Lapatinib
Other name
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International/Other brands
Tykerb
Groups
Approved
Structure
Prescription products
| Name | Dosage | Strength | Route | Labeller |
|---|---|---|---|---|
| Tykerb | Tablet | 250 mg/1 | Oral | Glaxosmithkline Inc |
| Tykerb | Tablet | 250 mg | Oral | Novartis |
| Tykerb | Tablet | 250 mg/1 | Oral | Novartis |
| Tyverb | Tablet, film coated | 250 mg | Oral | Novartis Europharm Limited |
Target
-
Description
Lapatinib 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. Lapatinib is human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1) tyrosine kinases inhibitor. It binds to the intracellular phosphorylation domain to prevent receptor autophosphorylation upon ligand binding.
Indications
Metastatic Breast Cancer (MBC); Refractory, advanced Breast cancer; Refractory, metastatic Breast cancer
Other indications
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Mechaism of action
-
Absorption
Absorption following oral administration of lapatinib is incomplete and variable.
Metabolism
Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.
Toxicity
There has been a report of one patient who took 3,000 mg of lapatinib for 10 days. This patient had grade 3 diarrhea and vomiting on day 10.