Axitinib


Concise Prescribing Info
Indications/Uses
Advanced renal cell carcinoma.
Dosage/Direction for Use
Adult : PO Initial: 5 mg bid (approx 12 hrly), may be increased to 7 mg bid then 10 mg bid, based on patient’s tolerance. The 5 mg bid dose may be reduced to 3 mg bid and further to 2 mg bid, if necessary.
Dosage Details
Oral
Advanced renal cell carcinoma
Adult: Initially, 5 mg bid (given approx 12 hrly), may be increased further to 7 mg bid, then 10 mg bid, if the initial dose is tolerated (patients w/ no AR above grade 2, w/ normal BP, and are not receiving antihypertensive therapy) for at least 2 consecutive wk. If dosage reduction is needed due to AR, 5 mg bid dose may be reduced to 3 mg bid and further to 2 mg bid.
Special Patient Group
Patients taking strong CYP3A4/5 inhibitors: Reduce to approx 50% of the usual initial dose (e.g. 5 mg bid reduced to 2 mg bid), w/ further adjustments according to response.
Hepatic Impairment
Moderate (Child-Pugh Class B): Reduce to approx 50% of the usual initial dose (e.g. 5 mg bid reduced to 2 mg bid), w/ further adjustments according to response. Severe (Child-Pugh Class C): Contraindicated.
Administration
May be taken with or without food.
Contraindications
Recent active GI bleeding, untreated brain metastases. Severe hepatic impairment (Child-Pugh Class C). Lactation.
Special Precautions
Patient w/ HTN, cardiac disease, history of or risk for thrombosis. Patients taking strong CYP3A4 inhibitors. Withhold treatment at least 24 hr prior to scheduled surgery. Moderate hepatic impairment (Child-Pugh Class B). Pregnancy.
Adverse Reactions
Significant: HTN, posterior reversible leukoencephalopathy syndrome, proteinuria, thyroid dysfunction, increased Hb or haematocrit, impaired wound healing.
Nervous: Headache, fatigue, asthenia.
GI: GI disturbance, decreased appetite, nausea, vomiting, oral mucositis, taste disturbance, vocal changes, dysphonia, abdominal pain, dyspepsia, diarrhoea, constipation.
Hepatic: Increased hepatic enzymes and bilirubin.
Endocrine: Wt loss.
Musculoskeletal: Arthralgia, myalgia.
Dermatologic: Palmar-plantar erythrodysaesthesia, rash, dry skin, itch, erythema, alopecia.
Others: Electrolyte disturbance.
Potentially Fatal: Cardiac failure, arterial thrombotic events (e.g. MI, TIA, CVA, retinal artery exclusion), venous thrombotic events (e.g. DVT, pulmonary embolism, retinal vein occlusion or thrombosis), hypertensive crisis, haemorrhagic events (e.g. GI or cerebral haemorrhage, haemoptysis, haematuria, melaena), GI perforation and fistula formation.
Patient Counseling Information
This drug may cause dizziness and fatigue, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor BP, Hb or haematocrit, LFT, thyroid function, and urinalysis (for proteinuria) prior to and during treatment.
Overdosage
Symptoms: Dizziness, HTN, seizures, haemoptysis. Management: Supportive treatment.
Drug Interactions
Plasma concentration is increased by strong CYP3A4/5 inhibitors (e.g. ketoconazole, ritonavir, clarithromycin) and decreased by strong CYP3A4/5 inducers (e.g. rifampicin, phenytoin, carbamazepine). May enhance adverse effects (e.g. osteonecrosis of the jaw) of bisphosphonate derivatives.
Food Interaction
Increased plasma concentrations w/ grapefruit or grapefruit juice. Reduced plasma concentrations w/ St John’s wort.
Action
Description: Axitinib, a selective 2nd generation tyrosine kinase inhibitor, blocks angiogenesis, tumour growth, and cancer progression by inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3).
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 58%. Time to peak plasma concentration: 2.5-4 hr.
Distribution: Volume of distribution: 160 L. Plasma protein binding: >99%, mainly to albumin and α1-acid glycoprotein.
Metabolism: Metabolised in the liver mainly by CYP3A4/5, and to a lesser extent by CYP1A2, CYP2C19, and UGT1A1.
Excretion: Via faeces (approx 41%, 12% as unchanged drug) and urine (approx 23%, as metabolites). Elimination half-life: 2.5-6.1 hr.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store between 20-25°C.
This is a cytotoxic drug. Use appropriate personal protective equipment (e.g. gloves) for receiving, handling, admin, and disposal. Any unused portions should be disposed of in accordance w/ local requirements.
ATC Classification
L01XE17 - axitinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Disclaimer: This information is independently developed by MIMS based on Axitinib from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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