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How to use Selpercatinib(Retevmo)?
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Article source: Seagull Pharmacy
Jun 30, 2025

Selpercatinib is not only effective in the treatment of RET fusion-positive non-small cell lung disease and thyroid disease, but also explores the therapeutic potential of other RET gene fusion solid tumors. Its wide range of application prospects brings more choices to patients. So, how is Selpercatinib used for Selpercatinib(Retevmo)?

How to use Selpercatinib(Retevmo)?

Selpercatinib is an oral, highly selective RET kinase inhibitor, and according to the label, the following is an introduction to how to use Selpercatinib:

Dosage and frequency of medication

The dose of Selpercatinib is determined based on the patient's weight. For patients weighing less than 50 kg, the recommended dose is 120 mg each time; For patients weighing 50 kg and above, the recommended dose is 160 mg each time. Oral administration is required twice daily, approximately every 12 hours, until disease progression or unacceptable toxicity occurs.

Medication method

Selpercatinib should be swallowed whole in the form of a capsule and the capsule shell should not be crushed or chewed. Do not miss any dose unless it takes more than 6 hours to miss the next scheduled dose. If vomiting occurs after taking the medicine, it should not be retaken, and the next dose should still be carried out at the original interval.

Selpercatinib is a potent RET kinase inhibitor, and special attention needs to be paid to dose adjustment, adverse reaction monitoring, and interactions with other drugs during use. Patients should be treated individually under the guidance of a physician and followed up regularly to assess the effectiveness of treatment.

Pharmacokinetics of Selpercatinib(Retevmo)

Selpercatinib is a novel small molecule inhibitor of RET kinase. The following is a detailed elaboration of its pharmacokinetics:

Absorption

Selpercatinib can be quickly absorbed by the body after oral administration. In clinical trials, patients take Selpercatinib orally and typically reach peak plasma drug concentrations within a short period of time. This feature allows Selpercatinib to act rapidly and exert an inhibitory effect on RET kinase.

Distribution

Selpercatinib is widely distributed in the body and can penetrate into a variety of tissues and organs. The drug has a high protein binding rate in plasma, which helps to prolong its half-life in the body, thereby increasing the efficacy of the drug. Selpercatinib can also cross the blood-brain barrier and inhibit RET kinases in the central nervous system, which is of great significance for the treatment of patients with brain metastases.

Selpercatinib has unique pharmacokinetic profiles that allow Selpercatinib to maintain effective drug concentrations in vivo and thus exert a sustained therapeutic effect.

Note: For internal discussion among medical personnel only. For specific medication, please consult the attending physician. Drug information may change over time. For the latest information, we recommend adding a medical consultant or consulting for free online.
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