Drug intelligence / Profile preview

giredestrant + inavolisib + abemaciclib

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

**Giredestrant + inavolisib + abemaciclib** is an investigational oral combination therapy for **estrogen receptor-positive, HER2-negative, locally advanced or metastatic breast cancer**. - **Giredestrant** is a next-generation, oral, non-steroidal selective estrogen receptor degrader (**SERD**) that antagonizes and degrades the estrogen receptor. - **Inavolisib** is a potent, selective inhibitor of the phosphatidylinositol 3-kinase catalytic subunit alpha (**PIK3CA**), blocking PI3K signaling that is often upregulated in breast cancer. - **Abemaciclib** is a small molecule inhibitor of cyclin-dependent kinase (**CDK**) 4 and 6, which halts cell cycle progression in cancer cells. This triple combination is being studied for its potential to improve outcomes in hormone receptor-positive breast cancer by targeting three critical pathways: estrogen signaling, PI3K/AKT/mTOR pathway, and cell cycle progression[2][4][6].

02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ER (Estrogen receptor)

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