# Zovegalisib

Source: https://onco.cc/drugs/zovegalisib/  
OnCo record `zovegalisib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

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.

## Summary

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.

## Fields

- Kind: Treatment
- Status: phase-3
- Last checked: 2026-09-11
- Tags: pipeline; ctgov-ingest
- Modality: small molecule
- Mechanism: 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.

## Sources

- ClinicalTrials.gov: trials of Zovegalisib: https://clinicaltrials.gov/search?intr=Zovegalisib
- Sponsor pipeline page: https://relaytx.com/pipeline/

## Connected records

- cancers: [HR-positive / HER2-negative breast cancer](https://onco.cc/cancers/breast-hr-positive/)
- targets: [PIK3CA / PI3K-alpha](https://onco.cc/targets/pik3ca/)
- companies: [Relay Therapeutics](https://onco.cc/companies/relay-therapeutics/)
- trials: [Phase 3 Study of RLY-2608 + Fulvestrant vs Capivasertib + Fulvestrant as Treatment for Locally Advanced or Metastatic PIK3CA-mutant HR+/HER2- Breast Cancer](https://onco.cc/trials/nct06982521/)

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