Synonyms: ARRY-380 | Example 11 [WO2007059257A2] | ONT-380 | Tukysa®
tucatinib is an approved drug (FDA (2020), EMA (2021))
Compound class:
Synthetic organic
Comment: Tucatinib is an orally bioavailable ERBB2 (HER2) receptor tyrosine kinase inhibitor that was developed as a novel antineoplastic agent by Seattle Genetics [2]. The chemical structure is claimed as Example 11 in Array Biopharma patent WO2007059257A2 [3], and was exemplified as ARRY-380 in the later patent WO2013056183A1 [1]. Tucatinib contains a quinazoline core that is conserved in other tyrosine kinase inhibitors including lapatinib, erlotinib, and gefitinib [2].
The INN tucatinib replaced the earlier INN irbinitinib that was associated with this chemical entity. ![]() Ligand Activity Visualisation ChartsThese 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. ✖ |
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Bioactivity Comments |
Lapatinib and neratinib do not exhibit the selectivity for ERBB2 compared to EGFR that tucatinib does [2]. In a biochemical screen of 223 kinases, tucatinib showed selectivity within the EGFR kinase family, and inhibition of other kinases was minimal. Tucatinib inhibits HER2 signalling activity in BT-474 HER2-driven breast cancer cells (receptor phosphorylation; IC50 7 nM) and proliferation of these cells (IC50 33 nM), These effects were less potent in EGFR-driven A431 cells. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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