20140828 future chemistry pieter nieuwland

FutureCh

emistry

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

FutureCh

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Our design philosophy

• Easy and fast set‐up• ‘Understanding on first sight’• Modularity

Inline analysis Gas‐liquid Photo chemistry

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Flow chemistry: an enabling technology

Nanoparticles

Pharmaceuticals

PET tracers Key activities‐ Flow chemistry instruments ‐ PET tracer for imaging‐ New chemical products

PorousGelatinParticles

FutureCh

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FutureChemistry’s FlowSafe

Patents pending

FF+DC

FF

Efficient chemistry Accelerate R&D Compliance

18FLT

Radio tracer report

Example: Fluorothymidine (18FLT) Target: High proliferating cells Mode:  DNA synthesis

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0,00 5,00 10,00 15,00 min

RAD

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0,50

1,00 CPS *1000

Reg #1

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UV_A (215 nm)

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2,00mAU *1000Required:

radiochemical purity >95% [18F]‐fluoride <5% Specific activity >3.750 GBq/mmol [K222] <25 µg/mL Acidity pH = 6‐8

Showcase:FLT‐Production with FlowSafe (known tracer)

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

FutureCh

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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)

PET/CT imaging (known tracer)

ConfidentialFigure 2: PET/CT image

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Current trajectory

Discovery Preclinical Clinical (I-III)

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• Costs add up from preclinical phase• Earlier selection leads to cost reduction and better value creation

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Current method

Drug candidate Radio tracer Molecular Imaging

ProsEarly decision makingLogical step to clinicalLess experimentsHigh sensitivity and resolution

ConsLong development neededHigh direct costs

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New method

+ =

‘Time to Image’

tot 2014 2015

6‐9 monts 2‐4 weeks

ProsEarly decision makingLogical step to clinicalLess experimentsHigh sensitivity and resolution

SolutionShorter developmentLower direct costsUnique methodIntellectual property

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Improved trajectory

Discovery Prekliniek Kliniek (I-III)

• Earlier ‘funneling’ reduces unnecessary leads

5 110,00010,000

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Accelerating drug development by fast radiolabelling

Focus:  

Shorter development cycles for implementation and development of PET‐tracers

Production for pre‐clinical imaging 

DC1 DC1FF FF

FF FF =18F=19F

Drug Candidate  Tracer ProductionFast Tracer Development PET imaging studies

Patents pending

FF+

= drug candidateDC1FF

FutureCh

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Molecular imaging service

Molecular Labeling (18F) Administration

Molecular imaging

Biomolecule orsmall molecule

FutureChemistry

Drug Developer

Question: where will my new drug candidate/biomarker be distributed in vivo?  

Biodistribution data

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Time‐to‐image:Accelerating  drug development 

TTI wordt mede mogelijk gemaakt dankzij een bijdrage  uit het 

Europese Fonds voor Regionale Ontwikkeling (EFRO)

FutureCh

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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.

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genome-wide approaches

gnawing

DNA 

RNA

(phospho)protein

HDAC inhibitors are candidates asschizophrenia drugs

molecular profiles

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Molecular imaging service

Molecular Labeling (18F)

Administration

Molecular imaging

Biomolecule orsmall molecule

FutureChemistry

Drug Developer

Biodistribution data

Radboud Translational Medicine B.V.

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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

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Challenges

• Meet strict timelines• Offer contract research, while balancing flexibility and 

cost‐effective routine• Increase awareness of benefits of imaging• Build up credibility

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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