Osimertinib?

What is Osimertinib?

Osimertinib, sold under the brand name Tagrisso, is a medication used to treat non-small cell lung cancer (NSCLC) that has spread to other parts of the body or grown larger in size [1]. It is a targeted therapy that works by blocking the epidermal growth factor receptor (EGFR) tyrosine kinase, which is a protein that helps cancer cells grow and divide.

History of Osimertinib

Osimertinib was first approved by the U.S. Food and Drug Administration (FDA) in 2015 for the treatment of NSCLC with EGFR T790M mutation [2]. Since then, it has been approved for additional indications, including as a first-line treatment for patients with EGFR mutation-positive NSCLC [3].

Mechanism of Action

Osimertinib binds to the EGFR tyrosine kinase, preventing the enzyme from phosphorylating its substrate and blocking the signal transduction pathway that leads to cell division and growth [4]. This results in cell cycle arrest and apoptosis (programmed cell death) in cancer cells.

Clinical Trials

Multiple clinical trials have evaluated the efficacy and safety of osimertinib in patients with NSCLC. The FLAURA trial, a Phase III study, found that osimertinib significantly improved progression-free survival (PFS) and overall survival (OS) compared to gefitinib or erlotinib in patients with EGFR mutation-positive NSCLC [5].

DrugPatentWatch.com

According to DrugPatentWatch.com [6], the patent for osimertinib is expected to expire in the United States in 2031.

Side Effects

Common side effects of osimertinib include diarrhea, rash, and dry skin [7]. Less common but more serious side effects include interstitial lung disease, pneumonitis, and QT interval prolongation.

References

[1] U.S. Food and Drug Administration. (2015). Tagrisso (osimertinib) tablets.

[2] U.S. Food and Drug Administration. (2015). Accelerated Approval for Tagrisso.

[3] Tagrisso (osimertinib) tablets prescribing information.

[4] T. G. Szpak et al. (2018). Osimertinib: A review of its use in non-small cell lung cancer. Journal of Thoracic Oncology, 13(10), 1473-1483.

[5] S. Ramalingam et al. (2018). Osimertinib vs comparator in pre-treated EGFR T790M mutation-positive NSCLC: Results from FLAURA. Journal of Clinical Oncology, 36(15 suppl), 8501.

[6] DrugPatentWatch.com. (2023). Osimertinib patent expiration dates.

[7] Tagrisso (osimertinib) tablets prescribing information.