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Posters – Immunology and Oncology NAME OF THE PROJECT NAME OF THE MAIN CONTACT ORGANISATION NAME Bio-specific and Bio-stable Reagent for Thiols Ligation Jérémie Fournier SATT Conectus Alsace Technology APN technology allows modification of native biomolecules through reaction with cysteine residues of proteins and antibodies. Conjugates formed by this technology were shown to be more stable in plasma and inside cells comparing to maleimide conjugates that are currently used in the majority of Antibody-Drug Conjugates (ADC) therapies. This stability is of crucial importance for biomedical applications as it can substantially increase therapeutic index of new ADCs. Customers / Target market The market of Antibody-Drug Conjugates is in its dawn with only 2 recently approved drugs: Kadcyla and Adcetris. The worldwide sales of ADCs are estimated to reach $2.8B by 2018. The clinical pipeline is growing at an increasing rate and currently includes more than 40 drug candidates. Technology providers play crucial role in this market as illustrated by the substantial increase in upfront (from $3M to $20M average) and milestone (from $38M to $240M average) payments received by these companies since 2005. Today’s market of conjugation technologies for the preparation of ADC is mainly represented by two technology providers: ImmunoGen and Seattle Genetics. Their conjugation technologies are used in 90% of ADCs in the clinical development. Industry and competitors Financing need / Commercial opportunity IP – Patent situation The technologies of both leading technology providers are based on the maleimide-thiol conjugation chemistry. However, the resulting conjugates were recently shown to have limited in vivo stability, which leads to premature release of the toxic payload. This increases the off-target toxicity of the ADCs and causes a variety of severe side effects. Conectus Alsace will transfer an exclusive licence to the start-up company Syndivia. This company seeks 1.5M Eur in equity financing in order to carry on with the preclinical development of its lead candidate and to develop the pipeline of partnered drug candidates. An European patent application was filed on 4th of July 2013 and a PCT international application was filed on 4th of July 2014. This application was published under the reference WO2015001117. The start-up company (Syndivia) will be granted an exclusive worldwide license for the APN technology Future steps / Milestones The technology will be licensed to the start-up company (Syndivia) which seeks for partnerships and co-development opportunities with: 1. Biotechnology and pharmaceutical companies interested in entering the ADC market. 2. Companies developing therapeutic monoclonal antibodies. 3. Companies developing cytotoxic compounds. 1) www.syndivia.com Further reading 2) Koniev, O., et al. (2014) Selective irreversible chemical tagging of cysteine with 3arylpropiolonitriles. Bioconjug. Chem. 25, 202–206. 3) Kolodych, S., et al. (2015) CBTF: New Amine-to-Thiol Coupling Reagent for Preparation of Antibody Conjugates with Increased Plasma Stability. Bioconjug. Chem. 26, 197–200. 4) Koniev, O., et al. (2015) MAPN: First-in-Class Reagent for Kinetically Resolved Thiol-toThiol Conjugation. Bioconjug. Chem. 26, 1863–1867. Contact person Jérémie Fournier, PhD, Project [email protected] 1/2 leader, SATT Conectus Alsace