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CNT-9982

Development stage: Preclinical
Lead developer: Centessa Pharmaceuticals
Modality: Small Molecules
Administration: Oral

Overview

CNT-9982 is an orally available, brain-penetrating small molecule orexin receptor 2 (OX2R) agonist being developed by Centessa Pharmaceuticals. It is primarily targeted for the treatment of major depressive disorder (MDD) and hypersomnolence. The compound exhibits high potency with an EC50 of less than 100 picomolar and is highly selective, showing over 5000-fold selectivity for OX2R compared to OX1R. Preclinical studies have demonstrated that CNT-9982 can normalize hypersomnolent phenotypes and alleviate behavioral despair in rat models of depression, as well as promote wakefulness in marmosets by activating histaminergic neurons in the tuberomammillary nucleus (TMN).

Targets

HCRTR2 (Orexin/hypocretin receptor type 2)

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