Drug intelligence / Profile preview

GDC-0077 + fulvestrant + palbociclib

Development stage
Unknown
Lead developer
Genentech
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Oral, Intramuscular
01

Overview

This is a combination therapy consisting of inavolisib (GDC-0077), fulvestrant, and palbociclib. Inavolisib is a highly selective, oral small molecule inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kα) that also promotes the degradation of mutant p110α protein, the catalytic subunit encoded by PIK3CA. Fulvestrant is an estrogen receptor antagonist used as hormonal therapy for hormone receptor-positive breast cancer. Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression. This combination targets multiple pathways involved in tumor growth and proliferation—PI3K signaling, estrogen receptor signaling, and cell cycle regulation—and has been investigated primarily for patients with PIK3CA-mutated, hormone receptor-positive (HR+), HER2-negative locally advanced or metastatic breast cancer whose disease progressed during or after endocrine therapy[1][2][4][5].

Other names
inavolisib + fulvestrant + palbociclib
02

Targets

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

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