.png | CAS_number = 183321-74-6 | ATC_prefix = L01 | ATC_suffix = XX34 | ATC_supplemental = | PubChem = 176870 | DrugBank = APRD00951 | chemical_formula = C₂₂H₂₃N₃O₄ | molecular_weight = 393.436 g/mol | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | pregnancy_category = | legal_status = | routes_of_administration = }} Erlotinib hydrochloride (Tarceva®, Genentech/OSIP) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer.

Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. Unlike gefitinib, erlotinib has shown a survival benefit in the treatment of lung cancer in phase III trials. It has been approved for the treatment of locally advanced or metastatic non small cell lung cancer that has failed at least one prior chemotherapy regimen. In November 2005, the FDA approved the use of erlotinib in combination with gemcitabine for treatment of locally advanced, unresectable, or metastatic pancreatic cancer.

A test for the EGFR mutation in cancer patients has been developed by Genzyme. This may predict who will respond to erlotinib and other tyrosine kinase inhibitors. It is reported that responses among patients with lung cancer are seen most often in females never-smokers, particularly asian women.

Administration

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Oral tablets

Side effects

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Common side effects include:

• Diarrhea
• Rash occurs in the majority of patients. This resembles acne and primarily involves the face and neck. It is self-limited and resolves in the majority of cases, even with continued use.
• Loss of appetite
• Fatigue
• Rarely, interstitial pneumonitis, which is characterized by cough & increased dyspnea. This may be severe and must be considered among those patients whose breathing acutely worsens.

References

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• Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305:1163-7. PMID 15284455.
• Genzyme "Genzyme Launches Exclusive Lung Cancer Test" Press Release September 27, 2005

Tyrosine kinase inhibitors | Cancer treatments

טרסבה | erlotynib