Therapeutics

SUVN-G3031

Overview

Name: SUVN-G3031
Therapy Type: Small Molecule (timeline)
Target Type: Cholinergic System (timeline), Other Neurotransmitters (timeline)
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Phase 1)
Company: Suven Life Sciences Ltd

Background

SUVN-G3031 is an orally active histamine H3 receptor antagonist being developed to treat cognitive deficits in Alzheimer's disease and schizophrenia. Histamine H3 receptors are widely expressed in healthy and Alzheimer's disease brains (Medhurst et al., 2009). They exert neuromodulatory functions on the cholinergic, adrenergic, and dopaminergic neurotransmitter systems. Preclinically, inhibiting this receptor has been shown in mice and rats to enhance cholinergic signaling, reduce tau phosphorylation, and reverse behavioral deficits (Medhurst et al., 2007Bitner et al., 2011). Previous histamine H3 receptor antagonists that were in Phase 2 clinical development for cognition in Alzheimer's include Servier's S 38093ABT 288, and GSK239512.

No peer-reviewed scientific studies have been published for SUVN-G3031. At the 2014 AAIC conference, Suven Life Sciences reported positive data on exposure, safety, pharmacokinetics, and behavioral assays in rats. The poster claimed an increase in cortical histamine and acetylcholine levels as well as reversal of memory deficits (Babu et al., 2014). Further preclinical data were presented at AAIC in 2015 (Benade et al., 2015).

Findings

Between September 2014 and August 2015, CRO Quintiles conducted a Phase 1 safety, tolerability, and pharmacokinetics study in 64 healthy men in the state of Kansas. This was a single- and multiple-ascending dose trial.

For registered trials on this compound, see clinicaltrials.gov.

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References

Therapeutics Citations

  1. S 38093
  2. ABT-288
  3. GSK239512

Paper Citations

  1. . Characterization of histamine H3 receptors in Alzheimer's Disease brain and amyloid over-expressing TASTPM mice. Br J Pharmacol. 2009 May;157(1):130-8. PubMed.
  2. . GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. PubMed.
  3. . In-vivo histamine H3 receptor antagonism activates cellular signaling suggestive of symptomatic and disease modifying efficacy in Alzheimer's disease. Neuropharmacology. 2011 Feb-Mar;60(2-3):460-6. PubMed.
  4. . SUVN-G3031: A Novel and Potent Histamine H3 Receptor Antagonist for Potential Treatment of Cognitive Deficits. July 2014, Volume 10, Issue 4, Supplement, Pages P459–P460
  5. . Suvn-g3031, an h3 receptor inverse agonist, produces procognitive effects without affecting sleep in preclinical models. July 2015, Volume 11, Issue 7, Supplement, Page 475

External Citations

  1. clinicaltrials.gov

Further Reading

No Available Further Reading