Delving into the Latest Updates on CeNeS Pharmaceuticals Plc with Synapse

Overview

A RANDOMISED, DOUBLE BLIND STUDY TO COMPARE THE ANALGESIC EFFICACY AND SAFETY PROFILES OF MORPHINE-6-GLUCURONIDE AND MORPHINE SULPHATE, GIVEN AS A LOADING DOSE FOLLOWED BY PATIENT-CONTROLLED ANALGESIA (PCA), IN PATIENTS SUFFERING MODERATE TO SEVERE POST-OPERATIVE PAIN REQUIRING PCA FOR AT LEAST 24 HOURS - N/A

Start Date21 Jun 2006

Sponsor / Collaborator

Cenes Ltd.

100 Clinical Results associated with CeNeS Pharmaceuticals Plc

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0 Patents (Medical) associated with CeNeS Pharmaceuticals Plc

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28

Literatures (Medical) associated with CeNeS Pharmaceuticals Plc

01 Jul 2007·AnesthesiologyQ1 · MEDICINE

CNS 7056

Q1 · MEDICINE

Article

Author: Waszczak, Barbara L. ; Kilpatrick, Gavin J. ; Cox, Richard F. ; Lovell, Gwyer G. ; Wiard, Robert P. ; McIntyre, Margaret S. ; Stafford, Jeffrey A. ; Pacofsky, Gregory J. ; Tilbrook, Gary S. ; Collins, Holly ; Feldman, Paul L.

AbstractBackground:A new benzodiazepine derivative, CNS 7056, has been developed to permit a superior sedative profile to current agents, i.e., more predictable fast onset, short duration of sedative action, and rapid recovery profile. This goal has been achieved by rendering the compound susceptible to metabolism via esterases. The authors now report on the profile of CNS 7056 in vitro and in vivo.Methods:The affinity of CNS 7056 and its carboxylic acid metabolite, CNS 7054, for benzodiazepine receptors and their selectivity profiles were evaluated using radioligand binding. The activity of CNS 7056 and midazolam at subtypes (α1β2γ2, α2β2γ2, α3β2γ2, α5β2γ2) of the γ-aminobutyric acid type A (GABAA) receptor was evaluated using the whole cell patch clamp technique. The activity of CNS 7056 at brain benzodiazepine receptors in vivo was measured in rats using extracellular electrophysiology in the substantia nigra pars reticulata. The sedative profile was measured in rodents using the loss of righting reflex test.Results:CNS 7056 bound to brain benzodiazepine sites with high affinity. The carboxylic acid metabolite, CNS 7054, showed around 300 times lower affinity. CNS 7056 and CNS 7054 (10 μm) showed no affinity for a range of other receptors. CNS 7056 enhanced GABA currents in cells stably transfected with subtypes of the GABAA receptor. CNS 7056, like midazolam and other classic benzodiazepines, did not show clear selectivity between subtypes of the GABAA receptor. CNS 7056 (intravenous) caused a dose-dependent inhibition of substantia nigra pars reticulata neuronal firing and recovery to baseline firing rates was reached rapidly. CNS 7056 (intravenous) induced loss of the righting reflex in rodents. The duration of loss of righting reflex was short (< 10 min) and was inhibited by pretreatment with flumazenil.Conclusions:CNS 7065 is a high-affinity and selective ligand for the benzodiazepine site on the GABAA receptor. CNS 7056 does not show selectivity between GABAA receptor subtypes. CNS 7056 is a potent sedative in rodents with a short duration of action. Inhibition of substantia nigra pars reticulata firing and the inhibition of the effects of CNS 7056 by flumazenil show that it acts at the brain benzodiazepine receptor.

01 Aug 2006·Current Opinion in AnaesthesiologyQ3 · MEDICINE

Drug development in anaesthesia: industrial perspective

Q3 · MEDICINE

Review

Author: Kilpatrick, Gavin J ; Tilbrook, Gary S

PURPOSE OF REVIEWIn this review, we summarize the new drugs in development in the anaesthesia field.RECENT FINDINGSThere are some interesting approaches, including pro-drugs of propofol such as Aquavan (MGI Pharma, Bloomington, Minnesota, USA) and novel 'soft-drug' sedatives and hypnotics (e.g. CNS-7259X and TD-4756) as well as a novel approach to terminate the action of steroidal neuromuscular blockers (sugammadex). There is also significant activity in the field of novel analgesics. Particularly addressing the fields of sedatives, hypnotics and neuromuscular blockers, however, there is relatively little drug discovery activity currently. Part of the reason for this may be that the mechanisms of action of anaesthetics are not fully understood. This cannot be the whole story, however, since attractive new targets have recently been identified. For example, an agent with selective actions at the beta3-containing subunit of the gamma-amino butyric acid-A receptor is likely to have the hypnotic effects of propofol without the cardiac depressant side-effects.SUMMARYWe consider the main reason for low activity is the perception in industry that there is little need for new drugs in anaesthesia because the needs are well addressed by existing agents. If this is not the case then anaesthesiologists need to be more effective in communicating their requirements.

01 May 2002·Current opinion in investigational drugs (London, England : 2000)

Memantine. Merz.

Review

Author: Kilpatrick, Gavin J ; Tilbrook, Gary S

Memantine hydrochloride, an NMDA antagonist, was launched in Germany by Merz in 1989 for the treatment of dementia, an indication for which development was continuing in other markets. It is also under development by Merz, Lundbeck, Neurobiological Technologies Inc (NTI) Forest Laboratories and Suntory for the potential treatment of Alzheimer's disease (AD), AIDS-related dementia and pain in patients with neuropathy, and by Allergan for the potential treatment of ocular disease. By July 2001, a regulatory filing for neuropathic pain was expected in 2003. In February 2002, the CPMP recommended to the EU commission to approve memantine for the treatment of moderately severe-to-severe Alzheimer's disease. At this time, marketing authorization was expected late in the first half of 2002, and Lundbeck planned to launch memantine under the brand name Ebixa during the second half of 2002. Merz and Lundbeck, filed memantine for AD in the EU in September 2000 and an NDA was submitted in November of that year. The compound was in phase H trials in the US for the treatment of AIDS-related dementia and pain by August 1996 and phase III trials for glaucoma and neuroprotection by 1999. Analysts at Merrill Lynch predicted in October 2001 that Allergan would make regulatory filings in the US for memantine in glaucoma and ocular hypertension in 2005, and that Forest Laboratories would file for memantine in the US as a supplement to Alzheimer's disease data in early 2002, and for the treatment of neuropathic pain in 2003. Sales of $25 million in 2004, rising to $75 million in 2005, were predicted by Merrill Lynch for this product.

100 Deals associated with CeNeS Pharmaceuticals Plc

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100 Translational Medicine associated with CeNeS Pharmaceuticals Plc

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Pipeline

Pipeline Snapshot as of 05 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

SPD-451 ( D1 receptor )	Parkinson Disease More	Discontinued
CNS-1161 ( NMDA receptor )	Esophageal Carcinoma More	Discontinued
CNS-1169 ( Opioid receptors x σ1 receptor )	Schizophrenia More	Discontinued
CNS-1531 ( NMDA receptor )	Nervous System Diseases More	Discontinued
Cerestat ( NMDA receptor )	Stroke More	Discontinued