|Trade names||Tagrisso, Tagrix|
|Protein binding||Probably high|
|Biological half-life||48 hours|
|Excretion||Feces (68%), urine (14%)|
|Chemical and physical data|
|Molar mass||499.62 g·mol−1|
|3D model (Jmol)||Interactive image|
Osimertinib (previously known as mereletinib or AZD9291; trade name Tagrisso) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug developed by AstraZeneca Pharmaceuticals – for mutated EGFR cancers.
Approvals and indications
In November 2015, after a Priority Review, the US FDA granted accelerated approval to osimertinib for the treatment of metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA-approved test, which has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.
The FDA approval made reference to two clinical trials, in which an EGFR T790M mutation was confirmed by a Cobas EGFR mutation test; osimertinib was given as 80 mg once daily.
- "Tagrisso (osimertinib) Tablet, for Oral Use. Full Prescribing Information" (PDF). AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850. Retrieved 16 November 2015.
- "Proposed INN: List 113" (PDF). International Nonproprietary Names for Pharmaceutical Substances (INN). 29 (2): 285. 2015. Retrieved 16 November 2015.
- Ayeni D, Politi K, Goldberg SB (2015). "Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer". Clin. Cancer Res. 21 (17): 3818–20. doi:10.1158/1078-0432.CCR-15-1211. PMID 26169963.
- Tan CS, Gilligan D, Pacey S (2015). "Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer". Lancet Oncol. 16 (9): e447–59. doi:10.1016/S1470-2045(15)00246-6. PMID 26370354.
- U.S. Food and Drug Administration. Hematology/Oncology (Cancer) Approvals & Safety Notifications.
- Xu M, Xie Y, Ni S, Liu H (2015). "The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC)". Ann Transl Med. 3 (7): 96. doi:10.3978/j.issn.2305-5839.2015.03.60. PMC 4430733. PMID 26015938.
- U.S. Food and Drug Administration. "Osimertinib".
- Tagrisso (osimertinib) approved in EU as first-in-class treatment for patients with EGFR T790M mutation-positive metastatic non-small cell lung cancer
- First-Line Osimertinib Yields Nearly 80% Response in Advanced Lung Cancer. April 2016