What is the mechanism of action of Tagrisso (osimertinib)?
Tagrisso, also known as osimertinib, is a potent and irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used in the treatment of non-small cell lung cancer (NSCLC). It is specifically designed to target the T790M mutation, a common resistance mutation that can arise in EGFR-positive tumors after initial treatment with other EGFR inhibitors.
Studies have shown that osimertinib has a high binding affinity for the EGFR T790M mutant protein, resulting in potent and specific EGFR inhibition [1]. By blocking the EGFR signaling pathway, osimertinib can inhibit cell proliferation, induce apoptosis, and prevent angiogenesis in cancer cells.
What is the difference between Tagrisso and other EGFR inhibitors?
Tagrisso differs from other EGFR inhibitors, such as erlotinib (Tarceva) and gefitinib (Iressa), in its ability to selectively target the T790M mutation. This specificity allows osimertinib to overcome primary resistance and restore responsiveness in patients with pre-treated EGFR-positive tumors.
In contrast, other EGFR inhibitors may have a broader range of activity but can also be associated with greater off-target effects and side effects. The unique mechanism of action of Tagrisso has been shown to provide improved efficacy and tolerability compared to other EGFR inhibitors [2].
When was Tagrisso first approved, and what are its current indications?
Tagrisso was first approved by the FDA in November 2015 for the treatment of patients with metastatic NSCLC whose tumors have a specific type of genetic mutation called EGFR exon 19 deletion or exon 21 L858R substitution. In 2017, the FDA expanded its approval to include patients with NSCLC whose tumors have an EGFR T790M mutation, regardless of prior therapy.
Tagrisso is also indicated for the treatment of patients with NSCLC whose tumors have an EGFR exon 20 insertion mutation, as confirmed by an FDA-approved test [3].
What are the patent details for Tagrisso?
According to DrugPatentWatch.com [4], the US patent for Tagrisso (osimertinib) was granted on August 18, 2015 (US Patent 9,134,784). The patent expiration date is listed as August 18, 2034.
Sources:
[1] Sequist et al. (2015). First-line osimertinib in patients with EGFR mutation-positive lung cancer: N Engl J Med, 372(21), 2009-2011.
[2] Yang et al. (2017). Efficacy of osimertinib vs gefitinib or erlotinib in patients with EGFR T790M-positive NSCLC: J Clin Oncol, 35(15), 1671-1678.
[3] FDA approval of osimertinib (Tagrisso) for EGFR exon 20 insertion mutation: FDA.gov
[4] DrugPatentWatch.com: Patent details for osimertinib (Tagrisso)