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20140828 future chemistry pieter nieuwland

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20140828 future chemistry pieter nieuwland

  1. 1. FutureChemistry FutureChemistry Holding BV Incorporated December 2007 100% privately owned Housed in Mercator III; assembly, laboratory and office facilities Collaborations with Radboud University and Radboudumc Focus on exploiting flow chemistry Confidential
  2. 2. FutureChemistry Our design philosophy • Easy and fast set‐up • ‘Understanding on first sight’ • Modularity Inline analysis Gas‐liquid Photo chemistry
  3. 3. FutureChemistry Flow chemistry: an enabling technology Nanoparticles Pharmaceuticals PET tracers Key activities Porous Gelatin Particles ‐ Flow chemistry instruments ‐ PET tracer for imaging ‐ New chemical products
  4. 4. FutureChemistry FutureChemistry’s FlowSafe Patents pending + F DC F  Efficient chemistry  Accelerate R&D  Compliance 18FLT Radio tracer report  Example: Fluorothymidine (18FLT)  Target: High proliferating cells  Mode: DNA synthesis
  5. 5. FutureChemistry Showcase: FLT‐Production with FlowSafe (known tracer) UV_A (215 nm) mAU *1000 Required: 2,00 0,00 0,00 5,00 10,00 15,00 min RAD 1,00 CPS *1000 0,50 0,00 Reg #1 0,00 5,00 10,00 15,00 min  radiochemical purity >95%  [18F]‐fluoride <5%  Specific activity >3.750 GBq/mmol  [K222] <25 μg/mL  Acidity pH = 6‐8  Ready for injection into subject Results:  Starting activity 2.5 GBq (68 mCi)  Radiochemical yield 95%  Radiochemical purity >99%  Quantity 150 MBq (4 mCi) (non corrected)  Volume 0.3 mL  Specific activity 5.760 GBq/mmol  [K222] <25 μg/mL  Acidity pH = 6.7  Production time (including purification) 90 min Figure 1: HPLC‐profile of FLT
  6. 6. FutureChemistry PET/CT imaging (known tracer) Study design:  Biodistribution in mice having a FaDu tumor  FLT‐uptake after 45 minutes  PET/CT image (20 min)  Injection 10.0 MBq/0.2 mL 0.9% NaCl (270 μCi) Confidential Figure 2: PET/CT image
  7. 7. FutureChemistry Current trajectory Discovery Preclinical Clinical (I-III) 10,000 100 5 1 • Costs add up from preclinical phase • Earlier selection leads to cost reduction and better value creation
  8. 8. FutureChemistry Current method Drug candidate Radio tracer Molecular Imaging Pros Early decision making Logical step to clinical Less experiments High sensitivity and resolution Cons Long development needed High direct costs
  9. 9. FutureChemistry New method + = ‘Time to Image’ tot 2014 2015 6‐9 monts 2‐4 weeks Pros Early decision making Logical step to clinical Less experiments High sensitivity and resolution Solution Shorter development Lower direct costs Unique method Intellectual property
  10. 10. FutureChemistry Improved trajectory Discovery Prekliniek Kliniek (I-III) 10,000 5 1 • Earlier ‘funneling’ reduces unnecessary leads
  11. 11. FutureChemistry Accelerating drug development by fast radiolabelling F F DC1 DC1 Drug Candidate Fast Tracer Development Tracer Production PET imaging studies Focus: Shorter development cycles for implementation and development of PET‐tracers Production for pre‐clinical imaging F =19F F =18F Patents pending + F F DC1 = drug candidate
  12. 12. FutureChemistry Molecular imaging service Question: where will my new drug candidate/biomarker be distributed in vivo? Drug Developer Molecular Labeling (18F) Administration Molecular imaging Biomolecule or small molecule FutureChemistry Biodistribution data
  13. 13. FutureChemistry Time‐to‐image: Accelerating drug development TTI wordt mede mogelijk gemaakt dankzij een bijdrage uit het Europese Fonds voor Regionale Ontwikkeling (EFRO)
  14. 14. FutureChemistry Imaging for schizophrenia GOAL: Synthesize a radiotracer of an HDAC inhibitor and identify the locations of this radiotracer in the APO‐SUS and APO‐UNSUS rats through PET imaging, and determine its bioavailability and biodistribution in the brain. K 15 genome-wide approaches gnawing DNA RNA (phospho)protein molecular profiles HDAC inhibitors are candidates as schizophrenia drugs
  15. 15. FutureChemistry Molecular imaging service Molecular Labeling (18F) Drug Developer Administration Molecular imaging Biomolecule or small molecule FutureChemistry Biodistribution data Radboud Translational Medicine B.V.
  16. 16. FutureChemistry Ambitions • Offer FAST access to radiolabelled compounds and imaging • Make preclinical imaging much more attractive as an early drug development tool • Allow drug developers to make decisions in an earlier stage K 17
  17. 17. FutureChemistry Challenges • Meet strict timelines • Offer contract research, while balancing flexibility and cost‐effective routine • Increase awareness of benefits of imaging • Build up credibility K 18
  18. 18. w w w . f u t u r e c h e m i s t r y . c o m