Selpercatinib: RET Inhibitor for Lung & Thyroid Cancer
Selpercatinib is a highly selective inhibitor of the receptor tyrosine kinase RET. It is a first-in-class targeted therapy specifically designed to treat cancers driven by genetic alterations (mutations or fusions) in the RET gene.
The drug inhibits the activity of the abnormal RET protein, effectively halting the uncontrolled proliferation of cancer cells. On Unifarm, you can find details regarding original medications (such as Retevmo/Retsevmo) containing this active ingredient.
Indications
- Non-Small Cell Lung Cancer (NSCLC): Metastatic RET fusion-positive NSCLC in adults.
- Medullary Thyroid Cancer (MTC): Advanced or metastatic RET-mutant MTC in adults and pediatric patients (12+ years) who require systemic therapy.
- Thyroid Cancer: Advanced or metastatic RET fusion-positive thyroid cancer refractory to radioactive iodine.
- Solid Tumors: Locally advanced or metastatic RET fusion-positive solid tumors (tumor-agnostic indication in some regions).
Dosage and administration
The medication is taken orally as capsules twice daily (approximately every 12 hours), with or without food. Dosing is weight-based.
Standard Regimen:
- Body weight < 50 kg: 120 mg twice daily.
- Body weight ≥ 50 kg: 160 mg twice daily.
Capsules should be swallowed whole. Dosage modifications may be required based on toxicity.
- Hypersensitivity to Selpercatinib.
- Pregnancy (can cause fetal harm).
- Breastfeeding (should be discontinued during treatment and for one week after the final dose).
- Severe hepatic impairment (requires careful dose adjustment).
Treatment requires regular monitoring of blood tests and ECG. Common adverse reactions include:
- Hepatic: Increased AST and ALT enzymes (hepatotoxicity).
- Cardiovascular: Hypertension, QT interval prolongation.
- Gastrointestinal: Dry mouth, diarrhea, constipation, nausea.
- General: Fatigue, edema, rash.
- Hematologic: Decreased leukocyte and platelet counts.
