carbon-14 labelled apis - sean kitson, biotrinity 2012
DESCRIPTION
Workshop presentation given by Sean Kitson, Investigator of Radiochemistry at Almac at Biotrinity April 2012TRANSCRIPT
Carbon-14 Labelled Peptide APIsSolid Phase Peptide Synthesis, BIOTINylation & PEGylation
Dr Sean KitsonInvestigator of Radiochemisty
14C 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-iodination
S L Kitson. Accelerated Radiochemistry, PMPS Manufacturing, pp. 68-70, 2010
14C 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
14C 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)
14C Peptide Strategy
S L Kitson. Keeping Tags on Biomolecules, Manufacturing Chemist April 2012
API Development & Supply: Peptides
• Non-GMP Custom Synthesis
• GMP Manufacture– Bulk supply
• Expertise in Difficult Peptides– Long sequences– Hydrophobic peptides– Conjugates
• PEGylation
Isotope Labelling
Almac can...• Synthesise• Label• Formulate
...any small molecule or peptide
• MHRA audited for 14C IMP• Doubled capacity in 2010