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Selpercatinib

Cytotoxic Chemotherapy Prescription
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Indications

Cancer

Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer Selpercatinib is used to treat adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC). This use was approved under accelerated approval, based on overall response rate and duration of response. Continued approval may depend on confirmatory trials verifying and describing the clinical benefit. RET-Mutant Medullary Thyroid Cancer Selpercatinib is used to treat adults and children aged 12 years and older who have advanced or metastatic RET-mutant medullary thyroid cancer (MTC) and need systemic therapy. This use was also approved under accelerated approval, based on overall response rate and duration of response. Continued approval may depend on confirmatory trials verifying and describing the clinical benefit. RET Fusion-Positive Thyroid Cancer Selpercatinib is used to treat adults and children aged 12 years and older who have advanced or metastatic RET fusion-positive thyroid cancer, need systemic therapy, and are radioactive iodine-refractory (if radioactive iodine is appropriate). Again, this use was approved under accelerated approval, based on overall response rate and duration of response. Continued approval may depend on confirmatory trials verifying and describing the clinical benefit.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Selpercatinib is a kinase inhibitor. In enzyme assays it blocked wild-type RET and several mutated RET isoforms, and also VEGFR1 and VEGFR3, with IC50 values from 0.92 nM to 67.8 nM. It also blocked FGFR 1, 2, and 3 in other enzyme assays, but only at higher concentrations, which are still clinically achievable. In cellular assays, Selpercatinib inhibited RET at approximately 60-fold lower concentrations than FGFR1 and 2, and at approximately 8-fold lower concentration than VEGFR3.

Pregnancy & Breastfeeding

Selpercatinib can cause fetal harm when given to a pregnant woman. This is based on findings from animal studies and on how the medicine works. There are no data on selpercatinib use in pregnant women, so the exact risk to the fetus isn't known. When pregnant rats were given selpercatinib during organogenesis, it caused embryolethality and malformations, at maternal exposures roughly equal to the human exposure at the clinical dose of 160 mg twice daily. Pregnant women should be told about the potential risk to the fetus.

Lactation: There are no data on whether selpercatinib or its metabolites pass into human milk, or what they do to the breastfed child or to milk production. Because breastfed children could have serious adverse reactions, women should be advised not to breastfeed during treatment with selpercatinib and for 1 week after the final dose.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: The recommended dose of Selpercatinib depends on body weight. People who weigh less than 50 kg take 120 mg, and people who weigh 50 kg or more take 160 mg. Take it by mouth twice daily, about every 12 hours, until the disease gets worse or the side effects become unacceptable. Swallow the capsules whole. Don't crush or chew them. If you miss a dose, don't take it unless the next scheduled dose is more than 6 hours away. If you vomit after taking Selpercatinib, don't take an extra dose. Just take the next dose at the usual time. Dosage Modifications for Concomitant Use of Acid-Reducing Agents Try to avoid using a PPI, a histamine-2 (H2) receptor antagonist or a locally-acting antacid together with Selpercatinib. If you can't avoid using them together, take Selpercatinib with food when it is given with a PPI. When it is given with an H2 receptor antagonist, take Selpercatinib 2 hours before or 10 hours after the H2 receptor antagonist. With a locally-acting antacid, take Selpercatinib 2 hours before or 2 hours after the antacid.