Molecular and clinical features of second-generation anaplastic lymphoma kinase inhibitors: Ceritinib

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3 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)2629-2644
Number of pages16
JournalFuture Oncology
Volume13
Issue number29
DOIs
Publication statusPublished - Dec 1 2017

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Non-Small Cell Lung Carcinoma
Drug Delivery Systems
Disease Progression
Phosphotransferases
Clinical Trials
Pharmacology
Safety
anaplastic lymphoma kinase
ceritinib
crizotinib

Keywords

  • ALK
  • ceritinib
  • NSCLC
  • resistance mechanisms
  • targeted therapy

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

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