fbpx

molecules of the month

NITD-688

pan-serotype dengue virus NS4B inhibitor

oral preclin. candidate, trial planned

From 1.5M cmpd phenotypic screen + opt.

Sci. Transl. Med., Feb. 3, 2021

Novartis (NITD), Emeryville, CA

NITD-688
1 min read

14. The Novartis pan-serotype dengue virus (DENV) NS4B protein inhibitor, NITD-688, is a preclinical candidate with strong activity against all four serotypes of DENV in vitro and excellent oral efficacy in a mouse model. The starting point was identified through phenotypic screening of 1.5M compounds and counterselection against host factors and cytotoxicity. The target was identified through resistance mutations and binding confirmed by 15N-NMR. Allometric scaling was used to predict a human efficacious dose of 35 mg QD. Non-GLP studies showed good tolerability in dog up to 80 mg/kg, and QTc prolongation was not observed despite partial inhibition of hERG in vitro. The authors allude to designing a trial to ensure patients are recruited within 48 h of fever onset…


request a trial

Drug Hunter is commited to helping industry innovators make informed decisions. Premium members have access to our library of the latest stories in science, written by scientists.

Request a trial to access insights powering the pros in our industry.


already a member? log in: