iNovacia                                                 Brief Overview                                                 20...
The History of iNovacia    1996    Merger of Pharmacia & Upjohn    Small molecule Center of Excellence    formed in Stockh...
iNovacia Laboratories         Diversity         Novelty         Lead-likeness         ~280,000 compounds              Comp...
Typical Project ScopesCustomer            Characteristics                        Typical ServiceSegmentSmaller Biotechs   ...
Key Success Factors       The Right   PEOPLE                               The Right   ATTITUDEExcellence in   OPERATiONS ...
The Right People                 Dedicated to deliveryDedication       Want to make a difference                 Drug hunt...
The Right Attitude  Key Mission: To Maximize Value for the Customer• Trust and commitment - necessary for efficient sharin...
Excellence in Operations               Biophysical measurements implemented in assay optimization and               hit va...
Vast Pharma Experience• We have experience from a wide range of targets and  technologies• We have experience ranging from...
Assay Development & Screening LAB              Diversity              Novelty              Lead-likeness              ~280...
Assay Development & Screening LAB                        High-Throughput Screening•   Successfully developed and used a la...
Assay Development & Screening LAB                    Compound Collection• ~280,000 cherry-picked compounds• High level of ...
Assay Development & Screening LAB         Due Diligence Compound Collection              Report from top-5 Pharma•   95 % ...
Assay Development & Screening LAB       Fast and Flexible Sample Storage and Retrieval•   Storage under N2, at +4 C, dark ...
Assay Development & Screening LAB                    Filters introduced 2010 for Screening Set•       The publication of n...
Assay Development & Screening LAB                  Fragment-Based Screening• Scientists at iNovacia pioneers in developing...
Assay Development & Screening LAB                                  Hit Validation & Profiling Identity/Purity/Stability/So...
iNovacia Laboratories         Diversity         Novelty         Lead-likeness         ~280,000 compounds              Comp...
Structure-Based Optimization LAB   Validated Hits to Competitive Lead Series• Efficient chemical expansion and increasing ...
Thank You!Markus ThorChief Business Officer                 right from the startmarkus.thor@inovacia.sewww.inovacia.se    ...
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Inovacia drug discovery 2011

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iNovacia is an established quality provider of lead generation services including high-throughput screening and fragmen based screening. This is supported by a compound collection (ca 300,000 cmpds) and screening libraries of highest international standards with focus on diversity and novelty.

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Inovacia drug discovery 2011

  1. 1. iNovacia Brief Overview 2011 High-Throughput Screening Fragment Based Screening Assay Development Lead GenerationMarkus ThorChief Business Officer right from the startmarkus.thor@inovacia.sewww.inovacia.se iNovacia
  2. 2. The History of iNovacia 1996 Merger of Pharmacia & Upjohn Small molecule Center of Excellence formed in Stockholm 2001 Biovitrum spins out from Pharmacia CorporationBiovitrum small molecule deals Continued investments in small molecule R&D2002 - 5HT2c deal with GSK2003 - 11beta HSD deal with Amgen 2006 Management buy-out of iNovacia Asinex Ltd invests in iNovacia 2007 iNovacia: First Big Pharma deal 2008 iNovacia: First deal in the US 2010 2011 Karolinska professors and iNovacia Kancera acquires iNovacia and management establish Kancera AB is listed on the Nasdaq OMX First North right from the start iNovacia
  3. 3. iNovacia Laboratories Diversity Novelty Lead-likeness ~280,000 compounds Compound Collection Screening Structure- & Assay BasedTarget Lead Compounds Development Optimization LAB LAB High-Throughput Screening Medicinal Chemistry Fragment-Based Screening Crystallography Assay Development Mechanism of Action Studies Hit Validation Biophysical toolbox right from the start iNovacia
  4. 4. Typical Project ScopesCustomer Characteristics Typical ServiceSegmentSmaller Biotechs Typically strong in specific disease General step-wise support in drug area biology. discovery ranging from assay development to lead optimization Seek access to drug discovery expertise and technologyLarger Biotechs Fully integrated research in-house Full projects ranging from assayand Often lack HTS/FBS capacity development to lead series generation.Mid-sized Pharmas Seek access to additional screening technologies, novel lead seriesBig Pharmas Fully integrated research in-house Full projects ranging from assay development to lead series generation. Seek chemical diversity/novel lead series, additional capacity, complementing approaches and fresh thinking right from the start iNovacia
  5. 5. Key Success Factors The Right PEOPLE The Right ATTITUDEExcellence in OPERATiONS Vast Pharma EXPERiENCE right from the start iNovacia
  6. 6. The Right People Dedicated to deliveryDedication Want to make a difference Drug hunter’s attitude Speak their minds Take pride in quality Pride Know quality is key to success Pride in delivering result Extensive experience and skillsExperience Know what works, know what doesn’t work Understand big pharma as well as small biotech right from the start iNovacia
  7. 7. The Right Attitude Key Mission: To Maximize Value for the Customer• Trust and commitment - necessary for efficient sharing and value maximizing• Integrity• Big and small treated the same• Adapting to the customer’s specific needs – still speaking our mind• Continuously seeking to improve right from the start iNovacia
  8. 8. Excellence in Operations Biophysical measurements implemented in assay optimization and hit validation to ensure e.g. assay quality and only compoundsQuality acting by right mechanism of action are considered for SAR development Extensive hit profiling to secure quality in downstream chemistry program Continuous and systematic approach to minimize false positives Efficient working procedures, with all scientist actively involved Speed in the work flow Efficient screening approach Broad and state-of-the art technology base Flexibility Broad experience in designing screening and validation assays, including very challenging assays Modular approach with flexibility in project scope right from the start iNovacia
  9. 9. Vast Pharma Experience• We have experience from a wide range of targets and technologies• We have experience ranging from early discovery to clinical stage• We understand the industry challenges and trends We Understand the Customer’s Need for True Innovation, Quality and Speed right from the start iNovacia
  10. 10. Assay Development & Screening LAB Diversity Novelty Lead-likeness ~280,000 compounds Compound Collection Screening Structure- & Assay BasedTarget Lead Compounds Development Optimization LAB LAB High-Throughput Screening Medicinal Chemistry Fragment-Based Screening Crystallography Assay Development Mechanism of Action Studies Hit Validation & Profiling Biophysical toolbox right from the start iNovacia
  11. 11. Assay Development & Screening LAB High-Throughput Screening• Successfully developed and used a large number of high-throughput screening assays• Successfull delivery of qualified chemical series in over 30 screening projects• Quality and speed in all steps e.g. use of acoustic dispensing to avoid artifacts Targets Format Examples of Technologies Nuclear receptors 384 FRET 384 Reporter Gene Assay Kinases 384 HTRF Proteases 384 FRET Metabolic enzymes 96-384 SPA, HTRF, Isotopic GPCRs 384 Ca-kinetics 384 cAMP, Isotopic Ion channels 384 Cellux: voltage/ion sens. probe right from the start Functional cell assays 96-384 Luminescence, fluorescence iNovacia
  12. 12. Assay Development & Screening LAB Compound Collection• ~280,000 cherry-picked compounds• High level of diversity (~100 compounds per scaffold)• Mix of exclusive, semi-exclusive and commercial Cherry- picked• Contains novel scaffolds Cherry- Biovitrum ~70,000 picked• Experimental ADME profiling Asinex and others ~200,000• Chemical protocols available• QC by LC-MS validates integrity Exclusive, in iterative development ~10,000 right from the start iNovacia
  13. 13. Assay Development & Screening LAB Due Diligence Compound Collection Report from top-5 Pharma• 95 % of the compounds passed their stringent drug likeness criteria• 79 % where unique compared to their extensive compound collection• <1,5 % published with biological data• 35 % are not, or have not been, commercially available right from the start iNovacia
  14. 14. Assay Development & Screening LAB Fast and Flexible Sample Storage and Retrieval• Storage under N2, at +4 C, dark and dry. No measurable degradation since 2006.• Compound handling under inert atmosphere.• ~280,000 compounds in 1.4 ml microtubes• 10 mM dry DMSO stock solutions• All microtubes individually traceable• Fast cherry-picking• Ability to pick and plate during an HTS campaign to verify and validate. right from the start iNovacia
  15. 15. Assay Development & Screening LAB Filters introduced 2010 for Screening Set• The publication of new substructure filters for removal of Pan Assay Interference Compounds (PAINS) promted us to apply these filters and remove all PAINS from the iNovacia screening set. These compounds are not recognized by the filters commonly used to identify reactive compounds. (J. B. Baell and G. A. Holloway, J. Med. Chem., 2010, 53, 2719-2740.)• Redox active compounds identified by an in-house assay have been removed. Interestingly, we see a correlation between redox activity and PAINS. In a recent HTS, 79 hits were identified as being PAINS and 53 of those (67%) were also identified as redox active.• A few substructures that are not identified by the two filters above, but still appear as frequent hitters or suffer from lack of chemical stability have been removed. O O N S HN S N right from the start O N O H Examples of PAIN substructures iNovacia
  16. 16. Assay Development & Screening LAB Fragment-Based Screening• Scientists at iNovacia pioneers in developing fragment-based screening• Long experience and world-class competencies in NMR screening• Fragment libraries for primary screening – Primary screening by NMR: 900+ fragments containing 9-20 heavy atoms. Carefully designed with large numbers of readily available analogues from both commercial sources and the in-house iNovacia compound collection – Primary screening by biochemical assay at high compound concentration: 20,000 ”larger fragments” with MWs 200 - 350 right from the start iNovacia
  17. 17. Assay Development & Screening LAB Hit Validation & Profiling Identity/Purity/Stability/Solubility DRC and analysis HTS single Counter assays Clustering of confirmed hits point data Chemistry evaluation of hit series Tractability Library expansion Emerging SAR IP spaceBiophysical assays Dynamic Light Scattering (DLS) Nuclear Magnetic Resonance (NMR) Microcalorimetry (DSC/ITC) Final prioritization Surface Plasmon Resonance (SPR) of hit series Mass spectrometry (ESI-MS/MALDI-MS) Full chemistryAnalogs In-house, commercialy available, small program expansions by parallel chemistry, SAR analysisIn vitro ADME assays HSA binding, CYP inhibition, membrane affinity, metabolic stability, hERG binding, right from the start cytotoxicity iNovacia
  18. 18. iNovacia Laboratories Diversity Novelty Lead-likeness ~280,000 compounds Compound Collection Screening Structure- & Assay BasedTarget Lead Compounds Development Optimization LAB LAB High-Throughput Screening Medicinal Chemistry Fragment-Based Screening Crystallography Assay Development Mechanism of Action Studies Hit Validation Biophysical toolbox right from the start iNovacia
  19. 19. Structure-Based Optimization LAB Validated Hits to Competitive Lead Series• Efficient chemical expansion and increasing the odds – Through early SAR generation (in-house analogs, parallel chemistry and/or x-ray crystallography) – Through high quality chemical starting points – Through high quality pharmacological profiling• Highly integrated work flow – Medicinal chemistry – Pharmacology – Crystallography (in collaboration with Sprint Biosciences) – ADME – Automatic data capture and ELN right from the start – Humanized ex vivo and in vivo models within cancer iNovacia
  20. 20. Thank You!Markus ThorChief Business Officer right from the startmarkus.thor@inovacia.sewww.inovacia.se iNovacia

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