Drug intelligence / Profile preview

BGT226

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

BGT226 (also known as NVP-BGT226 or BGT-226) is an orally bioavailable, small molecule dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR). It acts as a potent pan-class I PI3K inhibitor with preference for the alpha isoform and inhibits both mTORC1 and mTORC2 complexes. By blocking the PI3K/AKT/mTOR signaling pathway, it suppresses cell growth, induces G0/G1 cell cycle arrest, promotes autophagy, and may trigger apoptotic cell death in cancer cells. Developed by Novartis for the treatment of solid tumors including advanced breast cancer and pancreatic cancer, its maximum clinical trial phase reached was Phase II before development was discontinued[1][2][6][7][8].

Other names
BGT226 maleateBGT-226 maleateBGT 226 maleateBGT-226 free baseBGT226 free baseBGT 226 free base
02

Targets

PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3C3 (PI3K class III)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)

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