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Sunvozertinib, also known as DZD9008, is an oral, potent, irreversible, and selective EGFR tyrosine kinase inhibitor. Sunvozertinib shows activity against EGFRexon20ins and other mutations. In both cell lines and xenograft models, sunvozertinib shows potent antitumor activity. In the two ongoing phase I clinical studies, sunvozertinib was tolerated up to 400 mg once daily.

Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52)[1].

EGFR exon 20 insertion: 20.4 nM (IC₅₀); EGFR^L858R/T790M: 1.1 nM (IC₅₀); Her2 Exon20 YVMA: 7.5 nM (IC₅₀)

[1] Zhengtao LI, et al. Erbb/btk inhibitors. WO2019149164A1.