Products
Osimertinib was approved in the United States in 2015 and in the EU and Switzerland in 2016 in film-coated tablet form (Tagrisso).
Structure and properties
Osimertinib exists in the drug product as osimertinib mesilate (C28H33N7O2 – CH4O3S, Mr = 596 g/mol). It is a methylindole, aniline and pyrimidine derivative.
Effects
Osimertinib (ATC L01XE35) has antitumor and antiproliferative properties. The effects are due to selective and irreversible binding to mutant Epidermal Growth Factor Receptor (EGFR) variants. In contrast, EGFR wild-type is not inhibited. Osimertinib is also effective against EGFR with the T790M mutation. This mutation is commonly seen in treatment resistance and advanced lung cancer. In this case, a threonine at position 790 is replaced by a methionine. Osimertinib has a long half-life of 48 hours.
Indications
For the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with the EGFR T790M mutation who have experienced disease progression during or after EGFR TKI therapy.
Dosage
According to the SmPC. Tablets are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Concurrent use of St. John’s wort
Full precautions can be found in the drug label.
Interactions
Osimertinib is a substrate of CYP3A, P-glycoprotein, and BCRP, and corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include diarrhea, skin rash, dry skin, and nail toxicity.
