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Lapatinib oral


Tablets containing lapatinib

Drugs List

  • lapatinib 250mg film coated tablets
  • TYVERB 250mg film coated tablets
  • Therapeutic Indications


    Combined with aromatase inhibitor for ErbB2 positive breast cancer
    Combined with capecitabine for advanced/metastatic ErbB2 +ve breast cancer
    Combined with trastuzumab in hormone receptor-negative breast cancer

    In combination with capecitabine for the treatment of advanced or metastatic breast cancer for tumours that over express ErbB2 (HER2), following prior treatment with anthracyclines and taxanes and with trastuzumab in the metastatic setting.

    In combination with trastuzumab for patients with hormone receptor negative metastatic disease that has progressed on prior trastuzumab therapy(ies) in combination with chemotherapy.

    In combination with an aromatase inhibitor for postmenopausal women with hormone receptor positive metastatic breast cancer, not currently intended for chemotherapy.


    Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.

    Treatment should be initiated and supervised by physicians experienced in cancer chemotherapy.

    The dose should not be divided.


    In combination with capecitabine
    The recommended dose of lapatinib is 1250 mg once daily continuously.

    The recommended dose of capecitabine is 2000 mg/square metre/day taken in 2 doses with food 12 hours apart on days 1 to 14 in a 21 day cycle. (See capecitabine prescribing information for further information)

    In combination with trastuzumab
    The recommended dose of lapatinib is 1000 mg once daily continuously.

    The recommended dose of trastuzumab is 4 mg/kg administered as an intravenous loading dose, followed by 2 mg/kg intravenous weekly. (See trastuzumab prescribing information for further information)

    In combination with aromatase inhibitor
    The recommended dose of lapatinib is 1500 mg once daily continuously.

    Please refer to prescribing information of the co-administered aromatase inhibitor for dosing details.


    (See Dosage; Adult)

    Additional Dosage Information

    All grading is based on National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE)

    Cardiac events
    Grade 3 or greater left ventricular ejection fraction (LVEF) or LVEF drops below the institutions lower limit of normal: withhold treatment until symptoms have recovered to normal and the patient has been asymptomatic for a minimum period of 2 weeks.

    Lapatinib may be restarted at the following reduced doses:
    750 mg/day when administered with trastuzumab.
    1000 mg/day when administered with capecitabine.
    1250 mg/day when administered with an aromatase inhibitor.

    Interstitial lung disease/pneumonitis
    Grade 3 or greater: discontinue.

    Grade 3 or grade 1 or 2 with complicating features: withhold treatment until diarrhoea resolves to grade 1.

    Consider the following dose reduction upon reintroduction:
    750 mg/day when administered with trastuzumab.
    1000 mg/day when administered with capecitabine.
    1250 mg/day when administered with an aromatase inhibitor.

    Grade 4: discontinue permanently.

    Other toxicities
    Grade 2 or greater: consider discontinuation or interruption.
    Dosing can be restarted once toxicity recovers to grade 1 or less.

    If the toxicity recurs lapatinib should be restarted at:
    750 mg/day when administered with trastuzumab.
    1000 mg/day when administered with capecitabine.
    1250 mg/day when administered with an aromatase inhibitor.

    See prescribing individual information for capecitabine, trastuzumab and aromatase inhibitor for dose delay and reduction guidelines.

    Missed doses
    Missed doses should not be replaced and dosing should resume with the next scheduled dose.


    Lapatinib should be taken either at least 1 hour before or at least 1 hour after food. To minimise variability to the patient administration should be standardised in relation to food intake.


    Children under 18 years
    Long QT syndrome
    Torsade de pointes

    Precautions and Warnings

    Family history of long QT syndrome
    Electrolyte imbalance
    History of torsade de pointes
    Moderate hepatic impairment
    Reduced left ventricular function
    Severe renal impairment

    Correct electrolyte disorders before treatment
    Anti-diarrhoeals may be required during treatment
    Treatment to be prescribed under the supervision of a specialist
    Consult local policy on the safe use of oral anti-cancer drugs
    HER2 testing is mandatory prior to initiation of therapy
    Measurement of LV ejection fraction recommended before and during treatment
    Monitor ECG before, 1-2 weeks after treatment initiation and as indicated
    Monitor hepatic function before initiating and at monthly intervals
    Monitor for signs of pulmonary toxicity on long term therapy
    Monitor serum electrolytes
    Advise patient to report bowel dysfunction immediately
    Advise patient to report skin reaction, pain, erythema, pruritus
    Discontinue if pulmonary symptom grade 3 or worse occur
    Discontinue treatment if Stevens-Johnson Syndrome suspected
    Discontinue treatment if toxic epidermal necrolysis is suspected
    Consider suspending treatment for any grade 2 or worse toxicity
    Discontinue if severe hepatic changes occur
    Discontinue permanently if grade 4 diarrhoea occurs
    Interrupt treatment if diarrhoea grade 3 or grades 1 or 2 with complication
    Suspend treatment if LVEF falls below 40%
    Advise patient not to take St John's wort concurrently
    Advise patient grapefruit products may increase plasma level
    Female: Contraception required during and at least 5 days after treatment
    Advise patient to avoid exposure to direct sunlight

    Pregnancy and Lactation


    Contraindicated in pregnancy.

    Animal studies have shown no teratogenic effects in rats or rabbits at 30, 60 and 120 mg/kg/day. There were minor foetal abnormalities and increased abortions in rats and rabbits at maternally toxic doses.

    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 ( )


    Lapatinib is contraindicated in breastfeeding.

    Breastfeeding should be discontinued during and for 5 days after the last dose of lapatinib.

    It is unknown whether lapatinib is excreted in human breast milk. In rats, growth retardation was observed in pups that were exposed to lapatinib via breast milk.

    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

    Side Effects

    Abdominal pain
    Acne-like rash
    Back pain
    Cardiac failure
    Decreased ejection fraction
    Dry skin
    Erythema multiforme
    Extremity pain
    Hot flushes
    Hypersensitivity reactions
    Interstitial lung disease
    Mucosal inflammation
    Nail disorders
    Palmar-plantar erythrodysaesthesia
    Pulmonary hypertension
    Stevens-Johnson syndrome
    Toxic epidermal necrolysis


    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: December 2013

    Reference Sources

    Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 9th edition (2011) ed. Briggs, G., Freeman, R. and Yaffe, S. Lippincott Williams & Wilkins, Philadelphia.

    NICE Evidence Services Available at: Last accessed: 21 July 2015.

    Summary of Product Characteristics: Tyverb 250mg tablets. GlaxoSmithKline UK. Revised May 2019.

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

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