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Synonyms: AC0010 | AC0010MA | avitinib (superceded INN)
Compound class: Synthetic organic
Comment: Abivertinib (AC0010) is an orally active, irreversible EGFR inhibitor that selectively targets mutated EGFRs, and was designed to overcome T790M-induced resistance in tumours . It may also inhibit BTK, thus offering extended clinical utility . We show the structure for the free base form of the compound.
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.✖
1. Ma Y, Zheng X, Zhao H, Fang W, Zhang Y, Ge J, Wang L, Wang W, Jiang J, Chuai S et al.. (2018)
First-in-Human Phase I Study of AC0010, a Mutant-Selective EGFR Inhibitor in Non-Small Cell Lung Cancer: Safety, Efficacy, and Potential Mechanism of Resistance.
J Thorac Oncol, 13 (7): 968-977. [PMID:29626621]
2. Xu X, Mao L, Xu W, Tang W, Zhang X, Xi B, Xu R, Fang X, Liu J, Fang C et al.. (2016)
AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.
Mol Cancer Ther, 15 (11): 2586-2597. [PMID:27573423]
3. Yan X, Zhou Y, Huang S, Li X, Yu M, Huang J, Wang J, Ma Z, Jin J, Pan J et al.. (2018)
Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma.
J Cancer Res Clin Oncol, 144 (4): 697-706. [PMID:29392403]