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Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
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Molecular and clinical features of second-generation anaplastic lymphoma kinase inhibitors: ceritinib

Tommaso De Pas1, Laura Pala1, Chiara Catania2

  • 1Medical Oncology of Melanoma & Sarcoma Unit, European Institute of Oncology, Via Ripamonti, 435, 20141 Milan, Italy.

Future Oncology (London, England)
|September 12, 2017
PubMed

Insights

Ceritinib, a potent second-generation ALK inhibitor, shows significant efficacy in non-small-cell lung cancer (NSCLC) patients, overcoming resistance to earlier treatments like crizotinib.

Area of Science:

  • Oncology
  • Pharmacology

Background:

  • Anaplastic Lymphoma Kinase (ALK) rearrangements drive non-small-cell lung cancer (NSCLC) growth.
  • First-generation ALK inhibitors like crizotinib achieve initial responses but often face resistance, leading to disease progression.
  • Novel therapeutic strategies are crucial for managing ALK-rearranged NSCLC.

Purpose of the Study:

  • To review the preclinical and clinical data of ceritinib, a second-generation ALK inhibitor.
  • To evaluate ceritinib's pharmacology, clinical efficacy, and safety profile in NSCLC patients.
  • To understand ceritinib's role in overcoming resistance mechanisms to first-generation ALK inhibitors.

Main Methods:

  • Review of preclinical studies investigating ceritinib's mechanism of action and potency.
  • Analysis of data from five prospective clinical trials involving ceritinib in NSCLC.
  • Assessment of ceritinib's safety and tolerability in diverse patient populations.

Main Results:

  • Ceritinib demonstrates significantly higher potency compared to crizotinib.
  • Ceritinib effectively targets key resistance mechanisms developed against crizotinib.
  • Clinical trials show impressive response rates and activity in both treatment-naive and previously treated NSCLC patients.

Conclusions:

  • Ceritinib represents a promising therapeutic option for ALK-rearranged NSCLC.
  • Its enhanced potency and ability to overcome resistance offer improved outcomes for patients.
  • Further investigation into ceritinib's long-term efficacy and safety is warranted.
Keywords:
ALKNSCLCceritinibresistance mechanismstargeted therapy

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