Zovegalisib

Zovegalisib is a small-molecule drug developed by Relay Therapeutics. Its target is PIK3CA / PI3K-alpha (the sponsor names PI3Kα (mutant-selective)). The sponsor states: Described as the first allosteric, pan-mutant (including kinase-domain mutations such as H1047X and helical-domain mutations such as E542X/E545X) and isoform-selective PI3Kα inhibitor, designed using cryo-EM structural analysis and molecular dynamics simulations to differentiate mutant from wild-type PI3Kα. ClinicalTrials.gov describes the intervention as: 400 mg orally BID administered daily on a 28-day treatment cycle. It is the investigational product in 1 recruiting or active industry-led phase 2 and phase 3 interventional cancer trial, including the phase 3 study NCT06982521 (Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer), in HR-positive / HER2-negative breast cancer. The largest, NCT06982521, plans to enrol 540 participants with primary completion expected 2028-04-30. Status reflects the highest phase registered on ClinicalTrials.gov at the 2026-09-11 check; no efficacy results are recorded here.