molecules of the month


non-immunosuppressive cyclophilin inhibitor

oral activity in humanized HCV model

from semisynthetic deriv. of FR901459

Bioorg. Med. Chem. Lett., Jun. 2, 2020

Astellas Pharma, Ibaraki, JP

Structure of ASP-5286
1 min read

ASP5286 is an analog of the natural product cyclosporin A that maintains the anti-HCV activity of cyclosporin A by binding to cyclophilin, but was optimized to be less immunosuppresive than cyclosporin A. The macrocycle was identified through semisynthetic derivitization of a related natural product, FR901459. The Astellas team was able to optimize compounds from immunosuppresive compounds with poor oral exposure to the non-immunosuppressive clinical candidate 5286 with oral activity in a mouse humanized liver HCV model.

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