molecules of the month


potent, oral fusion inhibitor of RSV virus

efficacious in Ph. 2a challenge study in HV

from scaffold hop from known inhibitor

J. Med. Chem., Jun. 15, 2020

Janssen Pharmaceutica NV, Beerse, BE

Structure of small molecule fusion inhibitor JNJ-53718678
1 min read

JNJ-53718678 is a potent and orally available fusion inhibitor of the RSV virus, optimized from a prior oral inhibitor, BMS-433771. The prior inhibitor was challenged by moderate potency, suboptimal PK in preclinical species, limited lung distribution, and potential complications from CYP TDI due to an aminocyclopropyl moiety. The improved molecule is currently in clinical trials with hospitalized patients after demonstrating activity in healthy volunteers.

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