Synonyms: alflutinib (pseudo INN) | ASK120067 | AST-2818 | AST2818 | example 3 [US10072002B2] | furmonertinib | Ivesa®
firmonertinib is an approved drug (China (2021))
Compound class:
Synthetic organic
Comment: Firmonertinib (AST2818; formerly furmonertinib) is a receptor tyrosine kinase inhibitor that targets mutant forms of the EGFR more effectively than the wild type receptor kinase, with notable potency vs. the T790M resistance mutation. Firmonertinib is the formal WHO INN. It has an irreversible binding mode. AST2818's chemical structure is claimed as example 3 in Shanghai Allist Pharmaceuticals' patent US10072002B2 [2]. Note that AST2818 is administered clinically as the mesylate.
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Bioactivity Comments | ||||||||||||
Patent US10072002B2 does not provide IC50 or Ki values for the direct inhibition of specific kinases [2]. It reports the in vitro antiproliferative effects on cells lines that express different EGFR mutants or wild type EGFR. Results from these assays indicate that AST2818 potently inhibits growth of cell lines with activating or resistance mutations but only weakly inhibits growth of cells expressing wild type EGFR. AST2818 significantly reduces tumour volume in a xenograft model of human lung cancer H1975 cell tumours in nude mice. In vitro antiproliferative activity of AST2818 from US10072002B2 is tabulated below:
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Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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