Bioconjugation technology continues to drive pharmaceutical innovation by enabling precise biomolecule modifications that enhance drug performance, targeting, and safety profiles. A recent webinar hosted by Biosynth brought together leading scientists to explore advanced strategies in PEGylation, glycosylation, and peptide conjugation, highlighting the evolving landscape of targeted therapeutics.
PEGylation Addresses Critical Pharmacokinetic Challenges
Dr. Julia Wittmann, Bioconjugation Manager at Biosynth, opened the discussion by examining PEGylation—the attachment of polyethylene glycol (PEG) to biomolecules. The technology addresses a fundamental challenge in drug development: the rapid removal of peptides and small molecules from the body through renal secretion due to their low molecular weight.
"Peptides and small molecules are often rapidly removed from the body by renal secretion due to their low molecular weight," explained Dr. Wittmann. "This means they must be administered frequently and at high doses, which also increases unwanted side effects."
PEGylation offers a solution by increasing drug size upon PEG attachment, effectively slowing renal excretion and resulting in increased half-life with significant reduction in side effects. The technology is particularly well-suited for pharmaceutical applications due to PEG's high water solubility, non-toxic, and non-immunogenic properties, along with its ability to be synthesized in various molecular configurations.
Conjugate Vaccines Enhance Immunogenicity
The webinar emphasized the critical role of conjugate vaccines, where antigens with low or no immune response are conjugated to highly immunogenic carrier proteins. Dr. Wittmann detailed conjugation strategies for linking peptides to carrier proteins, specifically highlighting CRM197, which activates the immune system to recognize bound antigens and increase overall vaccine immunogenicity.
Dr. Hans Streicher, Scientific Advisor at Biosynth, expanded on carbohydrate conjugation strategies, emphasizing their role in biological recognition, drug targeting, and novel materials development. He discussed the glycoconjugate vaccine against H. influenza (Hib), where conjugation with carrier protein hemocyanin was necessary due to the polysaccharide's low immunogenicity alone.
"We want, through conjugation, to combine carbohydrate properties with those of the conjugated moiety," stated Dr. Streicher, highlighting the strategic approach to enhancing therapeutic efficacy through molecular combination.
The Golden Age of Peptide Conjugation
Dr. Laurent Caron, Peptide Market Development Specialist, concluded the webinar by focusing on peptide conjugation techniques. He characterized the current period as "the golden age for peptide bioconjugate tools and applications," exploring both established and emerging conjugation methods.
The discussion covered the complexity of bioconjugation targets and the need for additional modifications. Dr. Caron demonstrated the use of PTAD (4-phenyl-3H-1,2,4-triazole-3,5(4H)-dione) as a reagent for targeting tyrosine residues, with capacity for additional modifications when needed. He emphasized the importance of designing conjugation strategies economically, from reagent sourcing through conjugation implementation.
Comprehensive Service Portfolio
Biosynth offers bioconjugation services across all stages of bioconjugate development, partnering with clients from initial feasibility studies through process and analytical method development to GMP manufacturing. The company's expertise spans various conjugation methods, including PEGylation, glycoconjugation, and small molecule or peptide coupling.
The company provides end-to-end solutions in conjugate vaccines and conjugate drugs, activated PEGs, and polymer-based drug delivery excipients from early clinical phases through late clinical phases and regulatory approval. This comprehensive approach addresses the fundamental role of integrated manufacturing and analytical capabilities in transforming bioconjugation technologies from laboratory bench to commercial market.
