Drug Conjugates
Antibody drug conjugates (ADCs)
Antibody drug conjugates (ADCs) are a growing therapeutic modality for oncology applications.
The antibody allows selective targeting of cancer cells while a cytotoxic drug attached to it allows to kill the cells. A linker allows to bind the antibody with the cytotoxic drug.
Fatty acid derivatized peptides or proteins
Fatty acid derivatized peptides or proteins allow to extend therapeutic activity, with examples of peptides having an activity extended from several hours to a week. The lipidic part binds to albumin in the blood, which allows a prolonged release.
A linker is needed to attach the lipidic part to the peptide or protein.
Example of fatty acid derivatized structure: Liraglutide
Proteolysis Targeting Chimeras (PROTACs)
PROTACs are another emerging therapeutic modality allowing to address protein targets previously considered undruggable. Instead of being inhibited, the target protein is degraded. This is achieved using bifunctional compounds which hijack the protein degradation system within the cell. These compounds bind to both the target protein and to the degradation system (ubiquitin E3 ligase), which results in ubiquitinylation of the target protein followed by its degradation.
Example of PROTAC structure:
Such conjugates usually require linkers. Seqens has an expertise in linkers synthesis at required quality (cGMP) and scale, from kilo lab to multi-ton.
Seqens handles the different kinds of chemistry involved in linker synthesis such as ethylene glycol oligomers, amide couplings or piperazine / piperidine chemistry.
Seqens can also leverage on innovative technologies such as Flow chemistry, for safer generation of acyl chlorides or triazoles, or biocatalysis, for regioselective conversions to avoid protection/deprotection steps.