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capivasertib + ribociclib + fulvestrant
- Development stage
- Phase 3
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
Capivasertib + ribociclib + fulvestrant is an investigational combination regimen being studied in patients with hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) locally advanced, unresectable, or metastatic breast cancer. Capivasertib is an oral small molecule inhibitor of the serine/threonine kinase AKT, a critical component of the PI3K/AKT pathway, often altered in breast cancers through PIK3CA, AKT1, or PTEN mutations. Ribociclib is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6) that blocks cell cycle progression. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds, blocks, and degrades the estrogen receptor (ER), inhibiting estrogen signaling in breast cancer cells. Together, this triplet regimen aims to overcome therapeutic resistance and prolong progression-free survival in HR+/HER2- breast cancer. The combination is being studied in the CAPItello-292 trial (NCT04862663)[1][3][5][7][8].
02
Targets
AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT2 (Rac-beta serine/threonine-protein kinase)AKT3 (RAC-gamma serine/threonine-protein kinase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)
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