molecules of the month


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

1 min read

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.

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