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Rodin Therapeutics today announced the publication of a scientific paper demonstrating the efficacy of novel compounds which selectively inhibit the HDAC-CoREST complex. In preclinical models, the compounds promote synaptic growth and function while minimizing the hematological side effects observed with less selective HDAC inhibitors.
The paper, published in the journal ACS Chemical Neuroscience, presents preclinical data showing that selectively targeting the CoREST complex increased synaptic proteins, led to the creation of new synapses as well as durable structural improvements in dendritic spines, and restored long-term potentiation without serious dose-limiting toxicities. This safety profile indicates that the compound could be appropriate for testing in clinical trials enrolling patients with synaptopathies such as Alzheimer’s disease, Parkinson’s disease and frontotemporal dementia.
“HDAC inhibitors have been an attractive drug development target for years because they regulate synaptogenesis and synaptic plasticity – yet class-related toxicities have prevented them from being used in chronic neurologic conditions,” said Magnus Ivarsson, Ph.D., Rodin’s vice president, head of discovery and the lead author on the paper. “We’re excited to be able to demonstrate that we can achieve the pro-synaptic benefits of the class without the HDAC class toxicities by developing compounds that selectively target the CoREST complex, and we’re encouraged by these data as we move our lead compound into clinical trials.”
About Rodin Therapeutics
Rodin Therapeutics is discovering and developing first-in-class therapeutics for synaptopathies by applying novel chemical strategies to target specific HDAC complexes and upregulate key neuronal genes. Rodin’s targeted approach to enhancing synaptic integrity, backed by a robust translational strategy, has potential across multiple neurologic diseases, such as Alzheimer’s, frontotemporal dementia, Parkinson’s disease and schizophrenia, all of which are characterized by impaired neuronal and synaptic function. For more information, visit https://rodintherapeutics.com/ and follow Rodin on Twitter @Rodintx.
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