2. 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

3. FutureChemistry Our design philosophy
• Easy and fast set‐up
• ‘Understanding on first sight’
• Modularity
Inline analysis Gas‐liquid Photo chemistry

4. 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

5. 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

6. 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

7. 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

8. 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

9. 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

10. 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

11. FutureChemistry Improved trajectory
Discovery Prekliniek Kliniek (I-III)
10,000 5 1
• Earlier ‘funneling’ reduces unnecessary leads

12. 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

13. 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

14. FutureChemistry Time‐to‐image:
Accelerating drug development
TTI wordt mede mogelijk gemaakt
dankzij een bijdrage uit het
Europese Fonds voor Regionale
Ontwikkeling (EFRO)

15. 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

16. FutureChemistry Molecular imaging service
Molecular
Labeling (18F)
Drug Developer
Administration
Molecular imaging
Biomolecule or
small molecule
FutureChemistry
Biodistribution data
Radboud Translational Medicine B.V.

17. 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

18. 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

19. w w w . f u t u r e c h e m i s t r y . c o m
p.nieuwland@futurechemistry.com