oral CPSF3 inhibitor for Chagas
uniformly curative in naturally infected rhesus macaques
from benzoxaborole library screen and opt.
Nat. Microbiol.
Anacor Pharmaceuticals, Palo Alto, CA
Context. AN15368 (Anacor Pharmaceuticals) is an oral Cleavage And Polyadenylation Specificity Factor (CPSF3) inhibitor being developed for Chagas disease, also known as American trypanosomiasis. Chagas disease is caused by Trypanosoma cruzi and is estimated to affect 6-7 million people worldwide, primarily those living in Latin America. The significant unmet need for additional Chagas disease treatments is underscored by the fact that the two currently FDA-approved therapies for the disease, Exeltis’ first approved benznidazole and Bayer’s nifurtimox (Lampit), are only indicated for pediatric patients due to less conclusive efficacy data as well as safety/tolerability concerns for adults. The highly potent and promising preclinical candidate AN15368 (in vitro IC50 = 5nM) was developed based on a previously discovered new class of boron-containing…