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2013 Archived Content

6th Annual Targeting Pain with Novel Therapeutics

Translating Success from Preclinical Assays to the Clinic


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Monday, June 3

Recommended Short Courses* 

9:00 - 12:00 pm Animal Models of Pain: Progress and Challenges 

2:00 - 5:00 pm Epigenetic Mechanisms of Pain 

* Separate registration required

Tuesday, June 4

7:45 am Registration and Morning Coffee



8:30 Chairperson's Opening Remarks

Paul Karila, Ph.D., Head, Discovery Services, Cellectricon AB

8:40 We Must Work Together to Discover New Analgesics

Chas Bountra, Ph.D., Professor of Translational Medicine & Head, Structural Genomics Consortium, University of Oxford

Patients need new analgesics, the industry is struggling and the costs of R&D are rising. The only solution is to pool the resources and capabilities ofpublic and private funders, academics, patient groups and regulators. A pre-competitive partnership with rapid dissemination of reagents and data, will reduce the current wastage and needless exposure of patients to molecules destined for failure.

9:10 Virtual Discovery at AstraZeneca

Stephen Zicha, Ph.D., Project Director, Sciences, AstraZeneca Neuroscience Research & Development

Neuroscience drug discovery has experienced one of the highest failure rates in terms of bringing novel medicines to the patients who need them compared to other research areas, and no therapeutic targeting a novel mechanism has been approved for analgesic use in the past decade. One strategy to overcome this drought is to work collaboratively with multiple external groups to help accelerate the drug discovery process while benefitting from access to the world's best and newest scientific innovations. Some case studies highlighting this approach will be presented, with a particular focus on improving the translation of pre-clinical discoveries into successful clinical development.


Chantest9:40 Accelerating Pain Drug Discovery Targeting Ion Channels by Partnering with ChanTest

Emir Duzic, Ph.D., Senior Director, Discovery Services, ChanTest

10:10 Coffee Break

10:40 Discovery and Preclinical Validation of Novel Voltage-Gated Sodium and Calcium Channel Blockers with Analgesic Potential

Michael F. Jarvis, Ph.D., Volwiler Senior Research Fellow & Associate Director, Early Discovery, Pain, AbbVie, Inc.

The complexities associated with effective pain control are manifest by variations in underlying disease etiologies, functional interactions and redundancies in sensory pathways and low efficacy and/or poor tolerability for current analgesics. Voltage-gated sodium and calcium channels serve as final common modulators of neuronal membrane excitability and neurotransmitter release, respectively. Emerging genetic validation and biophysical data coupled with improved screening technologies have led to renewed interest in the discovery of novel blockers of these channels for pain management. The development of channel isoform selective blockers will be highlighted in this presentation.

11:10 State-Dependent Calcium Channel Blockers for Pain

Margaret S. Lee, Ph.D., Vice President, Research & Translational Medicine, Zalicus, Inc.

With prolonged excitation, such as during chronic pain signaling, the relative proportion of voltage gated calcium channel inactivation increases. Specifically targeting the inactivated state offers an opportunity for pharmacological selectivity that may broaden therapeutic window, minimize adverse effects and increase efficacy. We have discovered novel, first-in-class calcium channel blockers that demonstrate enhanced potency for the inactivated state. Z160 and Z944, selective, state-dependent, N- and T-type calcium channel blockers respectively, demonstrate potent effects in nonclinical pain models. Both are currently in clinical development for pain indications.


11:40 A New Selective Sigma-1 Receptor Antagonist (S1RA; E-52862) for the Treatment of Pain

José Miguel Vela, Ph.D., Drug Discovery & Preclinical Development, Esteve

Sigma 1 receptor (s1 receptor) is a unique ligand-regulated molecular chaperone which is activated under stress or pathological conditions and modulates the function of several neurotransmitter receptors and ion channels. Preclinical data obtained in sigma-1 receptor knockout mice and using several sigma-1 receptor ligands, particularly the s1 receptor antagonist S1RA (E-52862), are consistent with a role for s1 receptor in central sensitization and pain hypersensitivity and supports a potential therapeutic use of s1 receptor antagonists for the management of neuropathic pain. Moreover, data support their use in opioid adjuvant therapy: combination of S1RA with opioids results in potentiation of opioid analgesia, without significant increases in opioid-related unwanted effects. Results from clinical trials are thus eagerly awaited to ascertain the potential of s1 receptor modulation in pain therapy.

12:10 pm Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own

1:30 Plenary Keynote Panel Discussion: Advancing Pharma R&D through Communication & Collaborations: Bio-Connectivity at Work

Karim Dabbagh, Ph.D., Executive Director and Head, External R&D and Innovation Research Units, Pfizer Worldwide R&D

Glen N. Gaulton, Ph.D., Professor, Pathology and Laboratory Medicine; Executive Vice Dean and Chief Scientific Officer, Perelman School of Medicine, University of Pennsylvania

Peter Pitts, President and Co-Founder, Center for Medicine in the Public Interest

3:00 Grand Opening of the Exhibit Hall with Poster Viewing

4:00 AYX1 Drug Candidate For Preventing Post-Surgical Pain and Improving Functional Recovery

Julien Mamet, Ph.D., Founder & CSO, Adynxx, Inc.

AYX1 is a DNA decoy compound designed to prevent pain and facilitate functional recovery following surgery. Administered as a single intrathecal injection, AYX1 inhibits the activity of the transcription factor EGR1 focally in the spinal cord. Pharmacological studies demonstrate that AYX1 prevents mechanical hypersensitivity in preclinical models of neuropathic, incisional and inflammatory pain and improves functional recovery in models of spontaneous post-operative pain. AYX1 is under active clinical development.

4:30 Activation of Group II Metabotropic Glutamate (mGlu2/3) Receptors as a Treatment Strategy for Chronic Pain

Michael P. Johnson, Ph.D., Research Advisor, Pain/Migraine DHT, Neuroscience Discovery, Eli Lilly & Co.

The Group II metabotropic glutamate receptors (mGlu2 and mGlu3) are plasma-membrane associated G-protein-coupled proteins that function via presynaptic, postsynaptic and glial mechanisms to negatively modulate neuronal excitability. Within the pre-synaptic element, Group II mGlu receptors (primarily mGlu2) reside outside the synaptic zone where their activity appears to be dependent on an extrasynaptic, non-vesicular pool of glutamate. In addition, mGlu3 receptors are found within glial cells that are closely associate with neuronal synapses, and regulate sensitivity of synaptic transmission by controlling glutamate transporters and release of paracrine factors such as TGFβ. Activation of mGlu2/3 receptors by glutamate or by other exogenous agonists, such as LY379268, leads to the inhibition of synaptic glutamate release, thereby dampening downstream post-synaptic excitation. Thus, mGlu2/3 receptor agonists are efficacious in multiple animal models associated with hyper-glutamatergic tone including chronic pain [neuropathic, visceral and inflammatory pain models]. The relative importance of mGlu2 and mGlu3, as well as the novel epigenetic mechanism of some analgesic compounds will be discussed.

5:00 Development of a Phenotypic Pain Assay for Identification of Modulators of Excitability in Native Sensory Neurons

Paul Karila, Ph.D., Head, Discovery Services, Cellectricon AB

We have developed an enabling assay platform for chronic pain based on electric stimulation of primary DRG neuronal cultures. The biological relevance of the assay in combination with its ability to characterize a medium throughput screening libraryenables identification compounds for treatment of chronic pain early in the project lifecycle. Therefore, the platform is addingtrue value to the decision-making process. In addition, our phenotypic approach provides the possibility to address previously unknown targets within disease-relevant pathways.

5:30 Welcome Reception in the Exhibit Hall with Poster Viewing

6:30 Close of Day


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