Drug intelligence / Profile preview

inavolisib + pertuzumab + trastuzumab

Development stage
Unknown
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

This is a combination therapy consisting of inavolisib (a potent and selective PI3K alpha inhibitor), pertuzumab (a monoclonal antibody targeting HER2), and trastuzumab (another monoclonal antibody targeting HER2). Inavolisib works by inhibiting the phosphatidylinositol 3-kinase alpha isoform (PI3Kα) and promoting degradation of mutant p110α protein encoded by PIK3CA. Pertuzumab and trastuzumab both bind to different epitopes on the human epidermal growth factor receptor 2 (HER2/ERBB2), blocking its signaling pathways. This triplet regimen is being developed as maintenance therapy after induction treatment for patients with PIK3CA-mutated, HER2-positive locally advanced or metastatic breast cancer. The fixed-dose combination of pertuzumab + trastuzumab for subcutaneous injection is also known as Phesgo[1][4][8].

Other names
Phesgo (for the fixed-dose combination of pertuzumab and trastuzumab with hyaluronidase for subcutaneous injection)
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)PIK3CA (Phosphoinositide 3-kinase alpha)

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