Adult: As treatment in patients after failure of prior therapy with sunitinib, a cytokine, or 1 prior systemic therapy: Initially, 5 mg 12 hourly. If tolerated for at least 2 consecutive weeks, may increase to 7 mg 12 hourly, then to 10 mg 12 hourly. Alternatively, may decrease dose to 3 mg 12 hourly, then to 2 mg 12 hourly if necessary. Continue until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption or discontinuation may be required according to individual safety or tolerability (refer to detailed product guideline).
What are the brands available for Axitinib in Malaysia?
Patients taking strong CYP3A4 or CYP3A5 inhibitors: Reduce dose of axitinib by 50%.
Patients taking strong CYP3A4 or CYP3A5 inducers: Increase dose of axitinib gradually.
Hepatic Impairment
Moderate (Child-Pugh class B): Reduce initial dose by approx 50%.
Administration
Axitinib May be taken with or without food.
Special Precautions
Patient with history of or risk factors for arterial or venous thrombotic events; risk factors for hypertension, history of aneurysm. Not recommended in patients with untreated brain metastasis or recent active gastrointestinal bleeding. Patient taking strong CYP3A4 or CYP3A5 inhibitors or CYP3A4 or CYP3A5 inducers. Patient undergoing surgery. Renal and moderate to severe hepatic impairment. Pregnancy. Discontinue breastfeeding during therapy and for 2 weeks after the last dose.
Adverse Reactions
Significant: Increased AST, ALT or blood bilirubin; hypertension or hypertensive crisis, proteinuria, posterior reversible encephalopathy syndrome (PRES), hypothyroidism or hyperthyroidism, impaired wound healing, increased haemoglobin or haematocrit; formation of aneurysm and/or artery dissections. Blood and lymphatic system disorders: Anaemia, thrombocytopenia, polycythaemia. Ear and labyrinth disorders: Tinnitus. Gastrointestinal disorders: Diarrhoea, vomiting, abdominal pain, nausea, constipation, dysgeusia, stomatitis, dyspepsia, flatulence, upper abdominal pain, haemorrhoids, glossodynia. General disorders and administration site conditions: Fatigue, asthaenia, mucosal inflammation. Hepatobiliary disorders: Hyperbilirubinaemia, cholecystitis. Investigations: Decreased weight; increased lipase, amylase, alkaline phosphatase, creatinine or TSH. Metabolism and nutrition disorders: Decreased appetite, dehydration, hyperkalaemia, hypercalcaemia. Musculoskeletal and connective tissue disorders: Arthralgia, pain in extremity, myalgia. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: Renal failure. Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea, dysphonia, oropharyngeal pain. Skin and subcutaneous tissue disorders: Palmar-plantar erythrodysaesthesia (hand-foot syndrome), rash, dry skin, pruritus, erythema, alopecia. Potentially Fatal: Cardiac events (e.g. cardiac failure, CHF, cardiopulmonary failure, left ventricular dysfunction, decreased ejection fraction, right ventricular failure), gastrointestinal events (e.g. gastrointestinal perforation, fistulas), haemorrhagic events (e.g. cerebral haemorrhage, lower gastrointestinal haemorrhage, haematuria, haemoptysis, melaena), arterial thrombotic events (e.g. cerebrovascular accident, MI, retinal artery occlusion, TIA), venous thrombotic events (e.g. pulmonary embolism, deep vein thrombosis, retinal vein occlusion, retinal vein thrombosis).
PO: Z (Embryo-foetal death and harm were observed in animal studies. Not recommended.)
Patient Counseling Information
Women of childbearing potential and men with female partners of reproductive potential must use proven birth control methods during therapy and for 1 week after the last dose. Discontinue breastfeeding during therapy and for 2 weeks after the last dose. This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery.
Monitoring Parameters
Evaluate pregnancy status prior to therapy. Monitor thyroid function and liver function (e.g. ALT, AST, bilirubin) before and during treatment. Monitor blood pressure. Assess for signs and symptoms of heart failure and other CV events, gastrointestinal perforation or fistula, haemorrhage, thromboembolic events and wound healing complications during therapy.
Overdosage
Symptoms: Dizziness, hypertension, seizures associated with hypertension and haemoptysis. Management: Supportive treatment.
Drug Interactions
Increased plasma concentration with strong CYP3A4 or CYP3A5 inhibitors (e.g. ketoconazole, clarithromycin, atazanavir, nefazodone). Decreased plasma concentration with strong CYP3A4 or CYP3A5 inducers (e.g. rifampicin, carbamazepine, phenobarbital, dexamethasone). Increases plasma concentration of theophylline.
Food Interaction
Increased plasma concentration with grapefruit juice. Decreased plasma concentration with St. John's wort.
Action
Description: Mechanism of Action: Axitinib is a potent and selective 2nd-generation tyrosine kinase inhibitor. It inhibits vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), thereby blocking pathologic angiogenesis, tumour growth, and metastatic progression of cancer. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 58%. Time to peak plasma concentration: 2.5-4 hours. Distribution: Volume of distribution: 160 L. Plasma protein binding: >99%, primarily to albumin and α1-acid glycoprotein. Metabolism: Metabolised in the liver by CYP3A4 and CYP3A5, and to a lesser extent by CYP1A2, CYP2C19 and UGT1A1. Excretion: Via faeces (approx 41%; 12% as unchanged drug); urine (approx 23% as metabolites). Elimination half-life: 2.5-6.1 hours.
Chemical Structure
Axitinib Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6450551, Axitinib. https://pubchem.ncbi.nlm.nih.gov/compound/Axitinib. Accessed July 28, 2025.
Storage
Store between 15-30°C. Follow applicable procedures for receiving, handling, administration, and disposal.
L01EK01 - axitinib ; Belongs to the class of vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.
References
Axitinib 1 mg Film-coated Tablets (Accord Healthcare Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/07/2025.Axitinib. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/07/2025.Axitinib. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 07/07/2025.Brayfield A, Cadart C (eds). Axitinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2025.Inlyta 1 mg and 5 mg Film-coated Tablets (Pfizer [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/07/2025.Inlyta 5 mg Film-coated Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/07/2025.Inlyta Tablet, Film Coated (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/07/2025.Joint Formulary Committee. Axitinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/07/2025.Pfizer New Zealand Limited. Inlyta 1 mg and 5 mg Film-coated Tablets data sheet 06 February 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 07/07/2025.
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