PAGE TITLE
Neuroprotective agent for Parkinson’s Disease
PAGE SUMMARY
Parkinson’s Disease (PD) is a progressive neurological disorder whose prevalence increases with age and certain genetic predispositions. It is estimated that 7-10 million people are affected by Parkinson’s Disease worldwide, with 1 million in the United States. Currently, there are no small molecule drugs to halt or reverse the progression of PD. The gold standard therapy for treating the symptoms of PD is dopamine replacement therapy with Levodopa (L-dopa). However, 60-80% of patients treated with L-dopa develop complications, including a severe movement disorder called L-dopa-induced dyskinesia.
To address the unmet need of pharmaceutical interventions that can halt the progression of Parkinson’s Disease, researchers at Drexel University have developed GT951, a novel small molecule activator of glutamate transporter GLT-1 / excitatory amino acid transporter EAAT2. GT951 confers neuroprotection by scavenging out excess glutamate to prevent excitotoxicity and subsequent neurodegeneration. In preliminary studies, GT951 has demonstrated high specificity to GLT-1 and sub-nanomolar efficacy in removing glutamate from the synapse. A pilot efficacy study in a rodent PD model demonstrated that GL951 can prolong the time taken to form lesions and significantly reduce disease severity. GT951 is being optimized for pharmacokinetics, safety, and toxicology to develop a preclinical candidate for GLP studies.
APPLICATIONS
TITLE: Applications
Neuroprotective and disease-modifying agent for Parkinson’s Disease
Potential to halt disease progression
Reduce risk of dyskinesia
ADVANTAGES
TITLE:Advantages
Envisioned product of orally available drug
Small molecule activator of GLT-1/EAAT2
Reduce excitotoxicity in brain
Delay use of L-dopa therapy to prevent ON-OFF and L-dopa-induced dyskinesia
IP STATUS
Intellectual Property and Development Status
Pending PCT application PCT/US2018/013867
https://patents.google.com/patent/WO2018132829A1/en?oq=PCT%2fUS2018%2f013867
PUBLICATIONS
References
Kortagere S. et al. Identification of Novel Allosteric Modulators of Glutamate Transporters. ACS Chemical Neuroscience, 2018, 9(3), p. 522-534.
https://pubs.acs.org/doi/10.1021/acschemneuro.7b00308
Contact Information
Robert McGrath, Ph.D.
Sr. Associate Vice Provost
215-895-0303
rbm26@drexel.edu