The A2a receptor antagonist, which is in development for adult patients with advanced solid tumours, was co-invented and developed through a joint venture between Exscientia and Evotec, including application of Exscientia’s AI-design platform, as part of Centaur Chemist.
The new drug candidate brings the possibility of high selectivity for the target receptor, bringing together potential benefits of reduced systemic sides effects, as well as minimal brain exposure to avoid undesired psychological side effects.
Exscientia’s AI-designed A2a receptor antagonist is being investigated for its ability to prevent adenosine, which is produced by tumour cells and minimises immune system detection, from binding to the T-cell receptor, and potentially promote anti-tumour T-cell activity.
Pre-clinical data related to the project will be presented at the American Association for Cancer Research (AACR) annual meeting, to be held from the 9th-14th April 2021.
The announcement from Exscientia follows a previous venture, carried out alongside Sumitomo Dainippon Pharma, which saw the first AI-designed candidate for treating obsessive-compulsive disorder (OCD) go into clinical trials.
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“Immuno-oncology medicines are bringing benefit to a range of cancer patients,” said Andrew Hopkins, CEO of Exscientia.
“Our selective A2a receptor antagonist addresses a next-generation immuno-oncology strategy to empower the human immune system by reversing the effects of high adenosine concentrations.
“We set ambitious therapeutic objectives for this project, especially high selectivity for the A2a receptor and central nervous system (CNS) sparing properties, in order to reduce the likelihood of systemic side effects.
“Even with these challenging objectives, we were able to discover our candidate molecule within 8 months of project initiation.”