Selpercatinib

What it is and how it works

Selpercatinib is a highly selective inhibitor of the RET receptor tyrosine kinase, including wild-type RET, RET fusions and activating RET mutations. It inhibits RET-driven proliferation of tumour cells.

Indications

Advanced RET fusion-positive non-small cell lung cancer, RET fusion-positive thyroid cancer and RET-mutant medullary thyroid cancer, and other RET fusion-positive solid tumours, according to licence.

Dosage and administration (summary)

Taken orally twice daily; usually 160 mg twice daily in patients weighing 50 kg or more and 120 mg twice daily if under 50 kg, with dose reductions for toxicity.

Contraindications

Hypersensitivity to selpercatinib.

Warnings and precautions

Hepatotoxicity (raised transaminases), hypertension, QT prolongation, haemorrhage, hypersensitivity, impaired wound healing, tumour lysis syndrome and hypothyroidism may occur; monitor liver function, blood pressure, ECG and electrolytes. Avoid strong CYP3A4 inhibitors and inducers, and proton pump inhibitors require it to be taken with food.

Pregnancy

Should not be used in pregnancy because of potential fetal harm; effective contraception is required.

Storage and supply

Store below 30 °C.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.