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Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012
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Carbon-14 Labelled APIs - Sean Kitson, Biotrinity 2012

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Workshop presentation given by Sean Kitson, Investigator of Radiochemistry at Almac at Biotrinity April 2012

Workshop presentation given by Sean Kitson, Investigator of Radiochemistry at Almac at Biotrinity April 2012

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  • 1. Carbon-14 Labelled Peptide APIsSolid Phase Peptide Synthesis, BIOTINylation & PEGylation Dr Sean Kitson Investigator of Radiochemisty sean.kitson@almacgroup.com
  • 2. 14 C Labelled Drugs • A critical element of the development of any drug is an assessment of its ADME profile, most commonly performed using 14C labelled versions of the parent drug • For peptide labelling there are other options such as tritium labelling or radio-iodinationS L Kitson. Accelerated Radiochemistry, PMPS Manufacturing, pp. 68-70, 2010
  • 3. 14 C Peptides• One clear benefit of using a 14C for the ADME programme is the fact that the label is placed within the core of the drug, without any risk of wash out or need to use a modified structure 14C
  • 4. 14 C Peptides• One limitation of 14C is its rather modest maximum specific activity (62 mCi/mmol), a limitation that becomes ever more significant as the molecular weight of the molecule increases• This limitation can be overcome through the use of Accelerated Mass Spectrometry (AMS)
  • 5. 14 C Peptide StrategyS L Kitson. Keeping Tags on Biomolecules, Manufacturing Chemist April 2012
  • 6. API Development & Supply: Peptides • Non-GMP Custom Synthesis • GMP Manufacture – Bulk supply • Expertise in Difficult Peptides – Long sequences – Hydrophobic peptides – Conjugates • PEGylation
  • 7. Isotope LabellingAlmac can...• Synthesise• Label• Formulate...any small molecule or peptide• MHRA audited for 14C IMP• Doubled capacity in 2010

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