Erlotinib

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Information about Erlotinib

Erlotinib is a tyrosine kinase receptor inhibitor that is used in the therapy of advanced or metastatic pancreatic or non-small cell lung cancer.  

Liver safety of Erlotinib

Erlotinib therapy is associated with transient elevations in serum aminotransferase levels during therapy and rare instances of clinically apparent acute liver injury.

Mechanism of action of Erlotinib

Erlotinib (er loe' ti nib) is a selective inhibitor of several tyrosine kinase receptors which are associated with tumor growth and angiogenesis.  The tyrosine kinase receptors are often mutated and over expressed in tumor tissue and cause unregulated cell growth and proliferation.  Erlotinib is one of several tyrosine kinase inhibitors that have been introduced into cancer chemotherapy and are specially directed at molecular abnormalities that occur in cancer cells.  Inhibition of the receptor can lead to reversal of progression of the cancer, although clinical responses are sometimes limited by the development of tumor resistance caused by further mutations in the receptor gene. 

FDA approval information for Erlotinib

Erlotinib has special activity against the human epidermal growth factor (EGF) tyrosine kinase receptors HER-1 and EGFR which are found in several forms of cancer.  Erlotinib received approval for use in the United States in 2004. 

Clinical use of Erlotinib

Current indications are for locally advanced, unresectable or metastatic pancreatic cancer in combination with gemcitabine and for locally advanced or metastatic non-small-cell lung cancer as a first line treatment in patients with specific, erlotinib sensitive mutations in EGFR or after failure of at least one chemotherapy regimen. 

Dosage and administration for Erlotinib

Erlotinib is available in tablets of 25, 100 and 150 mg under the brand name Tarceva, and the typical dose is either 100 mg (pancreatic cancer) or 150 mg (lung cancer) once daily by mouth, continued until disease progresses or intolerable toxicity occurs. 

Side effects of Erlotinib

Side effects include fatigue, rash, diarrhea, anorexia, skin discoloration, hand-foot syndrome, edema, muscle cramps, arthralgias, headache, abdominal discomfort, anemia, cough, and pruritus.  Uncommon, but potentially severe side effects include heart failure, interstitial lung disease, gastrointestinal perforation, pancreatitis, renal failure, severe skin reactions and embryo-fetal toxicity.   

 


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