Lapatinib

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Lapatinib
Systematic (IUPAC) name
N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6- [5-[(2-methylsulfonylethylamino)methyl]-2-furyl] quinazolin-4-amine
Identifiers
CAS number	388082-78-8
ATC code	?
PubChem	208908
Chemical data
Formula	C29H26ClFN4O4S
Mol. mass	581.058 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	24 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	Oral

WikiDoc Resources for Lapatinib
Articles
Most recent articles on Lapatinib Most cited articles on Lapatinib Review articles on Lapatinib Articles on Lapatinib in N Eng J Med, Lancet, BMJ
Media
Powerpoint slides on Lapatinib Images of Lapatinib Photos of Lapatinib Podcasts & MP3s on Lapatinib Videos on Lapatinib
Evidence Based Medicine
Cochrane Collaboration on Lapatinib Bandolier on Lapatinib TRIP on Lapatinib
Clinical Trials
Ongoing Trials on Lapatinib at Clinical Trials.gov Trial results on Lapatinib Clinical Trials on Lapatinib at Google
Guidelines / Policies / Govt
US National Guidelines Clearinghouse on Lapatinib NICE Guidance on Lapatinib NHS PRODIGY Guidance FDA on Lapatinib CDC on Lapatinib
Books
Books on Lapatinib
News
Lapatinib in the news Be alerted to news on Lapatinib News trends on Lapatinib
Commentary
Blogs on Lapatinib
Definitions
Definitions of Lapatinib
Patient Resources / Community
Patient resources on Lapatinib Discussion groups on Lapatinib Patient Handouts on Lapatinib Directions to Hospitals Treating Lapatinib Risk calculators and risk factors for Lapatinib
Healthcare Provider Resources
Symptoms of Lapatinib Causes & Risk Factors for Lapatinib Diagnostic studies for Lapatinib Treatment of Lapatinib
Continuing Medical Education (CME)
CME Programs on Lapatinib
International
Lapatinib en Espanol Lapatinib en Francais
Business
Lapatinib in the Marketplace Patents on Lapatinib
Experimental / Informatics
List of terms related to Lapatinib

Overview

Lapatinib (INN) or lapatinib ditosylate (USAN), also known as GW572016, is an anti-cancer drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug capecitabine (Xeloda TM). It is marketed by GSK in the U.S. as Tykerb. Once regulatory approval has been granted, it will be marketed as Tyverb in Europe.

Lapatinib is a once-daily oral drug indicated for women who have received prior treatment with the intravenous drug trastuzumab (Herceptin TM) and cancer drugs called taxanes and anthracyclines. [1]

Lapatinib is an ATP-competitive epidermal growth factor receptor (EGFR) and HER2/neu (ErbB-2) dual tyrosine kinase inhibitor. It inhibits receptor autophosphorylation and activation by binding to the ATP-binding pocket of the EGFR/HER2 protein kinase domain.

In patients with HER2/neu positive metastatic breast cancer that has progressed following treatment with previous chemotherapy regimens that included an anthracycline, a taxane, and trastuzumab, randomized clinical trial has demonstrated that the addition of lapatinib to capecitabine delayed the time of further cancer growth compared to capecitabine alone.[2]

Additional images

• Lapatinib 3D.png

  3D structure of the Lapatinib molecule

References

• Burris H (2004). "Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib.". Oncologist 9 Suppl 3: 10-5. PMID 15163842.
• Nelson M, Dolder C (2006). "Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors.". Ann Pharmacother 40 (2): 261-9. PMID 16418322.
• Burris H. A., Hurwitz H. I., Dees E. C. (2005). "Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas.". J Clin Oncol 23 (23): 5305-13. PMID 15955900.
• Geyer CE, Forster J, Lindquist D, et al. (2006). "Lapatinib plus capecitabine for HER2-positive advanced breast cancer.". N Engl J Med 355 (26): 2733-43. PMID 17192538.
• Canadian drug touted for advanced breast cancer

External links

• Lapatinib Ditosylate - National Cancer Institute

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