Centessa presents ORX750 preclinical data; shows potential best-in-class profile for narcolepsy

Centessa Pharmaceuticals plc

ORX750 potently activates OX2R with EC50 of 0.11 nM and 9,800-fold selectivity over OX1R.
Oral doses as low as 0.1 mg/kg achieved 100% wake time for ≥3 hours and suppressed cataplexy for ≥6 hours in mouse models.
Effects on wake and cataplexy latency maintained for >14 days of dosing.
Clinical proof-of-concept data planned for 2024; IND-enabling studies ongoing.
Preclinical PK profile suggests high, early, and sustained brain exposure in multiple species.

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