HTL0039732 (also known as NXE0039732), is Nxera’s novel oral EP4 antagonist being investigated to treat a wide range of solid cancers in combination with other immunotherapies.
Cancer Research UK’s Centre for Drug Development is sponsoring and managing the ongoing Phase 1/2a trial of HTL0039732.
Cancer Research UK and Nxera Pharma announce that the first patient has been dosed in a phase 2a clinical trial (NCT05944237) evaluating Nxera’s investigational immunotherapy drug HTL0039732 (also known as NXE0039732) for advanced solid tumours.
The decision to advance to phase 2a follows the successful completion of the phase 1 part of the trial, which identified a safe and well-tolerated dose of HTL0039732 – a novel EP4 antagonist – in combination with checkpoint inhibitor atezolizumab that achieves good engagement of the intended target EP4, without significantly engaging EP2.
Study participants had advanced solid tumours that were resistant or refractory to standard therapy, and the phase 1 trial showed encouraging early efficacy including two confirmed partial responses in two distinct tumour types when administered in combination use with atezolizumab. The phase 1 trial results to date will be presented at the European Society for Medical Oncology Congress (ESMO) 2025 in October.
HTL0039732 is an oral small molecule drug candidate that blocks the signalling through the prostaglandin E2 (PGE2)-type prostanoid receptor 4 (EP4). PGE2 acts in the tumour microenvironment to trigger cancer cells to evade the immune system.
Targeting EP4 to block the effects of PGE2 increases the ability of the immune system to detect and control cancer cells and makes HTL0039732 a potential candidate to treat patients with cancers that generally do not respond well to current immunotherapies.
