Aptamers as inhibitors of target proteins

Abstract

Background: Aptamers as inhibitors of proteins in therapeutic applications offer great advantages over their antibody counterparts and the promise to be developed into the next generation therapeutic agents. However, the control of aptamer intellectual property (IP) by two major players has made aptamers an area difficult to operate and often off-putting for academic and commercial organisations. Yet, their great potential is keeping aptamers at the research forefront, with one aptamer in the clinic and various at different stages of clinical trials. Objective: To provide a comprehensive review of the aptamer IP landscape and the issues associated with aptamer therapeutics against protein targets. Methods: Extensive review of the scientific and patent literature. Conclusions: Following our experience in developing, patenting and commercialising our aptamers against MUC1 and an extensive review of the literature, we have identified a variety of issues pertaining to the development of aptamers against protein targets for therapeutic applications, their patenting and granting of patents, the original IP holders and their policy, as well as the current market and traits. Despite a slow start, aptamers have been developed against various therapeutic proteins and offer the promise of providing a novel generation of therapeutic entities with a variety of applications.

Keywords::

• aptamers
• patents
• SELEX
• therapeutics

Acknowledgements

The authors thank the project team of PLMCS, P Murphy, A Dixon and J Bates, who have assisted and advised on the commercialisation of our MUC1 aptamers and provided useful information, which has in part been utilised in this paper.