Lapatinib
Lapatanib was approved by the FDA in 2007 for use in combination with capecitabine for treatment of patients with advanced or metastaticThe term for a cancer that has spread beyond its point of origin. Metastatic disease is responsible for the majority of cancer deaths. breast cancer if a) their tumors overexpress HER2 and b) they have received prior therapy including anthracycline, a taxaneA derivative of the yew tree. This compound is the basis for several related chemotherapy drugs that work by inhibiting the function of microtubules., and trastuzumab. Lapatinib has the ability to penetrate the blood-brain barrier, so its use in treating brain metastasis is currently under investigation. Lapatinib is administered as an oral tablet.1
Lapatinib (Tykerb®) is a small molecule that functions as tyrosine kinaseAn enzyme that adds phosphate groups to target molecules. Often the targets of these enzymes are proteins that control the cell division process, so the enzymes play a key role in cell division. See also, kinase. inhibitor. It inhibits both EGFR (ErbB1) and HER2 (ErbB2See HER2/neu.). EGFR (epidermal growth factorA substance that stimulates cell division. Growth factors are usually small proteins or steroid hormones. They may be secreted by the same cells on which they act or by cells that reside in a different part of the body than the target cells. Some examples of growth factors include estrogen, a growth factor for breast cells, and VEGF, a growth factor that causes the development of blood vessels. Several different anti-cancer treatments are designed to inhibit the activity of growth factors. receptor) and HER2 (human epidermal growth factor receptor 2) are receptor proteins found on the surface of cells. They bind growth factors, triggering a sequence of events that lead to cell division and apoptosisAlso called programmed cell death. Apoptosis is a natural process that occurs throughout the lives of almost all animals and plants. The death of the cells is a carefully controlled process that does not generate any inflammation..1
The diagram above shows the 3D molecular structure of Lapatinib.
The most common side effect is diarrhea, as it occurs in 65% of patients. Along with this, other side effects can potentially include mouth sores, loss of appetite, indigestion, rash, nausea and vomiting, fatigue, hand-foot syndrome (redness, swelling, and pain on the palms of the hands and/or the soles of the feet.)1
Inform your doctor about any heart conditions prior to treatment with lapatinib. It has been shown to decrease left ventricle ejection fraction (LVEF) in some patients, therefore LVEF should be evaluated in all patients. Lapatinib may also cause toxic effects on the hepatic (liver) system, so inform your doctor about any pre-existing liver conditions. Lapatinib may have harmful effects on a developing fetus, women who are pregnant should not take lapatinib and any woman who becomes pregnant while on lapatinib should inform their doctor immediately. Also, women who are breast feeding should speak with their doctor; it is not known if lapatinib passes into breast milk or what effects it can have on a developing child. Some drugs may interact with lapatinib. Your doctor needs to know what prescription or nonprescription (supplements) drugs you are on to decide the correct dose of lapatinib.1
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