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Ligand id: 7719
View more information in the IUPHAR Pharmacology Education Project: osimertinib
Molecular properties generated using the CDK
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA (2015), EMA (2016))|
|International Nonproprietary Names|
|AZD 9291 | AZD-9291 | AZD9291 | mereletinib (obsolete INN) | Tagrisso®|
|Osimertinib (AZD9291) is a third-generation, potent, selective and irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase bearing mutations which either sensitise the receptor, or cause drug resistance (eg the T790M mutation) . The compound is less effective against the wild-type receptor.
This compound is included in AstaZeneca's Open Innovation Pharmacology Toolbox. There are reports of acquired resistance to osimertinib with tumours developing the C797S [5,8] and L718Q mutations  .
Third-generation mutant EGFR inhibitors are being developed to circumvent dose-limiting WT EGFR-driven toxicities such as gastrointestinal toxicity and rash. The progress being made in developing advanced generation EGFR inhibitors is discussed by Yu and Riely (2013)  and Ou and Soo (2015) .
|CAS Registry No.||1421373-65-0|
|GtoPdb PubChem SID||223366052|
|RCSB PDB Ligand||YY3|
|Search Google for chemical match using the InChIKey||DUYJMQONPNNFPI-UHFFFAOYSA-N|
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