Drug reference

Lapatinib

Tyrosine Kinase Inhibitor · Antineoplastic

Also known as GW572016

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid—

FDA category + note

Top interactionssee all 12 →

Aminolevulinic AcidSevereDatabaseDDInter
AmiodaroneSevereDatabaseDDInter
AmisulprideSevereDatabaseDDInter
AmprenavirSevereDatabaseDDInter

Mechanism

Lapatinib is a tyrosine kinase inhibitor. Its central nervous system (CNS) penetration is influenced by P-glycoprotein and breast cancer resistance protein, which exhibit a synergistic role.

Indications

Metastatic hormone-receptor-positive breast cancer that overexpresses human epidermal growth factor receptor 2 (HER2) (not recommended for first-line treatment in postmenopausal women when combined with an aromatase inhibitor)metastatic HER2-positive trastuzumab-refractory breast cancer (in combination with capecitabine)postmenopausal women with hormone receptor–positive, metastatic breast cancer that overexpresses HER2 (in combination with letrozole)Approved for use in early-stage breast cancer

Dosing

Adult: locally recurrent unresectable breast cancer, in adults who have not had previous anti-HER2 therapy or chemotherapy for their metastatic disease, only if the manufacturer provides pertuzumab within the agreed commercial access arrangement.…

Pharmacokinetics

Half-life

14 h

Metabolism

CYP3A4

Contraindications

First-line treatment in postmenopausal women with metastatic hormone-receptor-positive breast cancer that overexpresses human epidermal growth factor receptor 2 (HER2), when used in combination with an aromatase inhibitor