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dactolisib + binimetinib
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of two oral small-molecule targeted therapies: dactolisib, a dual PI3K/mTOR inhibitor (also reported to inhibit ATR), and binimetinib, a selective MEK1/2 inhibitor. The regimen is designed to co-inhibit the PI3K/AKT/mTOR and MAPK/MEK/ERK pathways to overcome resistance and enhance antitumor activity in advanced solid tumors harboring RAS/RAF/MAPK or PI3K-pathway alterations. This combination has been evaluated in a phase I dose-escalation study and other early-phase trials in advanced solid tumors; toxicity management is a key consideration in dual-pathway blockade.
- Other names
- dactolisib plus binimetinibBEZ235 plus MEK162BEZ-235 plus MEK162BEZ 235 plus MEK162
02
Targets
ATR (ATR serine/threonine kinase)mTOR (Mammalian target of rapamycin kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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