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At a glance

Lapatinib is used in the treatment of breast cancer. It stops or slows down the growth of cancer cells. It is used for HER2-overexpressing metastatic breast cancer and hormone-positive, HER2-positive breast cancer.

Indications
  • HER2-overexpressing metastatic breast cancer (in combination with capecitabine) - patients who have received prior anthracycline, taxane, and trastuzumab therapy
  • Hormone receptor-positive, HER2-positive breast cancer (in combination with letrozole) - postmenopausal women
Pharmacology

Lapatinib inhibits EGFR and HER2 tyrosine kinase domains, blocking ErbB-driven tumor cell growth. It inhibits angiogenesis and cellular proliferation.

Dosage

HER2-Positive Metastatic Breast Cancer:

  • 1,250 mg PO once daily on Days 1-21 + Capecitabine 2,000 mg/m²/day on Days 1-14 in a 21-day cycle
  • Take at least 1 hour before or 1 hour after a meal

Hormone Receptor-Positive, HER2-Positive Breast Cancer:

  • 1,500 mg PO once daily + Letrozole 2.5 mg once daily
  • Take at least 1 hour before or 1 hour after a meal

Hepatic Impairment (Child-Pugh C): 1,250→750 mg/day (HER2+) or 1,500→1,000 mg/day (HR+/HER2+)

Side effects

Common Side Effects (with Capecitabine):

  • Diarrhea
  • Palmar-plantar erythrodysesthesia
  • Nausea
  • Rash
  • Vomiting
  • Fatigue

Other Side Effects:

  • Abdominal pain, back pain, dyspnea, constipation, cough, headache, hot flashes, joint pain, hepatotoxicity, decreased appetite, stomatitis
Use in pregnancy

Use in Pregnancy: Lapatinib is unsafe during pregnancy; definite evidence of risk to the fetus. Use only in life-threatening situations with doctor's advice.

Precautions & warnings
  • Monitor for decreased LVEF (especially during first 12 weeks)
  • Monitor liver function tests every 4-6 weeks for hepatotoxicity
  • Monitor for diarrhea and treat with loperamide
  • Monitor for interstitial lung disease/pneumonitis
  • Monitor for QT prolongation
  • Monitor for severe cutaneous reactions (Stevens-Johnson, toxic epidermal necrolysis)
  • Can cause fetal harm during pregnancy
Overdose effects

No known antidote for overdose; doses of 2,500-9,000 mg/day have caused sore scalp, sinus tachycardia, mucosal inflammation. Hemodialysis is not effective.

Storage conditions

Store below 30°C in a dry place; keep out of reach of children.

Lapatinib — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.