Carbon-14 Labelled Peptide APIsSolid Phase Peptide Synthesis, BIOTINylation & PEGylation

Dr Sean KitsonInvestigator of Radiochemisty

sean.kitson@almacgroup.com

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