INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves "artemisinin-like" kill kinetics in vitro with a parasite clearance time of <24 h. INE963 is also potent against P. falciparum and P. vivax clinical isolates from Brazil and Uganda with EC50’s ranging from 0.01 to 7.0 nM

Pf3D7:6 nM(EC50)

INE963 is active against >15 drug-resistant Pf cell lines with EC50’s = 0.5–15 nM. The in vitro log parasite reduction ratio for INE963 is >8.0 at 10 × Pf 3D7 EC50 without a lag phase and a parasite clearance time (PCT99.9) of <24 h. The in vitro selectivity of INE963for Plasmodium vs human cells was exemplified by approximately 1000+ fold shifts against multiple human kinase biochemical assays[1].

Following four oral doses at 30 mg/kg of INE963, the frontrunner compounds tested showed significant parasitemia reduction (>99.9%) at day 5 compared to untreated control mice. In addition, the animals did not show any signs of recrudescence of parasite at day 60 post-treatment, indicating complete cure at these doses[1].