Drug intelligence / Profile preview

GNE-493

Development stage
Discontinued
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GNE-493 is a potent, selective, and orally bioavailable small molecule dual inhibitor of pan-phosphoinositide 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR). Developed by Genentech, it targets all four class I PI3K isoforms (α, β, δ, and γ) as well as mTOR, effectively blocking the PI3K/AKT/mTOR signaling pathway which is frequently deregulated in various cancers. In preclinical studies, GNE-493 has demonstrated efficacy in xenograft models of cancer, including high-grade serous ovarian cancer (HGS-OvCa), where it has been used to study apoptotic vulnerabilities and drug resistance mechanisms. It is primarily utilized as a research tool compound and has not been approved for human use.

Other names
GNE 493GNE493GNE-493
02

Targets

MAP3K9 (Mixed lineage kinase 1)mTOR (Mammalian target of rapamycin kinase)AURKA (Aurora kinase A)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)SYK (Spleen Tyrosine Kinase)

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