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zovegalisib + atirmociclib
- Development stage
- Unknown
- Lead developer
- Relay Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Zovegalisib + atirmociclib is an investigational, all-oral combination regimen consisting of zovegalisib (RLY-2608), a mutant-selective allosteric inhibitor of phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha (PI3Kα), and atirmociclib (PF-07220060), a selective cyclin-dependent kinase 4 (CDK4) inhibitor. Developed by Relay Therapeutics and Pfizer, this combination is designed to treat patients with PIK3CA-mutated, hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. By selectively targeting mutated PI3Kα and CDK4 while sparing wild-type PI3Kα and CDK6, the regimen aims to maximize antitumor efficacy and overcome endocrine resistance while minimizing class-associated toxicities such as hyperglycemia and neutropenia. The combination is being evaluated in the Phase 1/2 ReDiscover trial and is planned to enter Phase 3 clinical development in early 2027.
- Other names
- PF-07220060 + RLY-2608RLY-2608 + PF-07220060atirmociclib + zovegalisib
02
Targets
CDK4 (Cyclin-dependent kinase 4)PIK3CA (Phosphoinositide 3-kinase alpha)
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