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Published on: June 26, 2019
Evaluating entrectinib as a treatment option for non-small cell lung cancer
Jiyun Lee1, Sehhoon Park1, Hyun Ae Jung1
1Division of Hematology-Oncology, Department of Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine , Seoul, Korea.
Introduction:
Entrectinib, an oral pan-TRK, ALK, and ROS1 inhibitor is approved as a first-line treatment for NTRK-rearranged solid tumors and ROS1-rearranged non-small cell lung cancer (NSCLC). It has demonstrated clinical efficacy for patients harboring the relevant gene rearrangement in both systemic and intracranial disease, regardless of the tumor type.
Areas Covered:
In this review, the authors analyzed data from preclinical and clinical studies, the characteristics of entrectinib compared to those of other relevant inhibitors (currently available and/or under investigation), and the emerging resistance mechanisms. The authors then provide the readers with their future perspectives.
Expert Opinion:
Entrectinib has been well studied across many tumor types, including NSCLC with ALK, ROS1, and NTRK rearrangements. The drug has demonstrated favorable properties with oral administration, prolonged response duration, high intracranial efficacy, and a favorable toxicity profile. However, with acquisition of resistance and the development of newer generation TKIs, the optimal place for entrectinib in the landscape of targeted therapies for NSCLC warrants further validation.
Insights
Entrectinib is an effective oral targeted therapy for NTRK-rearranged solid tumors and ROS1-rearranged non-small cell lung cancer (NSCLC), showing efficacy in brain metastases. Further research is needed to define its role against emerging resistance and newer therapies.
Area of Science:
- Oncology
- Pharmacology
- Genomics
Background:
- Entrectinib is an approved oral pan-TRK, ALK, and ROS1 inhibitor.
- It is indicated for NTRK-rearranged solid tumors and ROS1-rearranged non-small cell lung cancer (NSCLC).
- Entrectinib demonstrates clinical efficacy in both systemic and central nervous system disease.
Purpose of the Study:
- To review entrectinib's efficacy and characteristics.
- To compare entrectinib with other relevant inhibitors.
- To discuss emerging resistance mechanisms and future perspectives.
Main Methods:
- Analysis of preclinical and clinical studies.
- Comparative analysis of entrectinib and other inhibitors.
- Review of resistance mechanisms and future outlook.
Main Results:
- Entrectinib shows favorable oral administration, prolonged response, and high intracranial efficacy.
- It has a favorable toxicity profile across various tumor types, including NSCLC with ALK, ROS1, and NTRK rearrangements.
- Emerging resistance mechanisms and newer generation TKIs present challenges.
Conclusions:
- Entrectinib is a well-studied targeted therapy with demonstrated benefits.
- Its optimal role in NSCLC treatment requires further validation against resistance and new therapies.
- The drug's favorable properties support its continued investigation in precision oncology.
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