What is Selpercatinib (Retevmo)?

What is Selpercatinib (Retevmo)?

Selpercatinib (generic name: selpercatinib) is a targeted therapy drug that can be used at home. It is the first FDA-approved drug for the treatment of RET-positive advanced non-small cell lung cancer, thyroid cancer, and certain other cancers. Unlike traditional chemotherapy, selpercatinib precisely targets cancer cells driven by abnormal RET genes. However, while acting on tumor cells, selpercatinib may also affect healthy cells, causing side effects, some of which can be severe. Before using this drug, doctors will perform testing to confirm whether a patient's tumor is RET-positive.

The relationship between the RET gene and cancer

The RET gene is a normal gene present in everyone's body, but in certain cancers, the RET gene undergoes changes (i.e., rearrangements or mutations) that become key drivers of tumor growth. If testing reveals an abnormality in the RET gene, it is called "RET-positive." RET positivity is commonly found in non-small cell lung cancer, medullary thyroid cancer, and other types of advanced solid tumors. Knowing whether a tumor is RET-positive helps doctors select the most appropriate targeted therapy. Biomarker testing can identify these relatively rare genetic alterations, opening the door to personalized treatment for patients.

How does Selpercatinib (Retevmo) work?

Selpercatinib is a selective RET inhibitor that works by blocking the activity of abnormal RET proteins, thereby inhibiting the growth and spread of cancer cells. In clinical trials, selpercatinib has demonstrated significant anti-tumor activity, shrinking tumors in the majority of RET-positive patients, with some achieving complete remission. Because this drug is an oral formulation, patients can take it at home without hospitalization, greatly improving treatment convenience and quality of life. However, regular monitoring of liver and kidney function, blood pressure, and electrocardiogram is required during treatment to ensure medication safety.