Together to Compete Stefano Manfredini

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1 University of Ferrara <Since 600 years we look forward > Together to Compete Stefano Manfredini

2 Converting research results into economic and social values Creative thinking Invention + ACTIO IOV-ATIO EXPERIMET-ATIO VALORIZ-ATIO

3 Inventors and Innovators To design a possible future

4 The value chain Thinking CULTURE IVETIO Making CREATIO PROTOTYPE Creating IDUSTRIALIZATIO DIFFUSIO

5 Guglielmo Marconi (Bologna, 25 april 1874 Roma, 20 July 1937) An example IVETOR (the experiments 1894) IOVATOR (the patent 1896) ETREPREEUR (la Marconi 1897)

6 A COMPLEX PATTER BUT TE KEY ISSUE: IMMAGIATIO othing happens unless first we dream (Quote by Carl Sandburg)

7 Graduated student Funky professor Company Man the three musketeers The idea started from a telephone call: why do not work together to train pepole?

8 DO IT BETTER

9 ITERATIO: ACADEMY COMPAY ACADEMY

Company: would benefit for an academic driven

return) Student: would benefit for a joint

10 Company: would benefit for an academic driven research project on basic science (long term investment) Academy: would benefit for a company driven research project (must have return) Student: would benefit for a joint driven research project on basic science (possible job returns)

11 4 Papers Experienced person trained in an industrial environment Follow-up on the other students in the labs Company benefits Student benefits

12 Innovative Approaches for the Identification of ovel Leads in Drug Discovery Alfredo Paio Director of Medicinal Chemistry at Aptuit - Verona former Director of Medicinal Chemistry at GlaxoSmithKline - Verona EUA - DOC-Carrier II Camerino th Oct

Project Context Inserted into Pharma R&D Process Target Validation Target validation Target to Lead it generation Lead generation Lead to Candidate Lead optimization Candidate Target Validation

13 Project Context Inserted into Pharma R&D Process Target Validation Target validation Target to Lead it generation Lead generation Lead to Candidate Lead optimization Candidate Target Validation TARGETS it Generation ITS it Exploration Lead Generation CEs Charact. LEADS Lead Exploration Lead Optimisation CEs Charact. CADIDATES Design Knowledge Design Knowledge LEAD GEERATIO Chemical tractability Consistency of SARs across compounds series Early developability Patentability novelty LEAD OPTIMIZAZIO In vitro potency Physico-chemical properties Selectivity panel ADME assays Preliminary PK PKPD model and human dose prediction Early safety studies (rat and dog), estimation of safety margin 13

14 Project Objectives To identify novel, developable chemotypes and leads to use as starting points for the Lead Optimization process Project Details To have access to a series of Proprietary and Privileged Scaffolds and Building Blocks to be used by Medicinal Chemists SCAFFOLDS BUILDIG BLOCKS FEATURES Provide OVELTY to lead series Intellectual Properties vital for Pharma Industry Comprise DEVELOPABILITY characteristics (physical-chemical properties, metabolic stability and toxicological profile ) CEMISTRY COMPLEXITY expected, nevertheless FEASIBLE structures 14

15 Privileged Scaffolds and Building Blocks STEP A: DESIG Fishing/exploiting validated scaffolds from successful programs Adapting scaffolds from competitors, literature R R 0,1 R Modulate physical-chemical properties of known fragments Mimic structural motives for CS targets F F C Adapting scaffolds from drugs in development/market 15

16 Privileged Scaffolds and Building Blocks STEP B: PREPARATIO Internal efforts Collaboration with Academic groups Outsourcing (CRO in Europe, India, China) Commercial sources Collaboration with Academic groups Reasons for the choice Access to Competences in Drug Design - Medicinal Chemistry Access to igh Competences in Modern Synthetic Organic Chemistry Access to highly skilled students Opportunity to participate to and drive students training Opportunity to identify industry future researchers 16

17 Privileged Scaffolds and Building Blocks STEP C: LOGISTICS Scaffolds_PSY Med Chem Project Creation (all PSY Med Chemists team members) Compounds Store at Verona Compounds Bank (reserved to all Med Chemists) ISIS ET db (Scaffolds_PSY Med Chem) creation 17

18 STEP D: APPLICATIOS Azabicyclo Oxadiazole Set: Cross-Fertilization Dopamine Receptors Ligand O Glutamate receptors ligands eurokinines inhibitors eurotrasmiters Re-uptake inhibitors O R EXO O R EDO R O R EXO O R EDO R = Me, para-f-phenyl R R O ongoing O planned Ion Channel ligands CS tailored compound collections for focused screening 18

19 Innovative Approaches: Integration of Competences and Processes In house programs Academic Know-how Competitor patents DESIG and PRODUCTIO of Compounds Sets DESIG/ IDETIFICATIO of PRIVILEGED SCAFFOLDS SCREEIG of Tailored SET Literature Development/ Marketed drugs Commercial sources Innovative Leads IOVATIVE and BETTER MEDICIES igh quality Clinical Candidates 19

20 University of Ferrara <Since 600 years we look forward > Together to Compete Carmela apolitano

21 About myself MSc (Chemistry), Università degli Studi di apoli Federico II, apoli, Italy (2004) PhD, Università degli Studi di Ferrara, Ferrara, Italy (2008) Post-doctoral researcher, ational University of Ireland, Galway, Ireland ( ) Senior researcher, Aptuit, Verona, Italy (2011)

22 Why a PhD? One never notices what has been done; one can only see what remains to be done. (Marie Curie) Why the GSK-funded PhD? It seems plain and self-evident, yet it needs to be said: the isolated knowledge obtained by a group of specialists of a narrow field has in itself no value whatsoever, but only in its synthesis with all the rest of knowledge and only inasmuch as it really contributes in this synthesis towards answering the demand, who are we? (Erwing Schrödinger)

Doctoral course and dissertation Open competition Three-years doctoral course in Pharmaceutical Sciences osting institution: Università

23 Doctoral course and dissertation Open competition Three-years doctoral course in Pharmaceutical Sciences osting institution: Università degli Studi di Ferrara Sponsoring company: GlaxoSmithKline S.p.A. eurosciences Centre of Excellence for Drug Discovery (CEDD) Embargoed thesis

24 Management and organization osting laboratories School of Pharmacy, University of Ferrara (two years) GSK eurosciences CEDD of Verona (one year placement, member of the Medicinal Chemistry Department) Supervision Joint academia (Prof. Manfredini) industry (Dr Cardullo) supervision Sharing of the data/ results - Regular project meetings with both academic and industrial supervisors, as well as with any other appropriate project staff - Six monthly progress report compilation

25 Added values Advanced knowledge and understanding of current drug discovery process Awareness and understanding of current trends and developments in important areas such as pharmacology, pharmaceutical analysis, drug design and pharmaceutics ands-on experience of modern instrumentation used in drug discovery and development Practical and problem-solving skills commensurate with the encountered challenges Awareness of some aspects and issues of project management Teamwork and communication skills

26 Issues: publication and confidentiality Limited possibility to present the research findings to meetings/conferences (posters, oral communications) Delayed publication of the research outcomes due to investigation, application and/or patent protection of the data Embargo on public access to the thesis (three years) owever Three papers have been published on peer-reviewed scientific journals after completion of the doctoral programme; one is under approval process.

27 The overall experience Industrial relevance and academic quality User orientated i.e. strong business focus Flexibility Employability opportunities both inside and outside academia etwork of contacts outside academia

Real World Drug Discovery A Chemist's Guide to Biotech and Pharmaceutical Research

Real World Drug Discovery A Chemist's Guide to Biotech and Pharmaceutical Research Robert M. Rydzewski ELSEVIER Amsterdam Boston Heidelberg London New York Oxford Paris San Diego San Francisco Singapore