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• W2013674573 abstract "Two classes of epidermal growth factor receptor (EGFR) inhibitors are currently available for clinical use: tyrosine-kinase inhibitors (TKIs) and monoclonal antibodies. The introduction of pharmacological agents that are able to inhibit EGFR represents an important step in the management of patients with advanced non-small cell lung cancer (NSCLC), the leading cause of cancer death worldwide. The use of EGFR inhibitors has not only led to meaningful therapeutic gains for patients, but has also expanded our knowledge about the disease itself, as it is now recognized that activating mutations of EGFR play a pathogenetic role in NSCLC, especially in adenocarcinoma, patients who never smoked or former light smokers, females, and Asian individuals. Patients with NSCLC and one or more of these features are more likely to harbor tumors with EGFR mutations, and hence to respond to TKIs, than individuals without these features. Currently, TKIs are considered by many as the treatment of first choice in both the first- and second-line treatment of patients with clinical or molecular predictors of therapeutic benefit, and chemotherapy is a second option in these cases, especially when activating mutations of EGFR are present. Moreover, TKIs and anti- EGFR antibodies may be used in other settings, and their therapeutic role in NSCLC is clearly expanding. However, despite an initially successful treatment course, patients with advanced NSCLC eventually develop resistance to TKIs; and novel agents that hold promise for the future include irreversible EGFR inhibitors with activity against resistance-conferring EGFR mutations. Duas classes de inibidores do receptor do fator de crescimento epidérmico (EGFR) estão atualmente disponíveis para uso clínico: inibidores de tirosina-quinase (TKI) e anticorpos monoclonais. A introdução de agentes farmacológicos capazes de bloquear o EGFR representa um passo importante no manejo de pacientes com câncer de pulmão de células não pequenas (CPCNP) avançado, principal causa de morte por câncer no mundo. Além dos benefícios clínicos significativos obtidos com os inibidores de EGFR, o uso desses agentes proporcionou um maior conhecimento sobre a doença, sendo agora reconhecido que mutações ativadoras de EGFR desempenham um papel patogenético importante no CPCNP, especialmente em adenocarcinomas, indivíduos não fumantes, mulheres e asiáticos. Indivíduos com CPCNP e uma ou mais dessas características são mais propensos a apresentar tumores com mutações de EGFR e, portanto, a responder aos TKIs do que pacientes sem essas características. Atualmente, os TKIs são considerados por muitos como a estratégia terapêutica de escolha na primeira e segunda linhas de tratamento de pacientes com fatores clínicos ou moleculares preditivos de benefício terapêutico, com a quimioterapia sendo vista como a segunda opção nesses casos, especialmente na presença de mutações ativadoras de EGFR. Além disso, TKIs e anticorpos anti-EGFR podem ser usados em outras situações, e seu papel no CPCNP está em clara expansão. No entanto, apesar de um curso de tratamento inicialmente bem-sucedido, pacientes com CPCNP avançado eventualmente desenvolvem resistência aos TKIs. Novos agentes promissores incluem inibidores irreversíveis de EGFR com atividade contra formas mutantes de EGFR que conferem resistência." @default.
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• W2013674573 date "2012-03-01" @default.
• W2013674573 modified "2023-09-25" @default.
• W2013674573 title "Epidermal growth factor receptor inhibitors in non-small cell lung cancer: current status and future perspectives" @default.
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• W2013674573 doi "https://doi.org/10.1590/s0104-42302012000200025" @default.
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