Drug intelligence / Profile preview

inavolisib + endocrine therapy

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Inavolisib + endocrine therapy is a combination treatment regimen primarily used for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-), PIK3CA-mutated advanced or metastatic breast cancer. Inavolisib (Itovebi) is a potent and selective small molecule inhibitor of the PI3Kα isoform that also promotes the degradation of the mutant p110α protein. Endocrine therapy (ET) in this context typically refers to selective estrogen receptor degraders (SERDs) like fulvestrant or aromatase inhibitors. The combination is designed to simultaneously target the PI3K and estrogen receptor signaling pathways, which are frequently co-activated in this cancer subtype. In October 2024, the FDA approved inavolisib in combination with palbociclib (a CDK4/6 inhibitor) and fulvestrant for adults with endocrine-resistant, PIK3CA-mutated, HR+/HER2- locally advanced or metastatic breast cancer following recurrence on or after completing adjuvant endocrine therapy.

Other names
inavolisib plus endocrine therapy
02

Targets

PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)CDK4 (Cyclin-dependent kinase 4)ESR2 (ERβ)ESR1 (ERα)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CD (Phosphatidylinositol 3-kinase delta)CDK6 (Cyclin-dependent kinase 6)

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