Drug intelligence / Profile preview

inavolisib + trastuzumab deruxtecan

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

**Inavolisib + trastuzumab deruxtecan** is an experimental combination regimen under clinical investigation for cancers characterized by HER2 expression and/or activating PIK3CA mutations. - **Inavolisib** is a *potent and selective PI3K alpha inhibitor* (targeting the PIK3CA mutation), developed as an orally administered small molecule, aimed at blocking the aberrant PI3K signaling that drives tumor growth in certain breast cancers. - **Trastuzumab deruxtecan** is an *antibody-drug conjugate* (ADC) that consists of a humanized anti-HER2 monoclonal antibody (trastuzumab) linked to a topoisomerase I inhibitor payload (deruxtecan, DXd). This molecule targets HER2-expressing tumor cells, delivering the cytotoxic drug directly to the tumor and inducing DNA damage leading to cell death. Both are being investigated for treatment of advanced or metastatic breast and other HER2-positive solid tumors, particularly in cases with PIK3CA mutations or HER2 overexpression. The main primary indication in clinical studies is metastatic breast cancer, HER2-positive and/or hormone receptor-positive/PIK3CA-mutated subtypes[3][5].

Other names
inavolisib + DS-8201inavolisib + fam-trastuzumab deruxtecan-nxkiinavolisib + Enhertu
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)PIK3C2B (PI3K-C2β)

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