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

1. Carbon-14 Labelled Peptide APIs
Solid 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-iodination
S 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 Strategy
S 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 Labelling
Almac can...
• Synthesise
• Label
• Formulate
...any small molecule or peptide
• MHRA audited for 14C IMP
• Doubled capacity in 2010