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Ligand id: 7719
View more information in the IUPHAR Pharmacology Education Project: osimertinib
Molecular properties generated using the CDK
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|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|
|Search Google for chemicals with the same backbone||DUYJMQONPNNFPI|
|Search PubMed clinical trials||osimertinib|
|Search PubMed titles||osimertinib|
|Search PubMed titles/abstracts||osimertinib|
|Search UniChem for chemical match using the InChIKey||DUYJMQONPNNFPI-UHFFFAOYSA-N|
|Search UniChem for chemicals with the same backbone||DUYJMQONPNNFPI|