Relay Therapeutics Receives Breakthrough Therapy Designation for Zovegalisib for the Treatment of Advanced Breast Cancer
Relay Therapeutics has introduced zovegalisib for the treatment of patients with PIK3CA-mutant, hormone receptor-positive, HER2-negative advanced breast cancer, a common subtype of breast cancer characterised by mutations that promote tumour growth and progression.
Zovegalisib is a small molecule therapy designed to selectively target PI3Kα mutations, which are present in a significant proportion of patients with this type of breast cancer. By focusing on mutant forms of the enzyme, the therapy aims to improve tumour control while reducing the limitations associated with earlier treatments.
The designation is supported by clinical data from the Phase 1/2 ReDiscover trial, which is evaluating the safety, tolerability and early efficacy of zovegalisib in combination with fulvestrant, with or without CDK inhibitors. Results to date have shown encouraging anti-tumour activity across different dosing approaches, supporting continued development.
Further evaluation is ongoing in the Phase 3 ReDiscover-2 study, which is assessing zovegalisib at the selected dose in patients with advanced breast cancer. Additional clinical data are expected to be presented at upcoming scientific meetings.
Hormone receptor-positive, HER2-negative breast cancer is the most common subtype of breast cancer. Around 40 per cent of patients carry PIK3CA mutations, which are linked to tumour growth and poorer outcomes. Although CDK4/6 inhibitors combined with endocrine therapy are widely used, many patients experience disease progression, highlighting the need for new treatment options.
Zovegalisib has been developed using Relay Therapeutics’ Dynamo® platform and is designed as an allosteric, mutant-selective PI3Kα inhibitor. This approach aims to overcome the limitations of earlier PI3K inhibitors, which often lacked selectivity and were associated with safety concerns. The therapy is currently being studied across multiple clinical programmes in breast cancer and other conditions linked to PI3Kα mutations.
