Loading
Zovegalisib is an experimental small-molecule drug from Relay Therapeutics in phase 3 trials for HR-positive / HER2-negative breast cancer, aimed at PIK3CA / PI3K-alpha.
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; no efficacy results are recorded here.
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. Connects to PIK3CA / PI3K-alpha.
1.Zovegalisib slips into a pocket on PIK3CA / PI3K-alpha.
Country and place are remembered in this browser only. A postcode is sent to OpenStreetMap's Nominatim service to find coordinates when you press the button; nothing else leaves your device.
Query for this drug: (TITLE:"Zovegalisib" OR ABSTRACT:"Zovegalisib") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Zovegalisib, not a curated reading list.
Shares PIK3CA / PI3K-alpha, HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares PIK3CA / PI3K-alpha, HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.
Shares HR-positive / HER2-negative breast cancer and the tag pipeline.