NAEJA Pharmaceutical Inc.
            North America, Europe, Japan, Asia
Drug discovery Contract Research Organization (CR...
NAEJA Pharmaceutical Inc.
                    Client Base (2008‐2009)*


                      Biotech     Large 
        ...
NAEJA’s Role in                           – Infrastructure
Drug Discovery                            – Expertise
         ...
Computational 
    Chemistry                Infrastructure:
Molecular modeling/QSAR
 Survey chemical space
Target librarie...
Computational Chemistry

•   Hit Discovery:
     – ligand docking
     – pharmacophore generation

•   Lead Optimization: ...
Medicinal Chemistry      Infrastructure:
     Review TPP
     Review SAR

 Experience in design:
 ADME/DMPK/toxicity 
    ...
Staffing Chemistry: 71% 
 Director              Biology: 7%
  100% PhDs            Analytical: 5% 
                       ...
PhDs & Postdoc Training of NAEJA Scientists
Synthetic Chemistry
Infrastructure:          Over 60 Ph.D. Chemists
                        Reactions up to 22L scale

   ...
Analytical & Purification Support
            Purification                           Analytical
– Prep HPLC               ...
Infrastructure:


 Design    Synthesis




                       Biological Services
Analysis    Test          Microbiolo...
Select Organism Microbiology
Select Organism Microbiology
– Time‐kill studies
 – Time‐kill studies
– Post antibiotic effec...
In vivo Pharmacology Models
Septicemia                                      Pneumonia
     –   Staphylococcus aureus MRSA ...
Pharmacokinetics
             in vitro                           in vivo
– Aqueous solubility                  –   Bioavai...
Infrastructure:


                            Design    Synthesis



Scientific Support

 Internal: Directors
 Minimum ind...
NAEJA’s Role in                           – Infrastructure
Drug Discovery                            – Expertise
         ...
Anti‐infectives:
    Tazobactam             Track Record:
  β‐Lactamase Inhibitor
Collaboration with Taiho
Marketed by Wye...
Anti‐infectives:
     SYN‐2190                Track Record:
        Licensed: 
Anti‐infective Diagnostics
    WO 2009/0518...
Mofezolac (Disopain™)      Track Record:
   Commercial NSAID
Collaboration with Taiho
Marketed by Mitsubishi

            ...
Published TAs:

Track Record:             Anti‐Infectives:
                          Topoisomerases
                      ...
Cardiovascular Targets:
Track Record:           Antihypertensives ‐ Renin
                        Anticoagulants ‐ Factor ...
Track Record:


Design     Synthesis


                           Recent Publications:

                              MIC ...
Track Record:


                           Design    Synthesis


Scientific Support

Internal: Sr. Directors
 Medicinal Ch...
Papers and Patents
   238 in total
                     Track Record:


   Antiinfectives     Design    Synthesis
   Antif...
Track Record:


                                 Design    Synthesis


External Consultants
  Dr John Domagala
Senior Cons...
NAEJA’s Role in                           – Infrastructure
                                          – Expertise
Drug Disc...
Single Client – Concurrent Anti‐infectives
                 & Inflammation Programs




                                  ...
Other Successful Recent Programs




                                                 Candidate
Hit Generation     Hit to ...
Project starts: Q1
Project starts: Q1                                    Q1: Validated
                                   ...
NAEJA Business Models


Compound based               Program based 
fee‐for‐service              Drug discovery

Custom Sy...
NAEJA Packages:
Compound based 
fee‐for‐service                    Design     Synthesis



– Short term
– Fixed deliverabl...
Program Research:
FTE based R&D Service
– Staffing
     – 1 computational chemist
     – 5 synthetic/medicinal chemists
  ...
Contact Information

Dr. Sameeh Salama
Senior Director, 
Business Development


Dr. Chris Diaper 
Business Development 
As...
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NAEJA Presentation

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NAEJA Presentation

  1. 1. NAEJA Pharmaceutical Inc. North America, Europe, Japan, Asia Drug discovery Contract Research Organization (CRO) Previously SynPhar (1987‐1999) Privately owned 63,000 ft2 facility Based in Edmonton, Canada
  2. 2. NAEJA Pharmaceutical Inc. Client Base (2008‐2009)* Biotech Large  Pharma Japan US Longest collaboration Europe 12 years Longest contract 4 years *(% revenue)
  3. 3. NAEJA’s Role in  – Infrastructure Drug Discovery – Expertise – Experience Design Synthesis HIT CANDIDATE Analysis Test
  4. 4. Computational  Chemistry Infrastructure: Molecular modeling/QSAR Survey chemical space Target libraries: defined  physical properties Design Synthesis Analysis Test
  5. 5. Computational Chemistry • Hit Discovery: – ligand docking – pharmacophore generation • Lead Optimization:  – ligand docking – QSAR • Physical Properties:  – pKa, log P, log D, & solubility
  6. 6. Medicinal Chemistry Infrastructure: Review TPP Review SAR Experience in design: ADME/DMPK/toxicity  Design Synthesis Analysis Test
  7. 7. Staffing Chemistry: 71%  Director Biology: 7% 100% PhDs Analytical: 5%  Admin: 17% Project PhDs & Postdocs by Training Location Coordinator 100% PhDs Canada US Europe Scientist Asia 90% PhDs Japan
  8. 8. PhDs & Postdoc Training of NAEJA Scientists
  9. 9. Synthetic Chemistry Infrastructure: Over 60 Ph.D. Chemists Reactions up to 22L scale Access to SciFinder, Reaxys Access to NMR, MS, LC‐MS,  analytical and prep HPLC Design Synthesis Analysis Test
  10. 10. Analytical & Purification Support Purification Analytical – Prep HPLC – Chiral HPLC – Automated prep LC‐MS – CHIRALPAK™ AD, AD‐RH, OD, OD‐R,  – Routine scale 100‐500 mg OF, OB, OJ – Semi‐prep NP/chiral – LC‐MS – Routine scale 50‐100 mg – Elemental analysis, IR, & optical  – Biotage rotations – Routine NP/RP – Specialty columns also available 1H NMR e.g. alumina, cyano, ion‐exchange – – 2 × 400 MHz
  11. 11. Infrastructure: Design Synthesis Biological Services Analysis Test Microbiology DMPK Pharmacology Toxicity
  12. 12. Select Organism Microbiology Select Organism Microbiology – Time‐kill studies – Time‐kill studies – Post antibiotic effect (PAE) studies – Post antibiotic effect (PAE) studies Microbiology, DMPK – Frequency of resistance – Frequency of resistance Rodent in vivo Efficacy Rodent in vivo Efficacy & Toxicity – Superficial skin infection – Superficial skin infection – Pneumonia – Pneumonia Primary MIC Panel Primary MIC Panel – Septicemia – Septicemia – NCCL procedures – NCCL procedures – Sepsis In vitro PK In vitro PK – Sepsis – Gram +ve and –ve – Gram +ve and –ve – Thigh infection – Thigh infection – Physicochemical  – Physicochemical  In vitro Toxicity In vitro Toxicity – Anaerobes properties properties – hERG – Anaerobes – hERG – Fungi – Fungi Secondary Panel Secondary Panel – Chemical & metabolic  – Chemical & metabolic  – CYP 450 panel – CYP 450 panel Stability Stability – MIC90’s – MIC90’s In vivo Safety and PK In vivo Safety and PK – > 4000 clinical isolates – > 4000 clinical isolates – Acute/sub acute dosing – Acute/sub acute dosing – Includes 2009 strains – Includes 2009 strains – Cmax, Tmax, Vdd, t½, AUC, %F – Cmax, Tmax, V , t½, AUC, %F Hit Candidate
  13. 13. In vivo Pharmacology Models Septicemia Pneumonia – Staphylococcus aureus MRSA – Streptococcus pneumoniae – Staphylococcus Aureus MSSA – Aspergillus fumigatus – Candida albicans – Aspergillus fumigatus Sepsis Thigh infections – Staphylococcus aureus MRSA – Staphylococcus aureus MRSA – Staphylococcus aureus MSSA – Staphylococcus aureus MSSA – Escherichia coli – Streptococcus pneumoniae – Escherichia coli Superficial skin infection Animal Facilities (CCAC):  Level II biohazard – Staphylococcus aureus MSSA
  14. 14. Pharmacokinetics in vitro in vivo – Aqueous solubility – Bioavailability studies – Partition coefficients – Blood/plasma concentrations – Plasma protein binding – Tissue concentration/distribution – A‐B permeability (MDCK) – Metabolite profiling – Metabolic stability (microsomes,  hepatocytes) – UPLC‐MS‐MS screening Animal facilities adhere to CCAC
  15. 15. Infrastructure: Design Synthesis Scientific Support Internal: Directors Minimum industrial  Analysis Test experience – 15 years External: Consultants  Specific TAs/disciplines
  16. 16. NAEJA’s Role in  – Infrastructure Drug Discovery – Expertise – Experience Design Synthesis HIT CANDIDATE Analysis Test
  17. 17. Anti‐infectives: Tazobactam Track Record: β‐Lactamase Inhibitor Collaboration with Taiho Marketed by Wyeth/Pfizer Design Synthesis Analysis Test
  18. 18. Anti‐infectives: SYN‐2190 Track Record: Licensed:  Anti‐infective Diagnostics WO 2009/051838 Design Synthesis Analysis Test
  19. 19. Mofezolac (Disopain™) Track Record: Commercial NSAID Collaboration with Taiho Marketed by Mitsubishi Design Synthesis Analysis Test
  20. 20. Published TAs: Track Record: Anti‐Infectives: Topoisomerases DNA gyrase β‐Lactamases Histidine kinase PPB3, PDK, LeuRS Design Synthesis Efflux pump inhibitors Analysis Test
  21. 21. Cardiovascular Targets: Track Record: Antihypertensives ‐ Renin Anticoagulants ‐ Factor Xa Cancer: Cyclin‐dependant kinase Cdk4 Design Synthesis Dermatology: Androgen receptors CNS: NRI’s and 5‐HT1A  Inflammation: Analysis Test TNF‐α, IL‐23, & PDE4
  22. 22. Track Record: Design Synthesis Recent Publications: MIC screening Bioorg. Med. Chem. Lett. Analysis Test 2009, 19, 1292, 3374, & 4626 ICAAC 2009 Poster: Efficacy study:  MRSA mouse skin  infection model
  23. 23. Track Record: Design Synthesis Scientific Support Internal: Sr. Directors Medicinal Chemistry Analysis Test Dr Rajeshwar Singh 52 papers; 46 patents Dr S. N. Maiti 58 papers, 15 patents
  24. 24. Papers and Patents 238 in total Track Record: Antiinfectives Design Synthesis Antifungals CV Cancer Inflammation Mental Health COPD Analysis Test Auto Immune Synthesis Analytical
  25. 25. Track Record: Design Synthesis External Consultants Dr John Domagala Senior Consultant with IDSC  Previous position: Analysis Test Executive Director at Pfizer Prof. Mike James FRS University of Alberta Crystallography & Modeling
  26. 26. NAEJA’s Role in  – Infrastructure – Expertise Drug Discovery – Experience Design Synthesis HIT CANDIDATE Analysis Test
  27. 27. Single Client – Concurrent Anti‐infectives & Inflammation Programs Candidate Hit Generation  Hit to Lead  Lead  and Validation Optimization NAEJA CLIENT Phase 2 Phase 3 One program { On hold: biological liability Phase 1: 2009 Candidate selection: 2009 Lead declaration: 2009
  28. 28. Other Successful Recent Programs Candidate Hit Generation  Hit to Lead  Lead  and Validation Optimization NAEJA Phase 1b/2: Cardiovascular disease Clinical trials: Pain management Clinical trials: anti‐bacterial Clinical trials: anti‐fungal Alzheimer's program Anti‐viral program
  29. 29. Project starts: Q1 Project starts: Q1 Q1: Validated Q1: Validated thigh model Q3: Pre‐candidate  Q3: Pre‐candidate  #1 put on hold:  CASE STUDY Hit structure: narrow activity spectrum Hit structure: narrow activity spectrum thigh model #1 put on hold:  Racemic Racemic biological liability biological liability Anti‐infective Program Limited SAR Limited SAR Q1: ½ Kg = NAEJA Q1: ½ Kg Undeveloped chemistry: unusual scaffold Undeveloped chemistry: unusual scaffold pre‐candidate  pre‐candidate  = CLIENT No crystal structure No crystal structure synthesized synthesized Q1: Chemistry development, SAR, MIC panel Q1: Chemistry development, SAR, MIC panel Q1 to Q4 2009 Q1 to Q4 2009 Q4: Racemic Q4: Racemic Q1: Process development Q1: Process development Biochemistry Biochemistry lead #1 declared lead #1 declared Candidate declaration Candidate declaration >98% purity >98% purity Q3: Molecular modeling & SBDD Q3: Molecular modeling & SBDD Q2: chiral HPLC Q2: chiral HPLC >98% eefffff >98% eefffff Q3: Crystal  Q3: Crystal  Q1: Racemic lead  Q1: Racemic lead  structure structure #2 declared #2 declared Q1: ADME Q1: ADME 2007 2008 2009
  30. 30. NAEJA Business Models Compound based  Program based  fee‐for‐service Drug discovery Custom Synthesis FTE R&D Service Discovery Biology
  31. 31. NAEJA Packages: Compound based  fee‐for‐service Design Synthesis – Short term – Fixed deliverables Analysis Test – All materials & labor included – Literature searches included – Client owns 100% of the IP
  32. 32. Program Research: FTE based R&D Service – Staffing – 1 computational chemist – 5 synthetic/medicinal chemists – 1‐2 biologists Design Synthesis – Time frame – 6‐12 months lead generation – 1‐2 years lead optimization – Client owns 100% of the IP Analysis Test – Included in FTE price – Consumables – Literature/patent searching – Waste disposal
  33. 33. Contact Information Dr. Sameeh Salama Senior Director,  Business Development Dr. Chris Diaper  Business Development  Associate NAEJA Pharmaceutical Inc. 4290‐91A Street, Edmonton Alberta, Canada.  T6E 5V2 Tel: (780) 462‐4044 Fax: (780) 461‐0196 E‐mail: info@naeja.com
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