PsychoGenics is planning the development of RO7117997 for the treatment of multiple CNS conditions starting with sleep and seizure disorders

PGI Drug Discovery LLC (PsychoGenics), a phenotypic drug discovery platform company, announced that it has entered into an exclusive license agreement with Roche to obtain global development, manufacturing, and commercialization rights to RO7117997. RO7117997, is an IND-ready Equilibrative Nucleoside Transporter 1 (ENT1) inhibitor discovered in partnership with Roche using the PsychoGenics’ AI-enabled phenotypic screening platforms. PsychoGenics intends to evaluate RO7117997 as a potential treatment for several psychiatric and neurological conditions, starting with sleep and seizure disorders.

"RO7117997 was originally identified through our partnership with Roche, employing our SmartCube® platform, and subsequent research at Roche revealed it to act as an ENT1 inhibitor," stated Emer Leahy, PhD, President and CEO, PsychoGenics. "It is particularly gratifying that we have the opportunity to advance another phenotypically discovered drug candidate. Inhibition of ENT1 represents a novel approach for addressing a range of neuropsychiatric disorders. This license agreement perfectly aligns with our strategic objective of developing improved treatments for severely disabling CNS conditions."

“We are excited to expand our pipeline and are optimistic about the potential of ENT1 inhibitors in addressing a diverse array of disorders, as indicated by pre-clinical data,” said David Bleakman, PhD, President, Drug Discovery, PsychoGenics. “RO7117997 has already demonstrated a compelling safety profile in non-clinical studies, and we are on track to submit an IND application and commence clinical trials in 2024."

About ENT1 inhibition

ENT1 inhibitors block the activity of the ENT1 transporter. By doing so, they prevent the uptake of adenosine into cells, leading to an increase in the extracellular concentration of adenosine. An increase in adenosine levels can improve sleep quality and reduce the frequency and severity of seizures through activation of adenosine receptors. Other potential applications for an ENT1 inhibitor include the treatment of neuropsychiatric conditions such as schizophrenia and addiction, neurodegenerative disorders, pain and inflammation.

About PsychoGenics

PsychoGenics Inc. and its discovery arm, PGI Drug Discovery LLC (collectively known as PsychoGenics), have pioneered the translation of rodent behavioral and physiological responses into robust, high-throughput and high-content phenotyping. PsychoGenics’ drug discovery platforms, SmartCube®, NeuroCube®, PhenoCube® and eCube®, have been used in shared-risk partnerships with major pharmaceutical companies, including Sunovion, Roche and Karuna, resulting in the discovery of several novel compounds now in clinical trials or advanced preclinical development. PsychoGenics’ capabilities also include standard behavioral testing, electrophysiology, translational EEG, molecular biology, microdialysis and quantitative immunohistochemistry. In addition, the Company offers a variety of mouse models that support research in areas such as Huntington’s disease, autism spectrum disorders, psychosis/schizophrenia, depression, PTSD, Alzheimer’s disease, Parkinson’s disease, muscular dystrophy, ALS, seizure disorders and pain.

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