Concise Prescribing Info
Lapatinib ditosylate
In combination w/ capecitabine for patients w/ advanced or metastatic breast cancer whose tumors overexpress HER2 & who have received prior therapy including anthracycline, taxane & trastuzumab. In combination w/ letrozole for postmenopausal women w/ hormone receptor +ve metastatic breast cancer that overexpress HER2 receptor for whom hormonal therapy is indicated.
Dosage/Direction for Use
HER2 +ve metastatic breast cancer 1,250 mg once daily continuously on days 1-21 w/ capecitabine 2,000 mg/m2 daily in 2 doses approx 12 hr apart on days 1-14 for 21-day cycle. Severe hepatic impairment (Child-Pugh Class C) Reduce to 750 mg daily. Hormone receptor +ve, HER2 +ve metastatic breast cancer 1,500 mg once daily continuously w/ letrozole 2.5 mg once daily. Severe hepatic impairment (Child-Pugh Class C) Reduce to 1,000 mg daily.
Should be taken on an empty stomach: Take at least 1 hr before or 1 hr after a meal. Do not eat/drink grapefruit products.
Special Precautions
Discontinue use if erythema multiforme, SJS or TEN are suspected. ILD/pneumonitis; diarrhea. Conditions impairing left ventricular ejection fraction (LVEF); hypokalemia or hypomagnesemia, congenital long QT syndrome. Monitor LFTs prior to, every 4-6 wk during treatment & as clinically indicated. Evaluate LVEF & correct hypokalemia or -magnesemia prior to treatment. Avoid concomitant use w/ grapefruit, strong CYP3A4 inhibitors & inducers. Concomitant use w/ antiarrhythmics or other medicinal products w/ known risk for QT prolongation/Torsade de pointes, cumulative high-dose anthracycline therapy. Severe preexisting hepatic impairment. Male patients & women of childbearing potential should use effective contraception during & 1 wk after last dose. Pregnancy. Not to be used during lactation & for 1 wk after last dose. Ped.
Adverse Reactions
Diarrhea, nausea, vomiting, stomatitis, dyspepsia, anorexia; palmar-plantar erythrodysesthesia, rash, dry skin, alopecia, pruritus, nail disorder; mucosal inflammation, fatigue, asthenia; pain in extremity, back pain, arthralgia; dyspnea, epistaxis, cough; insomnia; headache; decreased appetite; paronychia; increased ALT & AST.
Drug Interactions
Increased systemic exposure of midazolam, paclitaxel, digoxin. Increased systemic exposure w/ ketoconazole. Decreased systemic exposure w/ carbamazepine. Increased plasma conc w/ P-gp inhibitors; grapefruit. Strong CYP3A4 inhibitors (eg, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole) & inducers (eg, dexamethasone, phenytoin, rifampin, rifabutin, rifapentine, phenobarb, St. John's wort).
MIMS Class
Targeted Cancer Therapy
ATC Classification
L01EH01 - lapatinib ; Belongs to the class of human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors. Used in the treatment of cancer.
Tykerb FC tab 250 mg
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