- Drugs List
- Therapeutic Indications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
Tablets containing axitinib.
Advanced renal cell carcinoma
Treatment of advanced renal cell carcinoma after failure of prior treatment with sunitinib or a cytokine.
Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.
The recommended starting dose is 5mg twice daily. Treatment should continue as long as clinical benefit is observed or until unacceptable toxicity occurs.
Patients who tolerate the starting dose of 5mg twice daily with no greater than Grade 2 adverse reactions for 2 consecutive weeks may have the dose increased to 7mg twice daily unless the patient's blood pressure is greater than 150/90mmHg or they are receiving antihypertensive treatment. If the patient tolerates the 7mg twice daily dose they may have their dose increased to a maximum of 10mg twice daily using the same criteria as before.
Some adverse reactions may require temporary or permanent discontinuation and/or dose reduction. When dose reduction is required, the axitinib dose may be reduced to 3mg twice daily and further to 2mg twice daily.
Patients with Hepatic Impairment
Child-Pugh Class A = Score between 5 and 6: No dose adjustment required
Child Pugh Class B = Score between 7 and 9: Starting dose should be reduced from 5mg twice daily to 2mg twice daily
Child-Pugh Class C = Score between 10 and 15: Contraindicated in these patients
Additional Dosage Information
Reduce dosage to approximately half the dose when given in conjunction with a strong CYP450 3A4/5 inhibitor.
Return to normal dose when the inhibitor is discontinued.
A gradual dose increase is recommended in patients when given in conjunction with a strong CYP450 3A4/5 inducer.
When the inducer is discontinued immediately return to previously prescribed dose of axitinib.
Children under 18 years
Severe hepatic impairment - Child-Pugh score greater than or equal to 10
Precautions and Warnings
Predisposition to thromboembolic disease
Deep vein thrombosis
Giant cell arteritis
Glucose-galactose malabsorption syndrome
Hepatic impairment - Child-Pugh score between 7 and 9
History of aneurysm
Ischaemic heart disease
Occlusive peripheral arterial disease
Renal impairment - creatinine clearance below 15ml/minute
Retinal blood vessel occlusion
Transient ischaemic attack
Vascular Ehlers-Danlos syndrome
Reduce dose in patients with moderate hepatic impairment
Advise ability to drive/operate machinery may be affected by side effects
Ensure hypertension is controlled prior to treatment
Treatment to be initiated and supervised by a specialist
Consult local policy on the safe use of oral anti-cancer drugs
Staff: Not to be handled by pregnant staff
Monitor for proteinuria before and periodically during treatment
Monitor haemoglobin prior to initiating therapy and periodically thereafter
Monitor hepatic function before treatment and regularly during treatment
Monitor thyroid function prior to and periodically during treatment
Monitor blood pressure regularly
Monitor for symptoms of gastrointestinal perforation or fistula
Monitor haematocrit values
Monitor patients for signs and symptoms of cardiac failure
Advise patient to report headaches, seizures, confusion, visual disturbance
Consider discontinuing therapy if significant cardiac failure develops
Consider dose reduction if cardiac failure occurs
Reduce dose if hypertension cannot be controlled
Discontinue treatment 24 hours prior to surgery
Discontinue if nephrotic syndrome occurs
Discontinue if posterior reversible encephalopathy syndrome (PRES) develops
Discontinue if significant proteinuria occurs, treat and restart therapy
Suspend treatment in severe hypertension that cannot be controlled
Suspend treatment if bleeding requiring medical treatment occurs
Advise patient not to take St John's wort concurrently
Advise patient grapefruit products may increase plasma level
May cause impaired fertility
Female: Contraception required during and for 1 week after treatment
Advise patient on giving up smoking
Posterior reversible encephalopathy syndrome (PRES) has been reported in some patients treated with this agent. If patients present with symptoms indicating PRES such as headache, altered mental state, seizures and visual disturbances, an MRI should be performed. If PRES is diagnosed, treatment should be discontinued and adequate blood pressure and seizure control administration is advisable. The safety of reinstating treatment in patients previously experiencing PRES is unknown.
Risk factors for aneurysm and artery dissection
Use of systemic VEGF inhibitors may promote the formation of aneurysms or artery dissections, mainly in relation to aortic aneurysm rupture and aortic dissection. It is therefore important to consider the risk of aneurysm and artery dissection in patients with risk factors such as hypertension, history of aneurysm, smoking, diabetes, coronary, cerebrovascular or peripheral arterial disease, and hyperlipidaemia. Other risk factors include Marfan syndrome, vascular Ehlers-Danlos syndrome, Takayasu arteritis, and the use of fluoroquinolones. In patients receiving VEGF inhibitors, any modifiable risk factors such as smoking and hypertension should be reduced as far as possible.
Pregnancy and Lactation
Axitinib is contraindicated for use during pregnancy.
Animal studies have shown reproductive toxicity including malformations.
The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Axitinib is contraindicated in breastfeeding.
It is unknown whether axitinib is excreted in human milk but a risk to the nursing infant cannot be excluded.
Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1
Advise patient that if they vomit or miss a dose, an additional dose should not be taken. The next prescribed dose should be taken at the usual time.
Advise patient to take orally twice daily approximately 12 hours apart with or with out food. Tablets should be swallowed whole with a glass of water.
Advise women of child bearing potential to take adequate contraception during and for 1 week after treatment.
Congestive cardiac failure
Decreased ejection fraction
Elevated amylase levels
Elevated serum lipase
Increase in alkaline phosphatase
Increase in creatinine
Increase in serum ALT/AST
Palmar-Plantar Erythrodysaesthesia syndrome
Posterior reversible encephalopathy syndrome (PRES)
Serum bilirubin increased
Upper abdominal pain
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Last Full Review Date: November 2015
Martindale: The Complete Drug Reference (online) London: Brayfield A (ed). Pharmaceutical Press. Accessed on 2 November 2015.
MHRA Drug Safety Update July 2020
Available at: https://www.gov.uk/drug-safety-update/systemically-administered-vegf-pathway-inhibitors-risk-of-aneurysm-and-artery-dissection
Last accessed: 10 November 2020
Summary of Product Characteristics: Inlyta 1mg 3mg, 5mg and 7mg film-coated tablets. Pfizer Ltd. November 2019.
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Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.