Lapatinib
- Atc Codes:L01XE07
- CAS Codes:388082-78-8#231277-92-2
- PHARMGKB ID:388082-78-8#231277-92-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Tyverb; Belgium: Tyverb; Bulgaria: Tyverb; Cyprus: Tyverb; Czech Republic: Tyverb; Denmark: Tyverb; Estonia: Tyverb; Finland: Tyverb; France: Tyverb; Germany: Tyverb; Greece: Tyverb; Hungary: Tyverb; Ireland: Tyverb; Italy: Tyverb; Latvia: Tyverb; Lithuania: Tyverb; Luxembourg: Tyverb; Malta: Tyverb; Netherlands: Tyverb; Poland: Tyverb; Portugal: Tyverb; Romania: Tyverb; Slovakia: Tyverb; Slovenia: Tyverb; Spain: Tyverb; Sweden: Tyverb; UK: Tyverb.North America
Canada: Tykerb; USA: Tykerb.
Drug combinations
Lapatinib and Capecitabine
Chemistry
Lapatinib Ditosylate: C~29~H~26~ClFN~4~O~4~S 2C~7~H~8~O~3~S H~2~O. Mw: 943.48. (1) 4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, bis(4-methylbenzenesulfonate), monohydrate; (2) N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]furan-2-yl]quinazolin-4-amine bis(4-methylbenzenesulfonate) monohydrate. CAS-388082-78-8; CAS-231277-92-2 (lapatinib)(2003).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. Epidermal Growth Factor Receptor Inhibitor. (ATC-Code: L01XE07).
Mechanism of action
Tyrosine kinase (dual kinase) inhibitor. Inhibitor of EGFR (ErbB1) and HER2/ERBB2 (ErbB2) by reversibly binding to tyrosine kinase, blocking phosphorylation and activation of downstream second messengers (Erk1, Erk2 and Akt), regulating cellular proliferation and survival in ErbB- and ErbB2-expressing tumors.
Therapeutic use
Treatment (in combination with capecitabine) of HER2/neu-overexpressing advanced or metastatic breast cancer, in patients who have received prior therapy (with an anthracycline, a taxane, and trastuzumab).
Pregnancy and lactiation implications
Increased pup deaths demonstrated in animal studies. There are no adequate studies in pregnant women. Lapatinib may cause fetal harm if administered during pregnancy. Not recommended during lactation.
Unlabeled use
Treatment of head and neck cancers.
Contraindications
None known to date.
Warnings and precautions
Hazardous agent. Diarrhea common, and may be severe. Hepatotoxicity might occur (may be severe and/or fatal). Left ventricular dysfunction possible. Use with caution in history of or predisposition (prior treatment with anthracyclines, chest wall irradiation) to left ventricular dysfunction. Pulmonary toxicity (interstitial lung disease and pneumonitis) reported (with lapatinib monotherapy and combination chemotherapy). QTc prolongation might occur. Concurrent use with other drugs which may prolong QTc interval may increase risk of potentially-fatal arrhythmias. Use with caution in hepatic dysfunction. High potential for CYP-mediated interactions.