How ELF can boost SME drug discovery programmes: examples from the chronic pain disease area

News
08 January 2021

The focus of the second European Lead Factory (ELF) webinar, which took place on Thursday 10 December, was on small and medium-sized enterprises (SMEs) and how ELF can help SMEs achieve their drug discovery ambitions.

The keynote speakers for the session were Dermott O’Callaghan, Consulting Scientist at The Research Network (TRN) and Graeme Wilkinson, Head of Virtual Drug Discovery at Medicines Discovery Catapult & former Pharmacologist at TRN. To showcase the potential and relevance of the ELF drug discovery platform and how it can be of benefit to SMEs, Dermott and Graeme talked the audience through their experience of working with ELF. In particular, they explained how ELF has helped TRN programmes progress, with a focus on two programmes to do with the central nervous system and compounds that modulate pain.

TRN looked to ELF to generate lead matter of therapeutic interest to move towards a drug candidate. As a result of the collaboration with ELF, two lead generation campaigns were established. During the webinar, Dermott and Graeme described the assay development process and the lessons learned along the way.

"Without ELF, we wouldn’t have reached the stage we’re at now with great starting points for optimisation," said Graeme.

"We came out with not just improved, but excellent tools to demonstrate the approach to follow for target validation. We have used these tools to generate high-quality lead matter, which can be further developed.”

Commenting on the process, Dermott said: "Overall, it was a very exciting collaboration that progressed well. Thanks to the European Lead Factory, we attained a series of extraordinarily good compounds for progression towards candidate nomination. The momentum within the project was excellent – rapid and efficient. In particular, the hit to lead follow-up was really good.”

In terms of where to go from here with these molecules, Dermott and Graeme emphasised that there is a wide variety of unmet medical need when it comes to chronic pain and noxious stimuli –from visceral pain itself, all the way through to itch and sensations of pruritus.

"We believe that both of these targets can be involved in reducing the threshold for sensation with the opportunity, ultimately, to move forward to the clinic to relieve pain and itch due to pruritus. The next step will be a lead optimisation campaign for both targets, exploitation of the chemistry, and de-risking to clinical candidate. We look forward to continuing to work with ELF and the EFPIA partners,” concluded Graeme.

The next ELF webinar will take place on Thursday 28 January from 11:00-12:00 (CET) and will focus on assay optimisation for High Throughput Screening and how to meet the ELF requirements. Registration for this and future ELF webinars is free via this link.