Pralsetinib is a potent and selective RET kinase inhibitor used primarily in the treatment of cancers driven by RET gene alterations. It is indicated for patients with non-small cell lung cancer (NSCLC) and thyroid cancers that have specific RET fusions or mutations, particularly in cases where the disease is metastatic or advanced. Due to its high selectivity, it shows strong efficacy in tumor response and durable progression-free survival, even in patients who have progressed on prior therapies, including other RET inhibitors. Pralsetinib is also active against central nervous system metastases, making it valuable in managing brain involvement in RET-altered cancers. Its oral bioavailability allows for convenient outpatient treatment, and it is increasingly used as a first-line option in RET-positive cancers based on clinical trial outcomes showing improved response rates and tolerability compared to chemotherapy or multi-kinase inhibitors.