Lapatinib
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| Clinical data | |
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| Trade names | Tykerb, Tyverb |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607055 |
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| Routes of administration |
By mouth (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | Variable, increased with food |
| Protein binding | >99% |
| Metabolism | Hepatic, mostly CYP3A-mediated (minor 2C19 and 2C8 involvement) |
| Biological half-life | 24 hours (repeated dosing), 14.2 hours (single dose) |
| Excretion | Mostly fecal |
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| ECHA InfoCard | 100.170.767 |
| Chemical and physical data | |
| Formula | C29H26ClFN4O4S |
| Molar mass | 581.058 g/mol |
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  (what is this?)
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Lapatinib (INN), used in the form of lapatinib ditosylate (USAN) (trade names Tykerb and Tyverb) is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).
On March 13, 2007, the U.S. Food and Drug Administration (FDA) approved lapatinib in combination therapy for breast cancer patients already using capecitabine (Xeloda). In January 2010, Tykerb received accelerated approval for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer that overexpresses the HER2 receptor and for whom hormonal therapy is indicated (in combination with letrozole).
Pharmaceutical company GlaxoSmithKline (GSK) markets the drug under the propriety names Tykerb (mostly U.S.) and Tyverb (mostly Europe and Russia). The drug currently has approval for sale and clinical use in the US, Australia, Bahrain, Kuwait, Venezuela, Brazil, New Zealand, South Korea, Switzerland, Japan, Jordan, the European Union, Lebanon, India and Pakistan.
On the August 2, 2013, India's Intellectual Property Appellate Board revoked the patent for Glaxo's Tykerb citing its derivative status, while upholding at the same time the original patent granted for lapatinib.
The drug lapatinib ditosylate is classified as S/NM (a synthetic compound showing competitive inhibition of the natural product) that is naturally derived or inspired substrate (Gordon M. Cragg, Paul G. Grothaus, and David J. Newman, Impact of Natural Products on Developing New Anti-Cancer Agents, Chem. Rev. 2009, 109, 3012–3043)
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