Adult: In patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-vascular endothelial growth factor (VEGF) therapy, and anti-epidermal growth factor receptor (EGFR) therapy (if RAS wild-type and medically appropriate): 5 mg once daily on the 1st 21 days of each 28-day cycle. Continue treatment until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guidelines).
What are the brands available for Fruquintinib in Hong Kong?
Severe (total bilirubin >3 times ULN and any AST): Not recommended.
Administration
Fruquintinib May be taken with or without food.
Special Precautions
Patient with recent history of thromboembolic events or with risk factors for arterial thrombosis (e.g. hypertension). Withhold treatment for at least 2 weeks before major surgery; do not administer for at least 2 weeks after major surgery and until adequate wound healing has occurred. Not recommended for severe hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Hypertension, proteinuria, palmar-plantar erythrodysaesthesia, impaired wound healing, increased risk of arterial thromboembolic events. Very rarely, posterior reversible encephalopathy syndrome. Endocrine disorders: Hypothyroidism. Gastrointestinal disorders: Stomatitis, abdominal pain, diarrhoea. General disorders and administration site conditions: Fatigue. Investigations: Increased serum creatinine, glucose, uric acid, triglycerides, cholesterol, AST, ALT, alkaline phosphatase or bilirubin; decreased serum Na, Ca, K, Mg, albumin or platelet count; prolonged aPTT. Metabolism and nutrition disorders: Anorexia. Musculoskeletal and connective tissue disorders: Musculoskeletal pain, back pain, arthralgia. Respiratory, thoracic and mediastinal disorders: Dysphonia, throat pain. Skin and subcutaneous tissue disorders: Rash. Potentially Fatal: Severe haemorrhage; gastrointestinal perforation; increased risk of infections (e.g. pneumonia, sepsis or septic shock, lower respiratory tract infection, bacterial infection). Rarely, hepatotoxicity (e.g. hepatic injury).
Patient Counseling Information
Women of childbearing potential and men with female partners of childbearing potential must use effective birth control methods during treatment and up to 1 month after treatment. Discontinue breastfeeding during treatment and for 2 weeks after the last dose.
Monitoring Parameters
Verify pregnancy status of women of childbearing potential before starting treatment. Monitor blood pressure (weekly during the 1st month, at least monthly thereafter and as clinically indicated); LFTs, presence of proteinuria (at baseline and periodically during treatment); INR in patients receiving anticoagulant therapy. Assess for signs and symptoms of dermatologic toxicity, gastrointestinal perforation, bleeding, thromboembolic events, impaired wound healing, infection and posterior reversible encephalopathy syndrome.
Drug Interactions
May reduce serum concentration and efficacy with moderate or strong CYP3A4 inducers (e.g. rifampicin).
Action
Description: Mechanism of Action: Fruquintinib, an antineoplastic agent, is a potent, highly selective, small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2 and -3. It inhibits VEGF-mediated endothelial cell proliferation, tubular formation, VEGFR-2 phosphorylation and tumour growth in in vitro and in vivo analyses. Pharmacokinetics: Absorption: Time to peak plasma concentration: Approx 2 hours. Distribution: Volume of distribution: Approx 46 L. Plasma protein binding: Approx 95%. Metabolism: Metabolised in the liver mainly by CYP450 (CYP3A4 and to a lesser extent by CYP2C8, CYP2C9 and CYP2C19 isoenzymes) and via sulfation and glucuronidation. Excretion: Via urine (approx 60%; 0.5% as unchanged drug); faeces (30%; 5% as unchanged drug). Elimination half-life: Approx 42 hours.
Chemical Structure
Fruquintinib Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 44480399, Fruquintinib. https://pubchem.ncbi.nlm.nih.gov/compound/Fruquintinib. Accessed Oct. 25, 2024.
Anon. Fruquintinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 30/09/2024.Elunate Capsules (Hutchmed Limited). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 30/09/2024.Fruquintinib. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 30/09/2024.Fruquintinib. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 30/09/2024.Fruzaqla Capsule (Takeda Pharmaceuticals America, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/09/2024.
Sign Out
Continue with Google