Osimertinib

What it is and how it works

Osimertinib irreversibly inhibits epidermal growth factor receptors carrying sensitising mutations (exon 19 deletion, exon 21 L858R) and the T790M resistance mutation, with relative sparing of wild-type EGFR; it has good central nervous system penetration.

Indications

EGFR mutation-positive non-small cell lung cancer: adjuvant treatment after complete resection, first-line treatment of locally advanced or metastatic disease (alone or with chemotherapy), after chemoradiation in unresectable stage III disease, and T790M-positive disease after progression on EGFR TKI therapy.

Dosage and administration (summary)

Oral: 80 mg once daily, with or without food, until disease progression or unacceptable toxicity (adjuvant use for up to 3 years).

Contraindications

Hypersensitivity; concomitant use with St John’s wort.

Warnings and precautions

Interstitial lung disease or pneumonitis may occur; interrupt treatment if suspected and discontinue if confirmed. QTc prolongation, reduced left ventricular ejection fraction, keratitis and severe skin reactions have been reported; monitor ECG and electrolytes in at-risk patients. Strong CYP3A4 inducers should be avoided as they reduce exposure.

Pregnancy

Avoid; it may cause fetal harm, and effective contraception is required during and after treatment.

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.