Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selectiveEGFRinhibitor, withK_iandK_inactof 31 nM and 0.222 min^–1on EGFR(L858R/790M) mutant, respectively.

Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC₅₀s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties^[1]. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC₅₀values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC₅₀values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC₅₀(compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively^[2].

In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg)^[1]. In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, –61% and –80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations^[2].

591.12

C₂₇H₃₅ClN₆O₅S

1508250-72-3

那扎替尼甲磺酸盐

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