Day One

30 January, 2013

8.00 Registration, Coffee & Networking

8.55 Chair’s Opening Remarks

Michael Lisanti, Director, Breakthrough Breast Cancer Research Unit, The University of Manchester

UNDERSTANDING THE BIOLOGY BEHIND WARBURG

9.00 Therapeutic Opportunities for the Exploiting the “Reverse Warburg Effect” and “Two-Compartment” Cancer Metabolism

A detailed overview of the “Reverse Warburg Effect” and “Two-Compartment Tumor Metabolism”
New strategies for diagnostics and therapeutics to target and prevent cancer metabolism, especially oxidative mitochondrial metabolism (OXPHOS) in tumor cells, allowing for personalized cancer treatment
Understanding the drug-resistance mechanism(s) that protect cancer cells via these new metabolic paradigms

Michael Lisanti, Director, Breakthrough Breast Cancer Research Unit, The University of Manchester

9.30 Case Study: First-in-class drug, CPI-613 simultaneously Targets Multiple Mitochondrial Metabolic Regulatory Processes in Tumor Cells

Understanding the profound alteration of mitochondrial metabolic regulation in malignant cells
Simultaneously attacking multiple, tumor-specific regulatory processes, selectively killing tumor cells

Paul Bingham, Vice President, Research, Cornerstone Pharmaceuticals

10.00 Applying Metabolytics to Achieve R&D Efficiency

Metabolytics is a key data stream for translational research
Discovery and preclinical utility of metabolytics
Biochemical conservation and the clinical translation of metabolytics

Andrea Eckhart, Associate Director, US Pharma/Biotech, Metabolon

EXPLORING THE LATEST TECHNOLOGY ADVANCES TO ENHANCE TARGET DISCOVERY

10.15 Speed Networking & Morning Refreshments

11.15 Using Sophisticated Technology to Study Cellular Metabolism in Cancer

Understanding the role of NAMPT in cancer cells and the inhibition of NAMPT by the tool compound FK866 for significant attenuation of glycolysis in tumor
Shedding new light on how NAMPT regulates tumor metabolism and illustrating the potential utility of NAMPT as a novel cancer target

Genshi Zhao, Research Advisor, Eli Lilly and Company

11.45 Establishing a project portfolio within tumor metabolism boosted by a fragment-based approach

Introducing an efficient platform for the discovery of small molecule inhibitors

Application to targets within the autophagy pathway, lipid metabolism and serine and proline biosynthesis
Understanding biological pathways using small-molecule inhibitors for early cell based assessment of effects
Describing a novel business model where early partnering gives customer an opportunity to guide discovery projects

Anders Åberg, CEO & Founder, Sprint Bioscience

12.15 Panel Discussion: Why Invest in Cancer Metabolism?

Exploring cancer metabolism as a viable venture for drug development
Discussing the potential of cancer metabolism drugs and demonstrating proof of concept

Anke Klippel-Giese, Senior Director, Oncology, Pfizer; Francis Kern, Senior Director, External Scientific Affairs, Daiichi Sankyo; Lars Ährlund-Richter, CSO, Kancera

12.45 Lunch

1.45 Using High Throughput Metabolomics, Flux Analysis, and Target Discovery to Target Novel Pathways in Cancer

Using these technologies to understand cell metabolism and key pathways used in cancer metabolism
Identifying pathways of interest in the pursuit of novel cancer metabolism targets

Edward Driggers, Senior Director, Cell Metabolism, Agios

EFFECTIVE TARGET IDENTIFICATION: LEARNING FROM THE INDUSTRY

2.15 Successfully Identifying Targets within Cancer Metabolism

Using sophisticated techniques to identify therapeutics targets within metabolism for successful drug development
Methods for validating new targets and progressing cancer metabolism drugs into the pipeline

Beat Nyfeler, Research Investigator, Novartis Institutes for BioMedical Research

3.15 Afternoon Refreshments

3.45 Tackling Potential Redundancies in Targeting Cancer Metabolism

Exploring targeting multiple pathways to achieve the best therapeutic results
Predicting the necessity to block multiple pathways to overcome redundancies and by-pass mechanisms

Valeria Fantin, Vice President, Tumor Cell Biology, Pfizer

4.15 Structure-based Identification of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors

Understanding how tumor and normal cells utilize metabolism pathways for drug discovery opportunities
Targeting important proteins across glycolysis, glutaminolysis, the TCA cycle and other pathways leading to amino acids, lipids and nucleic acid components
Discussing initial efforts on NAMPT Inhibitors

Kenneth Bair, SVP & Head of R&D, Forma Therapeutics

4.45 Case Study: IDH Mutations and Tumorigenecity

Mutations in the isocitrate dehydrogenase 1 (IDH1) and 2 (IDH2) genes cause a neomorphic enzyme activity that results in the production of 2-hydroxyglutarate (2HG)
Agios has generated small molecules capable of selectively inhibiting IDHm enzymes
Upon compound treatment, these compounds are able to lower 2HG by >90% in tumor xenograft models

Katharine Yen, Director, Biology, Agios