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Updated: Jul 15, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Efficacy and Safety of RET-Specific Kinase Inhibitors in RET-Altered Cancers: A Systematic Review
Muhammad Ashar Ali1, Syed S Shah2, Rimsha Ali3
1Department of Medicine, Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts, USA.
Abstract:
RET proto-oncogene encodes receptor tyrosine kinase. Selpercatinib and pralsetinib are the only RET-specific tyrosine kinase inhibitors approved by FDA in RET-altered tumors. We searched PubMed, Embase, Cochrane, WOS, and Clinicaltrials.gov. Objective-response, complete-response, and partial-response were 60-89%, 0-11%, and 55-89%, respectively, with the use of RET-specific drugs. ≥Grade 3 adverse events were seen in 28-53% of the patients, with hypertension, change in ALT, QT prolongation, neutropenia, and pneumonitis among the common side effects. Hence, selpercatinib and pralsetinib were effective and well tolerated by most of the patients with RET-altered tumors.
Insights
Selpercatinib and pralsetinib are effective RET-specific kinase inhibitors for RET-altered tumors, showing high response rates and manageable side effects in most patients.
Area of Science:
- Oncology
- Pharmacology
Background:
- The RET proto-oncogene encodes a receptor tyrosine kinase.
- Selpercatinib and pralsetinib are FDA-approved RET-specific tyrosine kinase inhibitors (TKIs).
Conclusions:
- Selpercatinib and pralsetinib demonstrate significant efficacy in patients with RET-altered tumors.
- These RET-specific TKIs are generally well-tolerated, with a manageable safety profile.
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