Selpercatinib, sold under the brand name Retevmo among others, is a targeted medication for the treatment of cancers in people whose tumors have an alteration (mutation or fusion) in a specific gene (RET which is short for "rearranged during transfection"). Before beginning treatment, the identification of a RET gene alteration must be determined using laboratory testing. Selpercatinib is taken by mouth. The most common side effects include changes in laboratory tests (including increased liver enzymes, increased blood sugar, decreased white cell and platelet counts, decreased protein level, decreased calcium, increased total cholesterol, increased creatinine, and decreased sodium) dry mouth, diarrhea, high blood pressure, fatigue, edema, rash, and constipation. Selpercatinib is a RET kinase inhibitor, meaning it inhibits the protein RET receptor kinase, which is mutated in the cancer cells and provides them with growth signals. Blocking the RET kinase blocks the main growth signal for cancer cells and thereby prevents them from dividing. Selpercatinib is the first therapy approved specifically for people with cancer harboring RET gene alterations. Selpercatinib received accelerated approval for this indication for patients aged twelve years of age and older in 2020. In June 2024, the US Food and Drug Administration granted traditional approval to selpercatinib for people aged two years of age and older.
Medical uses In the United States, selpercatinib is indicated for the treatment of:
adults with locally advanced or metastatic non-small cell lung cancer with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test. people aged twelve years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved test, who require systemic therapy. people aged twelve years of age and older with advanced or metastatic thyroid cancer with a RET gene fusion, as detected by an FDA-approved test, who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate). adults with locally advanced or metastatic solid tumors with a rearranged during transfection (RET) gene fusion that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options. In the European Union, selpercatinib, as monotherapy, is indicated for the treatment of adults with:
advanced RET fusion-positive non-small cell lung cancer who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy advanced RET fusion-positive thyroid cancer who require systemic therapy following prior treatment with sorafenib and/or lenvatinib and for the treatment of people aged twelve years of age and older with advanced RET-mutant medullary thyroid cancer (MTC) who require systemic therapy following prior treatment with cabozantinib and/or vandetanib. In September 2024, the FDA granted traditional approval to selpercatinib for people aged two years of age and older with advanced or metastatic medullary thyroid cancer with a RET mutation, as detected by an FDA-approved test, who require systemic therapy. Selpercatinib received accelerated approval for this indication for people 12 years of age and older in 2020. In May 2024, the FDA granted accelerated approval for this indication to people aged two years of age and older.
Adverse effects Selpercatinib can cause serious side effects including liver toxicity, high blood pressure, heart rhythm changes due to prolongation of heart electrical activity (QT prolongation), bleeding, allergic reactions and impaired wound healing. Selpercatinib may also cause harm to a developing fetus or a newborn baby. The most common adverse reactions (≥25%) were edema, diarrhea, fatigue, dry mouth, hypertension, abdominal pain, constipation, rash, nausea, and headache. The most common Grade 3 or 4 laboratory abnormalities (≥5%) were decreased lymphocytes, increased alanine aminotransferase (ALT), increased aspartate aminotransferase (AST), decreased sodium, and decreased calcium.
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