molecules of the month

“compound 12”

selective GluN2B negative allosteric mod.

active in brain, proj. oral dose of 120 mg

from cell-based HTS and opt.

J. Med. Chem., Jul. 31, 2020

Janssen R&D, San Diego, CA

Structure of compound 12
1 min read

“compound 12” is a selective negative allosteric modulator of the GluN2B subunit of NDMA receptors intended for treatment of mood disorders. In this program, poor solubility and permeability were a challenge for oral exposure, but was addressed with a nanosuspension formulation. The nanosuspension allowed them to get high enough margins in preclinical species to assess safety, and achieve a low predicted human dose of 120 mg. No dose limiting toxicities were observed up to 500 mg/kg/day for 14 days in rats (~125 mg/rat/day).

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