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Updated: Dec 19, 2025

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Abstract:
The FDA has greenlighted selpercatinib, the first targeted therapy for RET-altered non-small cell lung cancer (NSCLC) and certain types of thyroid cancer. Another RET inhibitor, pralsetinib, has been submitted for approval to treat NSCLC. Both drugs have shown effectiveness in treating brain metastases.
Insights
The FDA approved selpercatinib, a targeted therapy for RET-altered non-small cell lung cancer (NSCLC) and thyroid cancer. Pralsetinib, another RET inhibitor, is also under review, showing promise for brain metastases in NSCLC.
Area of Science:
- Oncology
- Pharmacology
- Genetics
Background:
- Non-small cell lung cancer (NSCLC) and thyroid cancer can harbor RET alterations.
- Targeted therapies offer new treatment avenues for cancers with specific genetic mutations.
Purpose of the Study:
- To report the FDA approval of selpercatinib for RET-altered NSCLC and thyroid cancer.
- To highlight the development and potential of pralsetinib, another RET inhibitor, for NSCLC treatment.
Main Methods:
- Review of clinical trial data and regulatory submissions for selpercatinib and pralsetinib.
- Analysis of drug efficacy, particularly in patients with brain metastases.
Main Results:
- Selpercatinib received FDA approval as the first targeted therapy for RET-altered NSCLC and certain thyroid cancers.
- Pralsetinib has been submitted for approval and demonstrated effectiveness in treating brain metastases in NSCLC patients.
Conclusions:
- Targeted inhibition of RET alterations represents a significant advancement in treating specific NSCLC and thyroid cancers.
- Both selpercatinib and pralsetinib show promise, offering new hope for patients, including those with brain metastases.
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