This site is intended for UK healthcare professionals
Medscape UK Univadis Logo
Medscape UK Univadis Logo

Axitinib oral


Tablets containing axitinib.

Drugs List

  • axitinib 1mg film coated tablets
  • axitinib 3mg film coated tablets
  • axitinib 5mg film coated tablets
  • axitinib 7mg film coated tablets
  • INLYTA 1mg film coated tablets
  • INLYTA 3mg film coated tablets
  • INLYTA 5mg film coated tablets
  • INLYTA 7mg film coated tablets
  • Therapeutic Indications


    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
    Brain neoplasm
    Gastrointestinal haemorrhage
    Severe hepatic impairment - Child-Pugh score greater than or equal to 10
    Uncontrolled hypertension

    Precautions and Warnings

    Predisposition to thromboembolic disease
    Tobacco smoking
    Arterial aneurysm
    Behcet's disease
    Cerebrovascular accident
    Cerebrovascular disorder
    Deep vein thrombosis
    Diabetes mellitus
    Giant cell arteritis
    Glucose-galactose malabsorption syndrome
    Hepatic impairment - Child-Pugh score between 7 and 9
    History of aneurysm
    Ischaemic heart disease
    Lactose intolerance
    Marfan syndrome
    Myocardial infarction
    Occlusive peripheral arterial disease
    Pulmonary embolism
    Renal impairment - creatinine clearance below 15ml/minute
    Retinal blood vessel occlusion
    Takayasu arteritis
    Thromboembolic disorder
    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
    Contains lactose
    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 ( ) or if this is unavailable at the backup site ( ).


    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


    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.

    Side Effects

    Abdominal pain
    Artery dissection
    Cardiac failure
    Cardiopulmonary failure
    Congestive cardiac failure
    Decreased appetite
    Decreased ejection fraction
    Dry skin
    Elevated amylase levels
    Elevated serum lipase
    Elevated TSH
    Extremity pain
    Gastro-intestinal fistulae
    Gastro-intestinal perforation
    Hypertensive crisis
    Increase in alkaline phosphatase
    Increase in creatinine
    Increase in serum ALT/AST
    Mucosal inflammation
    Oropharyngeal pain
    Palmar-Plantar Erythrodysaesthesia syndrome
    Posterior reversible encephalopathy syndrome (PRES)
    Renal failure
    Serum bilirubin increased
    Thromboembolic disorders
    Upper abdominal pain
    Ventricular dysfunction
    Weight loss


    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 ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: November 2015

    Reference Sources

    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:
    Last accessed: 10 November 2020

    Summary of Product Characteristics: Inlyta 1mg 3mg, 5mg and 7mg film-coated tablets. Pfizer Ltd. November 2019.

    Access the full UK drug database with a FREE Medscape UK Account
    It takes just a few minutes, and you’ll get unlimited access to information on over 11,000 UK drugs.
    Register for Free

    Already a member? Log in

    Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content

    FDB Logo

    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.