Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selectiveEGFRinhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.

Targets

mutant EGFR 0.031 μM(Ki)

In vitro

EGF816 is a novel, covalent, mutant-selective EGFR inhibitor with nearly equipotent activity on both oncogenic (L858R and ex19del) and T790M-resistant mutations and good selectivity over WT EGFR. EGF816 potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro. The cellular activity of EGF816 on EGFR mutants are assessed using three well-characterized cell lines, H3255, HCC827, and H1975, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively. After incubation with cells for 3 hours, EGF816 shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 values of 5, 1, and 3 nmol/L, respectively. Cellular-based assays shows that EGF816 is selective toward mutant over WT EGFR.

In vivo

EGF816 is well tolerated and possesses favorable physicochemical properties and good oral bioavailability in mice. It shows moderate volume of distribution and low to moderate clearance in rodents (30% and 35% of rat and mouse liver blood flow, respectively). In the dog, EGF816 shows high clearance and high volume of distribution. EGF816 also demonstrates antitumor activity in an exon 20 insertion mutant model. At levels above efficacious doses, EGF816 treatment leads to minimal inhibition of WT EGFR and is well tolerated. In single-dose studies, EGF816 provides sustained inhibition of EGFR phosphorylation, consistent with its ability for irreversible binding. EGF816 has a longer half-life in human than mouse and is currently being evaluated in phase I/II clinical trials in patients harboring EGFR mutations, including T790M.

Cell Research(from reference)

Cell lines：H1975, H3255, HCC827, A431, and HaCaT cells

Incubation Time：3 h

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