Monograph Details
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Neoplasms
> Kinase inhibitors
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TYKERB |
| Manufacturer |
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GlaxoSmithKline Pharmaceuticals |
| Legal Classification |
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Rx
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| Pharmacological Class |
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Tyrosine kinase inhibitor. |
| Generic Name |
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Lapatinib 250mg; tabs. |
| Indications |
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In combination with capecitabine, for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab. |
| Children |
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Not recommended. |
| Adults |
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Take 1 hour before or 1 hour after a meal. Take once daily on Days 1–21 continuously with capecitabine (see literature for capecitabine dose) in a repeating 21 day cycle; continue until disease progression or unacceptable toxicity occurs. 1250mg (5 tablets). Severe hepatic dysfunction (Child-Pugh Class C): 750mg (no clinical data for this dose adjustment). After recovery from left ventricular ejection fraction (LVEF) decrease: 1g. Concomitant potent CYP3A4 inhibitors: 500mg (no clinical data for this dose adjustment). Concomitant potent CYP3A4 inducers: may titrate up to 4500mg (no clinical data for this dose adjustment). Discontinue if ≥grade 2 NCI CTC toxicity occurs; may restart at 1250mg if toxicity improves to grade 1; if recurs, may restart at 1g. |
| Precautions |
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Confirm normal LVEF before starting. Discontinue if ≥grade 2 decrease in LVEF occurs, or if LVEF falls below institution's lower limit of normal; may restart after at least 2 weeks at reduced dose if asymptomatic and LVEF recovers. Conditions that impair left ventricular function, or risk factors for QT prolongation (eg, hypokalemia, hypomagnesemia, congenital long QT syndrome, concomitant antiarrhythmics, cumulative high dose anthracyclines); correct electrolyte disturbances before starting. Monitor for interstitial lung disease or pneumonitis; discontinue if pulmonary symptoms ≥grade 3 (NCI CTCAE). Severe hepatic impairment. Pretreat for diarrhea with antimotility drugs. Monitor ECG. Pregnancy (Cat.D). Nursing mothers: not recommended. |
| Interactions |
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Avoid potent CYP3A4 inhibitors (eg, ketoconazole), grapefruit; reduce dose if unavoidable. Avoid potent CYP3A4 inducers (eg, carbamazepine); slowly titrate dose up if unavoidable. May affect drugs that are affected by p-glycoprotein, CYP2C8. |
| Adverse Reactions |
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Diarrhea (may be severe), nausea, vomiting, hand/foot syndrome, rash, fatigue; decreased LVEF, QT prolongation, interstitial lung disease, pneumonitis. |
| How Supplied |
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Tabs—150 |
| Additional Resources |
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• Related Prescribing Note |
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