orally active beta-1,3-glucan synthesis inhibitor
eff. in fungal infect. model, discont. for alt.
from semisynthetic mod. of enfumafungin
Bioorg. Med. Chem. Lett., Jun. 19, 2020
Merck & Co., Kenilworth, NJ / Scynexis
MK-5204 is a broad spectrum Candida antifungal agent derived from the natural product, enfumafungin. I was impressed that the molecule not only demonstrates oral efficacy but also has good oral PK in higher species (dog, cyno), given that the molecule is a large zwitterion with several very polar groups, including a primary amide, primary amine, carboxylic acid, and triazole. Development of this molecule was discontinued in favor of a further optimized analog, ibrexafungerp (MK-3118, SCY-078), currently in phase III clinical trials.