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Drug intelligence / Profile preview
dactolisib
- Development stage
- Discontinued
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dactolisib is an orally bioavailable small molecule and imidazoquinoline derivative that acts as a dual inhibitor of phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR). It inhibits all PI3K isoforms and mTOR, targeting the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in cancer. By blocking this pathway, dactolisib induces tumor cell apoptosis and inhibits proliferation in PI3K/mTOR-overexpressing tumor cells. Dactolisib has been investigated for various indications including solid tumors, renal cancer, breast cancer, Cowden syndrome, glioblastoma, pancreatic neuroendocrine tumors, acute lymphoid leukemia, heart failure, respiratory tract infections (including COVID‑19), Parkinson's disease, and others. The drug was originally developed by Novartis and has also been associated with Adicet Bio[1][2][3][4][5][6].
- Other names
- dactolisibdactolisib-tosylateNVP-BEZ235-NXNVP-BEZ-235-NXNVP-BEZ 235-NXNVP-BEZ235-ANANVP-BEZ-235-ANANVP-BEZ 235-ANA
02
Targets
ATR (ATR serine/threonine kinase)mTOR (Mammalian target of rapamycin kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)
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