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DRUG:

MSU-42011

i
Other names: MSU-42011
Associations
Trials
Company:
Akeila Bio, Michigan State University
Drug class:
Retinoid X receptor agonist
Associations
Trials
over1year
MSU-42011, alone and in combination with selumetinib, reduces pERK levels in NF1 cancer cells and decreases CCL2 expression in THP-1 macrophages (AACR 2023)
Notably, MSU-42011 and selumetinib alone similarly inhibited CCL2 mRNA expression by 25% in THP1 macrophages stimulated with CM from PNF cells, and the inhibition of CCL2 mRNA expression was enhanced to 50% with combination treatment. Taken together, our data suggest that MSU-42011 should be tested in relevant preclinical models of NF1.
Combination therapy
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KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • CCL2 (Chemokine (C-C motif) ligand 2) • GLI2 (GLI Family Zinc Finger 2) • MRC1 (Mannose Receptor C-Type 1) • PERK (Pancreatic EIF2-Alpha Kinase)
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NF1 mutation
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Koselugo (selumetinib) • MSU-42011
over1year
Activation of the RXR nuclear receptor regulates CD4 T cell activity in a murine model of HER2+ breast cancer (AACR 2023)
In conclusion, MSU42011 increased recruitment and activation of CD4 T cells in vitro and in HER2+ mammary tumors. These data, in combination with our previous work showing that RXR agonists reduce expression of tumor-promoting FOXP3 T cells in vitro and in vivo, confirm a strong correlation between RXR pharmacologic activation and CD4 T cell activation within the tumor microenvironment.
Preclinical • PD(L)-1 Biomarker • IO biomarker
|
HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • ITGAM (Integrin, alpha M) • FOXP3 (Forkhead Box P3) • ITGAX (Integrin Subunit Alpha X)
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PD-L1 expression • FOXP3 expression
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MSU-42011