- Guide to PHARMACOLOGY
Synonyms: NSC 718781 | OSI 744 | OSI-774 | R 1415 | Tarceva®
erlotinib is an approved drug (FDA (2004), EMA (2005))
Compound class: Synthetic organic
Comment: Erlotinib is a clinically approved type-1 inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. This drug shows some selectivity for EGFR exon 19 deletion or exon 21 L858R mutations over the wild type receptor.
Subsequent studies have shown erlotinib to be a potent inhibitor of JAK2V617F activity. JAK2V617F, a mutant from of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. Study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. Specificity of inhibition with regard to other tyrosine kinase receptors remains to be fully characterized. Erlotinib is a Type-1 kinase inhibitor.
Ligand Activity Visualisation Charts
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.✖
View more information in the IUPHAR Pharmacology Education Project: erlotinib
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA (2004), EMA (2005))|
|WHO Essential Medicine||WHO Essential Medicines List (EML) (23rd List, 2023). Access PDF version.
Click to view more information about the WHO Model Lists of Essential Medicines.
|International Nonproprietary Names|
|NSC 718781 | OSI 744 | OSI-774 | R 1415 | Tarceva®|
|CAS Registry No.||183321-74-6|
|GtoPdb PubChem SID||178101619|
|RCSB PDB Ligand||AQ4|
|Search Google for chemical match using the InChIKey||AAKJLRGGTJKAMG-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||AAKJLRGGTJKAMG|
|Search PubMed clinical trials||erlotinib|
|Search PubMed titles||erlotinib|
|Search PubMed titles/abstracts||erlotinib|
81179 (in complex with epidermal growth factor receptor)
79526 (in complex with epidermal growth factor receptor)
|UniChem Compound Search for chemical match using the InChIKey||AAKJLRGGTJKAMG-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||AAKJLRGGTJKAMG-UHFFFAOYSA-N|