molecules of the month


oral, BP, selective OX1R GPCR antagonist

orally efficacious in panic attack models

from optimization of internal OX2R antagonist

ACS Med. Chem. Lett., May 5, 2020

Janssen R&D, San Diego, CA

1 min read

JNJ-54717793 is a selective antagonist of the orexin-1 receptor intended for use in anxiety disorders, in contrast to dual orexin-1/2 inhibitors and orexin-2 inhibitors typically applied for sleep disorders. It’s a surprisingly large molecule (three aromatic rings and a bicycle) for an oral, brain-penetrant clinical candidate with predicted once-daily dosing in humans. This compound was very well-tolerated in preclinical species (NOAEL 250 mg/kg in rodent, 25 mg/kg in dog).

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