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.
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.
May be taken with or without food.
Chống chỉ định
Recent active GI bleeding, untreated brain metastases. Severe hepatic impairment (Child-Pugh Class C). Lactation.
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.
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.
Increased plasma concentrations w/ grapefruit or grapefruit juice. Reduced plasma concentrations w/ St John’s wort.
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.
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.
L01XE17 - axitinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Anon. Axitinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/05/2017 .Buckingham R (ed). Axitinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/05/2017 .Inlyta Tablet, Film Coated (Pfizer Laboratories Div, Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/05/2017 .Joint Formulary Committee. Axitinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/05/2017 .McEvoy GK, Snow EK, Miller J et al (eds). Axitinib. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/05/2017 .