Small Molecule mGlur5 Agonists for Remyelination in Multiple Sclerosis

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Invention Summary:

Multiple sclerosis (MS) is a debilitating autoimmune condition caused by an overactive immune system that destroys the myelin surrounding nerves cells. Symptoms of MS include pain, impaired coordination, vision loss, and overall weakness. Current treatment options work to suppress the immune system to slow progression of the disease and to manage symptoms. Currently, there are no approved treatments that reverse demyelination and/or stimulate new myelination.

Rutgers researchers have developed a series of novel small molecules that act as mGlur5 agonists to promote remyelination in multiple sclerosis. Designed as analogs of the known mGlur5 agonist CHPG, these compounds demonstrate enhanced potency and efficacy in stimulating myelin protein production in human oligodendrocytes and in vivo MS mouse models, addressing a critical unmet need for therapies that regenerate lost myelin rather than solely managing symptoms.

Market Applications:

• Development of disease-modifying drugs for multiple sclerosis
• Treatment options for other demyelinating disorders
• Pharmaceutical platforms focused on myelin regeneration
• Adjunct therapies combined with immune-modulating agents for MS

Advantages:

• Specifically targets mGlur5 receptor to stimulate natural myelin repair
• Greater potency at lower concentrations compared to existing mGlur5 agonists
• Demonstrated efficacy in both in vitro human cell models and in vivo animal models
• Potential to reverse demyelination and promote functional nerve repair
• Supported by federal grants and advanced preclinical testing

Publications:

• Huang, Y., et al., The mGluR5 agonist CHPG enhances human oligodendrocyte differentiation. Acta Neuropathol Commun, 2025. 13(1): p. 210. PMID: 41044782
• Saitta, K.S., et al., CHPG enhances BDNF and myelination in cuprizone-treated mice through astrocytic metabotropic glutamate receptor 5. Glia, 2021. 69(8): p. 1950-1965. PMID: 33811383

Intellectual Property & Development Status: Provisional application filed. Patent pending. Available for licensing and/or research collaboration. For any business development and other collaborative partnerships, contact:  marketingbd@research.rutgers.edu