Erlotinib
The FDA has approved erlotinib to treat: Locally 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. non-small cell lung cancer (after failure of at least one prior therapy), as well as locally advanced, unresectable or metastatic pancreatic cancer (in combination with gemcitabine).1
Erlotinib (Tarceva®) is a 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 associated with the human 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 (EGFR). By inhibiting the function of EGFR, which is overexpressed in cancer cells, erlotinib blocks cell proliferationRefers to cell division. The proliferation rate is an indicator of how quickly a tumor is growing. The proliferation rate may be represented as a percentage, showing what fraction of the cells are actively involved in the division process. and promotes death of cancer cells.1
The diagram below shows the 3D molecular structure of Erlotinib.
Side Effects include: Anemia and thrombocytopenia (low red and white blood cell counts), Diarrhea, anorexia, nausea and vomiting, Cough, Shortness of breath and Eye irritation. In addition to these, a very common side effect is pruritus, which is an intense skin rash that disperses negative effects throughout the whole body.1
Potentially serious adverse reactions to erlotinib include pulmonary toxicity (including pneumonia, interstitial lung disease and acute respiratory distress syndrome), myocardial infarction, hemorrhage and liver failure. Due to the potential for harm to the fetus, women should not become pregnant during or immediately following erlotinib treatment. Women who are already pregnant should be warned of this potential danger to the developing fetus. New mothers are advised not to nurse infants during treatment since it is possible that erlotinib can pass into breast milk. CYP3A4 inhibitors and inducers change the metabolismThe sum of all reactions in a cell or animal. Processes that lead to the creation of biomolecules such as proteins and nucleic acids are termed anabolic pathways. Processes in which biomolecules are broken down, such as the digestion of foods, are termed catabolic. Metabolism is a term that encompasses both sets of processes. of erlotinib and therefore special attention must be paid when the two treatments are administered simultaneously.1
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