Molecular and clinical features of second-generation anaplastic lymphoma kinase inhibitors: ceritinib.
Future Oncol
; 13(29): 2629-2644, 2017 Dec.
Article
en En
| MEDLINE
| ID: mdl-28891712
ABSTRACT
The discovery of ALK rearrangement in non-small-cell lung cancer (NSCLC) triggered rapid clinical development of a family of specific drugs targeting this alteration, called ALK inhibitors. Despite high rate of responses, the vast majority of patients treated with first-generation ALK inhibitor crizotinib will ultimately develop disease progression. The second-generation ALK inhibitor, ceritinib, is an oral, small-molecule that inhibits the ALK kinase activity with a potency 20-fold greater than crizotinib, being able to tackle some of the principal mechanisms of resistance to crizotinib. Evidences from five large prospective clinical trials have so far showed impressive activity of ceritinib in ALK inhibitor pretreated and naive NSCLC patients. This review will focus on the preclinical and clinical data available regarding ceritinib pharmacology, clinical efficacy and safety profile.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirimidinas
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Sulfonas
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Proteínas Tirosina Quinasas Receptoras
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Carcinoma de Pulmón de Células no Pequeñas
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Inhibidores de Proteínas Quinasas
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Neoplasias Pulmonares
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Antineoplásicos
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
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Humans
Idioma:
En
Año:
2017
Tipo del documento:
Article