OX1R

Centessa Pharmaceuticals Announces Preclinical Data Supporting ORX750’s Potential as a Best-in-Class Oral OX2R Agonist for the Treatment of Narcolepsy and Other Sleep-Wake Disorders

Retrieved on: 
Wednesday, October 25, 2023

BOSTON and LONDON, Oct. 25, 2023 (GLOBE NEWSWIRE) -- Centessa Pharmaceuticals plc (Nasdaq: CNTA), a clinical-stage pharmaceutical company that aims to discover and develop medicines that are transformational for patients, today announced a robust set of new preclinical data from in vivo and in vitro studies of its investigational, novel orexin receptor 2 (OX2R) agonist, ORX750, that support its potential best-in-class profile for the treatment of narcolepsy and other sleep-wake disorders.

Key Points: 
  • “The preclinical data showed ORX750 achieved maximal wake times and suppressed cataplexy at 0.1 mg/kg, the lowest oral dose tested in the DTA mouse model.
  • Notably, this activity was observed in both the DTA and Atax mouse models that recapitulate NT1 symptoms in humans.
  • Fluorescent imaging plate reader (FLIPR) assay with Chinese hamster ovary (CHO) cells stably expressing recombinant human OX1R or OX2R; OXA EC50 at hOX2R = 0.035 nM.
  • As measured by electroencephalogram (EEG) and electromyogram (EMG) with concurrent video in DTA and Atax mouse models.

Centessa Pharmaceuticals Reports Financial Results and Business Highlights for the Third Quarter of 2022

Retrieved on: 
Thursday, November 10, 2022

We continue to execute and build momentum with our core programs, said Saurabh Saha MD PhD, Chief Executive Officer of Centessa.

Key Points: 
  • We continue to execute and build momentum with our core programs, said Saurabh Saha MD PhD, Chief Executive Officer of Centessa.
  • Research & Development Expenses: $36.7 million for the quarter ended September 30, 2022, compared to $25.9 million for the quarter ended September 30, 2021.
  • General & Administrative Expenses: $12.3 million for the quarter ended September 30, 2022, compared to $12.5 million the quarter ended September 30, 2021.
  • Centessa Pharmaceuticals plc is a clinical-stage pharmaceutical company that aims to discover and develop medicines that are transformational for patients.

Centessa Pharmaceuticals Announces Poster Presentation Featuring Novel Orexin Receptor 2 (OX2R) Agonist Discovery Pipeline at the 26th Conference of the European Sleep Research Society (Sleep Europe 2022)

Retrieved on: 
Tuesday, September 20, 2022

BOSTON and LONDON, Sept. 20, 2022 (GLOBE NEWSWIRE) -- Centessa Pharmaceuticals plc (Nasdaq: CNTA), today announced that non-clinical data from its oral orexin receptor 2 (OX2R) agonist discovery pipeline have been accepted for poster presentation at the 26th Conference of the European Sleep Research Society meeting (Sleep Europe 2022) being held on September 27-30, 2022, in Athens, Greece. Centessa’s OX2R agonists are designed to directly target the underlying pathophysiology of orexin neuron loss in narcolepsy type 1 (NT1), with potential expansion into narcolepsy type 2 (NT2), and other sleep disorders.

Key Points: 
  • These novel OX2R agonist compounds showed high potency in activating recombinant human and endogenous mouse OX2Rs, with more than a thousand-fold selectivity for OX2R compared to OX1R.
  • Our innovative pipeline is both a testament to their expertise and strong validation of our approach to structure-based drug design.
  • We are encouraged by the non-clinical data and are rapidly progressing several potentially best-in-class oral small-molecule OX2R agonists through our discovery pipeline.
  • We are excited to showcase some of our small-molecule OX2R agonist discovery pipeline and share these data at Sleep Europe 2022, said Mario Alberto Accardi, PhD, Head, Centessa Orexin Program.