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zovegalisib + atirmociclib + aromatase inhibitor
- Development stage
- Unknown
- Lead developer
- Relay Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
zovegalisib + atirmociclib + aromatase inhibitor is an investigational all-oral triplet combination therapy being developed for the treatment of patients with PI3Kα-mutated, hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. The regimen combines zovegalisib (RLY-2608), a mutant-selective allosteric PI3Kα inhibitor developed by Relay Therapeutics, with atirmociclib (PF-07220060), a selective CDK4 inhibitor developed by Pfizer, and an aromatase inhibitor (such as letrozole, anastrozole, or exemestane). By selectively targeting mutated PI3Kα and CDK4 while sparing wild-type PI3Kα and CDK6, the combination aims to maximize antitumor efficacy while minimizing class-associated toxicities like hyperglycemia and neutropenia. The triplet is being evaluated in the Phase 1/2 ReDiscover trial and is planned to enter Phase 3 clinical development in 2027 as a frontline therapy.
- Other names
- RLY-2608 + PF-07220060 + AIRLY-2608 + PF-07220060 + aromatase inhibitorzovegalisib + atirmociclib + AIzovegalisib + atirmociclib + aromatase inhibitor
02
Targets
AKT (RAC-alpha serine/threonine-protein kinase)CCND1 (Cyclin D1)CDK4 (Cyclin-dependent kinase 4)mTOR (Mammalian target of rapamycin kinase)CYP19A1 (Aromatase)PIK3CA (Phosphoinositide 3-kinase alpha)
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