CHISHIKI

Drug Discovery

Discovery of HTL0039732: A Potent and Selective EP4 Receptor Antagonist for Cancer Immunotherapy

By Nigel Swain | Aug 7, 2022

Nigel Swain, a senior director in our Medicinal Chemistry department, recently presented at the 2022 Medicinal Chemistry Gordon Research Conference, showcasing rational design using Structure Based Drug Design (SBDD) and X-ray crystallography of the Sosei Heptares EP4 receptor antagonist preclinical candidate HTL0039732.

 

Conference

2022 Medicinal Chemistry Gordon Research Conference

7 – 11 August 2022

New London, NH, USA

 

Summary

Development of selective and potent prostaglandin EP4 receptor antagonists hold great potential for cancer immunotherapy. Prostaglandin E2 (PGE2) mediated signalling through EP4 can trigger cancer cells to evade the immune system and can also influence tumour cell growth. Therefore, blocking this type of receptor may improve patient survival, especially if used in combination with another immunotherapy. 

The presentation includes a first disclosure of the Sosei Heptares EP4 receptor antagonist preclinical candidate HTL0039732, showcasing rational design using Structure Based Drug Design (SBDD) and X-ray crystallography.  Data supporting its potential as a best-in-class EP4 antagonist for a wide range of cancers will be presented.