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Updated: Jul 14, 2025

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Selpercatinib for adult patients with locally advanced or metastatic RET-altered solid tumors

Dat Le1, Bhavana Konda2

  • 1Department of Pharmacy, The Arthur G. James Cancer Hospital and Richard J. Solove Institute, The Ohio State University, Columbus, OH, USA.

Expert Review of Anticancer Therapy
|October 5, 2023
PubMed
Abstract

Insights

Selpercatinib effectively treats cancers with rearranged during transfection (RET) mutations, showing durable responses and a good safety profile. Ongoing trials explore its optimal use in lung and thyroid cancers.

Area of Science:

  • Oncology
  • Pharmacology
  • Cancer Genetics

Background:

  • Rearranged during transfection (RET) mutations drive cancer development.
  • Selpercatinib is a selective RET inhibitor with demonstrated anti-tumor activity.
  • Approved indications include RET fusion-positive NSCLC, medullary thyroid cancer, and other RET-altered solid tumors.

Purpose of the Study:

  • To review the pharmacology, efficacy, safety, and resistance mechanisms of selpercatinib.
  • To summarize the clinical utility of selpercatinib in RET-mutated cancers.

Main Methods:

  • Literature review of selpercatinib's pharmacology.
  • Analysis of clinical trial data on efficacy and safety.
  • Examination of resistance mechanisms.

Main Results:

  • Selpercatinib demonstrates durable anti-tumor responses.
  • The drug exhibits a favorable safety profile.
  • Promising activity is observed in various RET-altered solid tumors.

Conclusions:

  • Selpercatinib is an excellent treatment option for RET-mutated cancers.
  • Further research is evaluating optimal sequencing in first-line settings.
  • It offers a new therapeutic avenue for patients with RET-altered solid tumors.
Keywords:
Non-small-cell lung cancerRET fusionRET-mutatedselpercatinibsolid tumorsthyroid cancer

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