BioCentury

Benzoxaborole-based CPSF3 inhibitor to treat infections

December 19, 2019 9:47 PM UTC

INDICATION: Cryptosporidium

Inhibiting the Cryptosporidium CPSF3 homolog with AN3661 could treat infections by the parasite, which can be lethal in young children and immunocompromised individuals. Anacor Pharmaceuticals Inc., which Pfizer Inc. (NYSE:PFE) acquired in 2016, had been developing the benzoxaborole-based compound as an antimalarial. In cultured human ileocecal cells, AN3661 inhibited C. parvum growth with a lower EC50 than the marketed anti-Cryptosporidium drug Alinia nitazoxanide (0.08 μM vs. 2.55 μM, respectively). In infected neonatal mice, a single dose of the compound reduced ileal parasite loads by up to 80%. AN3661 reduced parasite loads by up to 55% and 87% in two immunocompromised adult mouse models of infection. Next steps include testing AN3661 in larger animal models...