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International Research for Global Health NAEJA Pharmaceutical Inc. INTEGRATED MEDICINAL CHEMISTRY.

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Presentation on theme: "International Research for Global Health NAEJA Pharmaceutical Inc. INTEGRATED MEDICINAL CHEMISTRY."— Presentation transcript:

1 International Research for Global Health NAEJA Pharmaceutical Inc. INTEGRATED MEDICINAL CHEMISTRY

2 Drug discovery Contract Research Organization (CRO) Previously SynPhar Privately owned 63,000 ft 2 facility Based in Edmonton, Canada

3

4 Core Expertise Pre-Clinical Development HIT Validation Lead Identification Lead Optimization Target Validation IND & Clinical Trials

5 Track Record

6 Success Stories: Anti-infectives Tazobactam Design, Synthesis, & Screening of -Lactamase Inhibitor 4 Year Program Collaboration with Taiho Pharmaceuticals Marketed by Wyeth SYNPHAR TAIHO HIT Validation IND & Clinical Trials Lead Identification Lead Optimization

7 HIT Validation Lead Identification Lead Optimization IND & Clinical Trials Success Stories: Inflammation Mofezolac (Disopain TM ) Design & Synthesis of NSAID 4 Year Program Collaboration with Taiho Pharmaceuticals Marketed by Mitsubishi Pharmaceuticals SYNPHAR TAIHO

8 NAEJA Track Record Past 5 Years* *(% revenue) Large Pharma Biotech Longest collaboration 12 years Longest contract 4 years New market 2008 Multiple projects & clients Proven IP security

9 Single Client – Multiple Programs Anti-infectives & inflammation NAEJA Hit Generation and Validation Hit to Lead Lead Optimization Candidate CLIENT Phase 2 Phase 2b Phase 1: 2009 On hold: biological liability Candidate selection: 2009 Lead declaration { One program

10 Project starts: Q1 Hit structure: narrow activity spectrum Racemic Limited SAR Undeveloped chemistry: unusual scaffold No crystal structure Project starts: Q1 Hit structure: narrow activity spectrum Racemic Limited SAR Undeveloped chemistry: unusual scaffold No crystal structure Q3: Crystal structure Q1: ½ Kg pre-candidate synthesized Q1: ½ Kg pre-candidate synthesized Candidate declaration >98% purity >98% eefffff Candidate declaration >98% purity >98% eefffff Q4: Racemic lead #1 declared Q4: Racemic lead #1 declared Q1: Validated thigh model Q1: Validated thigh model Q3: Pre-candidate #1 put on hold: biological liability Q3: Pre-candidate #1 put on hold: biological liability Q1: Chemistry development, SAR, MIC panel Q1: Process development Q2: chiral HPLC Q1: ADME Q1: Racemic lead #2 declared Q3: Molecular modeling & SBDD CASE STUDY Anti-infective Program = NAEJA = CLIENT

11 Successful Recent Programs NAEJA Hit Generation and Validation Hit to Lead Lead Optimization Candidate Phase 1b/2: Cardiovascular disease Clinical trials: anti-fungal Alzheimer's program Anti-viral program Clinical trials: Pain management Clinical trials: anti-bacterial

12 Medicinal Chemistry Projects Papers 42 Patents 19 Papers 15 Patents 4 Papers 2 Patents 5 Papers 20 Patents 5 Papers 5 Patents 1 Papers 3 Papers 4 Patents 10 Papers 4 Patents 9

13 Services

14 Chemistry Services Full FTE: medicinal, synthetic, and process chemists. Medicinal chemistry programs: hit to candidate including process development (22 L). Custom synthesis. Chemical Information Support SciFinder, Reaxys, ACS journals online, NERAC, & CISTI.

15 NAEJA FTEs Director 100% PhDs Project Coordinator 100% PhDs Scientist 90% PhDs Staffing Chemistry: 71% Biology: 7% Analytical: 5% Admin: 17% PhDs & Postdocs by Training Location

16 Locations of Ph.D.s and Postdocs

17 Computational Chemistry Services Hit Discovery:ligand docking Sybyl, Glide/ pharmacophore generation Schrödinger Lead Optimization: ligand docking Sybyl, Glide/ QSAR Schrödinger Physical Properties: pKa, log P, log D, & solubility ACD software

18 Analytical Support: HPLC Separation & Purification WATERS Autopurification System WATERS PREP HPLC: routine scale: mg WATERS LC Module Plus: semi-prep NP/chiral; mg Analysis WATERS 600 Series Chiral analysis (CHIRALPAK-AD, AD-RH, OD, OD-R, OF, OB, OJ) LC-MS WATERS- Micromass ZQ LC/MS (EI & APcI) WATERS- Acquity LC/MS (Sample Manager; PDA Detector & SQ Mass Detector)

19 MIC Determination: NCCLS standard procedures & ATCC reference strain - Bacterial panels include Gram-positive, Gram-negative, and anerobes - Fungal panels include yeast and filamentous fungi Cross-resistance studies - Panels of strains expressing drug resistance mechanisms De novo resistance development studies Kill time studies Microbiology – in vitro studies

20 Post-antimicrobial effect (PAE) studies Effect of body milieus on activity Determination of activity on recently collected clinical isolates - Collection of over 4000 bacterial and fungal clinical isolates High-throughput screening of activity - Beckman 2000 automated workstation Drug-drug interaction studies Microbiology – in vitro studies

21 Bioavailability/Pharmacokinetics : in vitro testing parameters Aqueous solubility Partition coefficient (log D, n-octanol/PBS, pH 7.4) Plasma protein binding (ultrafiltration) A-B Permeability (MDCK) Metabolic stability (human liver microsomes, hepatocytes) UPLC-MS-MS Screen Drug Safety and Development: in vitro testing parameters Cytochrome P450 inhibition Cytochrome P450 induction

22 Animal Facilities (CCAC)* Capacity: Conventional housing Level II biohazard 200 mice/40 rats - PK 200 mice/24 rats – efficacy Preclinical PK: in vivo metabolism, preliminary acute & sub acute toxicology Bioavailablity studies (including preformulation using cosolvents) Blood/plasma concentrations (AUC, t ½, C max, CL, & V d ) Tissue concentration/distribution In vivo metabolite profiling Acute & sub acute toxicological evaluation in rodents *CCAC – Canadian Council of Animal Care

23 The NAEJA Package Included in the price of an FTE: Consumables Patent/literature searches (SciFinder, Reaxys, NERAC) Waste disposal (overseen by safety committee, SOPs in place) IP 100% owned by the client (confidentiality SOP in place)

24 NAEJA Summary Experience 22 year track record in drug discovery. Collaborations with over 125 pharmaceutical companies. Delivered candidates in a number of therapeutic areas. Expertise 90% of our research scientists are PhDs. Services Pre-clinical discovery Custom services to full range medicinal chemistry programs.

25 Contact Information Dr Sameeh SalamaDr Chris Diaper Senior DirectorAssociate Business & Development NAEJA Pharmaceutical Inc A Street, Edmonton, Alberta, Canada. T6E 5V2 Tel: (780) ; Fax: (780)


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