Abstract
The continuing advancements in bioconjugate medicines from delivery of potent cytotoxins to vaccine-, oligonucleotide-, radionuclide-, immunomodulator- and check-point inhibitor-conjugates, can start to address the large unmet medical need currently unattainable from current therapeutic approaches. As the field of bioconjugation develops, and the recent spate of antibody-drug conjugates (ADCs) approvals continues, the resulting knock-on effects for delivering a wider range of bioconjugated molecules will also continue to expand in utility.

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Authors: Mark Frigerio, Ph.D* and Fuan Kang, Ph.D.

Corresponding Author: Mark Frigerio, Ph.D., Vice President, Design and Development, Abzena, Babraham Research Campus, Cambridge, CB22 3AT, United Kingdom +44 1223 903498 E-mail: [email protected]

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Key terms: ADC, bioconjugation, therapeutic effect, manufacturing, oligonucleotides
Published In: ADC Review| Journal of Antibody-drug Conjugates

DOI: https://doi.org/10.14229/jadc.2020.04.08.001.


How to cite:
Frigerio M, Kang F. Addressing the Challenges of Bioconjugate Medicines – J. ADC. April 8, 2020. DOI: 10.14229/jadc.2020.04.08.001.


Last Editorial Review: April 8, 2020

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Article History:

  • Original Manuscript Received March 23, 2020
  • Review results received April 1, 2020
  • Manuscript accepted for publication April 6, 2020

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Mark Frigerio received his Ph.D. from University College London in 2003. His postgraduate research in the laboratory of Professor Karl Hale was synthesizing the antitumor macrolide Bryostatins resulting in the enantioselective formal total synthesis of Bryostatin 7. His drug development experience includes working as team leader at KuDOS Pharmaceuticals on targeting the DNA-PK and ATM kinases involved in double-strand DNA-damage repair pathways implicated in the treatment of cancers, at Pharminox developing G-Quadruplex binders targeting the non-canonical forms of DNA, as well as developing next-generation Temozolomide analogs designed to overcome the alkylation resistance mechanisms. Mark joined PolyTherics/Abzena in 2012 and his initial role focussed on the bioconjugation development of Antibody Drug Conjugates (ADCs). He is an expert in the design and development of ADC linkers and has been instrumental in building Abzena’s site-specific ThioBridge® conjugation technology platform for the production of stable and homogeneous ADCs, as well as Abzena’s site-specific polymer PEGylation linker technology, including TheraPEG™, CyPEG™, and HiPEG™, for the half-life extension of peptides and proteins. Mark has 37 publications and patents in the field of early-stage drug discovery and his focus in developability assessment has led to him taking a broader role in Abzena as VP Design and Development, responsible for the business operations of early-stage antibody and ADC drug developability programs.
Fu-An Kang, Ph.D., is an accomplished synthetic, medicinal and process scientist and expert with extensive experiences in chemical and pharmaceutical research and development. After he obtained his Ph.D. in Organic Chemistry at Beijing Normal University in China, he joined Professor Yoshito Kishi’s group at Harvard University for his postdoc research in 1999. He developed the asymmetric Ni/Cr coupling methodology and contributed to the practical synthesis of the Halichondrin derived anticancer drug Eribulin (Halaven, approved in 2010) in the Harvard-Eisai collaboration. He joined Johnson & Johnson PRD in 2002 and worked on various therapeutic areas with demonstrated expertise ranging from drug discovery to drug development. He discovered a novel series of oxa-mifepristone-like steroids as highly selective progesterone receptor modulators, which are potentially useful for breast cancer treatment. His contribution to the chemical development of the SGLT2 inhibitor Canagliflozin (Invokana, approved in 2013) to treat type 2 diabetes received a Johnson & Johnson Platinum Encore Award. He discovered and developed the “Phosphonium Coupling”, a new chemical methodology for the direct arylation of tautomerizable heterocycles, which has found many applications in medicinal chemistry, process chemistry and material sciences in recent years. He also published an interesting mathematical interpretation for the classical empirical “Woodward UV Rules”. Since 2011, he has moved into the CRO/CMO/PRO industry as senior managers for the research, development and cGMP manufacturing of pharmaceuticals. He served as CSO at Santai Labs in China, and VP at Wilmington Pharmatech in the US. He joined TCRS/Abzena in 2015 and currently serves as Senior Director of Chemistry overseeing the research and development of medicinal compounds, API KG production, material synthesis, and ADC payload development. He has over 50 scientific publications in journals and patents.