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M2-9SLP + mApoE-MEKi-liposomes
- Development stage
- Preclinical
- Lead developer
- Humanitas Research Hospital
- Modality
- Small Molecules, Peptides, Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
M2-9SLP + mApoE-MEKi-liposomes is an experimental, dual-functionalized liposomal nanoparticle system designed for the targeted delivery of a MEK inhibitor (specifically pimasertib) to glioblastoma (GBM). The system utilizes a modified Apolipoprotein E-derived peptide (mApoE) to facilitate transport across the blood-brain barrier (BBB) via the low-density lipoprotein receptor (LDLR). Additionally, it incorporates a matrix metalloproteinases 2 and 9 (MMP2/9)-sensitive lipopeptide (M2-9SLP), which triggers the release of the encapsulated MEK inhibitor specifically within the MMP-rich tumor microenvironment. This approach aims to overcome the poor BBB permeability of small-molecule MEK inhibitors and reduce off-target toxicity while effectively inhibiting the MEK/ERK signaling pathway in GBM stem-like cells (GSCs). The research was developed by academic investigators at IRCCS Istituto Clinico Humanitas and the University of Milan.
- Other names
- M2-9SLP/mApoE-liposomes encapsulating pimasertib
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MMP9 (Matrix metalloproteinase-9)LDLR (Low-density lipoprotein receptor)MMP2 (Matrix metalloproteinase-2)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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