7) ] . Posterior Reversible Encephalopathy Syndrome (PRES) [see Warnings and Precautions (5.8) ] . Most common adverse reactions (incidence ≥20%) are hypertension, palmar-plantar erythrodysesthesia, proteinuria, dysphonia, abdominal pain, diarrhea, and asthenia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals America, Inc. at 1-844-662-8532 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1. Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

8. USE IN SPECIFIC POPULATIONS Lactation: Advise not to breastfeed. ( 8.2 ) 8.1. Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action, FRUZAQLA can cause fetal harm when administered to a pregnant woman. In an embryo-fetal developmental study in pregnant rats, oral administration of fruquintinib during the period of organogenesis resulted in teratogenicity and embryo lethality at exposures below the clinical exposure (see Data ) . There are no data on the use of FRUZAQLA in pregnant women. Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In an embryo-fetal developmental study in pregnant rats, daily oral administration of fruquintinib at doses ≥0.1 mg/kg [approximately 0.2 times the recommended clinical dose of 5 mg based on body surface area (BSA)] during the period of organogenesis resulted in fetal external (edema and head and tail abnormalities), visceral, and skeletal malformations. At doses of 0.25 mg/kg (approximately 0.5 times the recommended clinical dose of 5 mg based on BSA), an increase in post-implantation loss and reduction in live fetuses was observed. 8.2.

Metabolism

12.3. Pharmacokinetics The fruquintinib steady-state geometric mean (% coefficient of variation [CV]) maximum concentration (C max ) is 300 ng/mL (28%) and area under the concentration-time curve for the dosing interval (AUC 0-24h ) is 5880 ng∙h/mL (29%) at the recommended dosage.

• Nov 8, 2023NDANDA217564Takeda Pharms Usa

1. 1Death82223%
2. 2Fatigue45713%
3. 3Colorectal Cancer Metastatic36710%
4. 4Colon Cancer3489.9%
5. 5Diarrhoea2667.6%
6. 6Blood Pressure Increased2627.5%
7. 7Asthenia2286.5%
8. 8Decreased Appetite2266.4%
9. 9Dysphonia2045.8%
10. 10Myelosuppression1775.1%
11. 11Hypertension1734.9%
12. 12Nausea1704.9%
13. 13Off Label Use1584.5%
14. 14Pain1494.3%
15. 15Product Dose Omission Issue1233.5%

The 10 most recently updated of 202 ClinicalTrials.gov registrations naming Fruquintinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Fruquintinib Plus FOLFIRI as Second-Line Treatment for Participants With Metastatic Colorectal Cancer (FRUITFUL)
  Recruiting · Phase 2 · Interventional · 60 enrolled · SCRI Development Innovations, LLC
  NCT07011576updated 2026-06-12
• Targeted Treatment Plus Tislelizumab and HAIC for Advanced CRCLM Failed From Standard Systemic Treatment
  Active not recruiting · Interventional · 47 enrolled · Peking University
  NCT06199232updated 2026-06-09
• A Study to Test DSP107 in Combination With Atezolizumab in Comparison With Fruquintinib as a New Treatment for Colorectal Cancer.
  Recruiting · Phase 2 · Interventional · 90 enrolled · Kahr Bio Australia Pty Ltd
  NCT07235293updated 2026-06-08
• A Single-arm, Open-label, Single-center Prospective Study of Fruquintinib Combined With Envafolimab in the Treatment of Advanced or Unresectable Locally Advanced Bone and Soft Tissue Sarcoma
  Suspended · Phase 2 · Interventional · 20 enrolled · Shanghai 6th People's Hospital
  NCT05941325updated 2026-06-05
• A Single-arm, Multicenter Clinical Study of Fruquintinib Combined With Serplulimab and Chemotherapy as First-line Treatment for Patients With RAS/BRAF-mutated Advanced Colorectal Cance
  Not yet recruiting · Phase 2 · Interventional · 80 enrolled · Jiangsu Cancer Institute & Hospital
  NCT07622550updated 2026-06-03
• Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies
  Completed · Phase 3 · Interventional · 404 enrolled · BeOne Medicines
  NCT04164199updated 2026-06-03
• A Study of Fruquintinib in Adults With Metastatic Colorectal Cancer in Poland
  Not yet recruiting · Observational · 110 enrolled · Takeda
  NCT07623174updated 2026-06-03
• A Phase Ib/II Study of HDM2017 in Combination With Standard of Care in Advanced Colorectal Cancer
  Not yet recruiting · Phase 1 · Phase 2 · Interventional · 120 enrolled · Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
  NCT07621159updated 2026-06-02
• A Phase 2 Trial of Fruquintinib and Tislelizumab in ctDNA-defined Minimal Residual Disease in Colorectal Cancer After Completion of Adjuvant Chemotherapy
  Recruiting · Phase 2 · Interventional · 20 enrolled · M.D. Anderson Cancer Center
  NCT07136077updated 2026-06-01
• Prospective National Cohort Evaluating Prognostic Factors for Efficacy of Fruquintinib Treatment in Patients With Metastatic Colorectal Cancer
  Recruiting · Interventional · 300 enrolled · Federation Francophone de Cancerologie Digestive
  NCT07124858updated 2026-05-26

Frequently asked questions

How does Fruquintinib work?

12.1. Mechanism of Action Fruquintinib is a small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 with IC 50 values of 33, 35, and 0.5 nM, respectively.

What is Fruquintinib used for?

According to FDA labeling, Fruquintinib carries indications including: 1. INDICATIONS AND USAGE FRUZAQLA is indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine‑, oxaliplatin‑, and irinotecan‑based chemotherapy, an anti‑VEGF therapy, and, if RAS wild‑type and medically appropriate, an anti-EGFR therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fruquintinib?

Fruquintinib is classified as Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors, Vascular Endothelial Growth Factor Receptor Inhibitors, VEGFR1 Inhibitors, VEGFR2 Inhibitors, VEGFR3 Inhibitors, Decreased Endothelial Proliferation.

What are the brand names for Fruquintinib?

Fruquintinib is marketed under brand names including Fruzaqla.

What are the contraindications for Fruquintinib?

Fruquintinib labeling lists contraindications including: 4. CONTRAINDICATIONS None.. Always consult the full prescribing information and a clinician.