NeurOp Receives FDA Orphan Drug Designation for NP10679 for Treatment of Subarachnoid Hemorrhage

Atlanta, GA – December 8, 2021 – NeurOp, Inc., a clinical-stage biotechnology company focused on neurological and psychiatric disorders, today announced that the U.S. Food and Drug Administration (FDA) has granted orphan drug designation to the company’s investigational candidate NP10679 for the treatment of subarachnoid hemorrhage (SAH).

SAH is a life-threatening type of stroke caused by bleeding into the space surrounding the brain. In patients who experience SAH caused by a ruptured aneurysm, vasospasm producing ischemic damage occurs in over one-third of patients during the week following the event and often results in permanent disability or death.

The mechanism by which ischemia damages the brain involves overactivation of NMDA receptors. Ischemia also induces acidity of brain tissue. Together, these insights led NeurOp to develop NMDA receptor blockers with increased potency in acidic tissue. NeurOp’s lead compound NP10679 is a highly selective antagonist for NMDA receptors and has greater potency in acidic conditions. These properties will enable it to provide neuroprotection against ischemic injury caused by vasospasm in SAH with fewer negative side effects than currently available NMDA inhibitors and other treatments.

“NP10679 demonstrated safety, tolerability and positive pharmacokinetics in our Phase 1 studies that make it an attractive candidate for prophylactic treatment following SAH,” said James McNamara, M.D., Executive Chairman of NeurOp. “Based on its encouraging profile, we look forward to commencing a Phase 2 clinical trial of NP10679 for SAH in 2023.”

The FDA Office of Orphan Products Development grants orphan drug designation to investigational drugs and biologics intended for the treatment, diagnosis or prevention of rare diseases, which are defined as those that affect fewer than 200,000 people in the U.S. The program provides certain benefits that include tax credits and application fee waivers designed to offset some development costs, as well as seven-year marketing exclusivity to sponsors of approved orphan products.

About NP10679
NeurOp is developing NP10679 as a subunit-specific NMDA receptor inhibitor for CNS disorders. NMDA receptors are activated by the neurotransmitter glutamate, the predominant excitatory transmitter in the brain. Several neurological disorders, including pain, treatment-resistant depression and brain damage resulting from acute brain injury, such as stroke or SAH, are associated with overactivity of these receptors. NP10679 is selective for a specific NMDA subtype, GluN2B, and has increased potency in acidic conditions. Its enhanced selectivity and disease context-dependent target engagement may provide neuroprotection with fewer negative side effects than currently available NMDA inhibitors.

About NeurOp, Inc.
NeurOp, Inc. is a privately held, clinical-stage biopharmaceutical company based in Atlanta, Georgia that is developing small-molecule therapies for central nervous system disorders, including severe pain, treatment-resistant depression, subarachnoid hemorrhage (SAH) and stroke. Its proprietary compounds selectively inhibit the GluN2B subunit of neuronal NMDA receptors and are designed for potential therapeutic benefit with an improved safety and tolerability profile relative to other NMDA receptor antagonists. For more information, please visit www.neuropinc.com or follow us on LinkedIn.

NeurOp Announces Positive Topline Data from Phase 1 Studies for Lead Candidate NP10679 for CNS Disorders

Results show excellent half-life and positive safety profile to enable testing in stroke, severe pain, subarachnoid hemorrhage and treatment-resistant depression

Atlanta, GA – May 28, 2020 – NeurOp, Inc., a privately held, clinical-stage biotechnology company focused on neurological and psychiatric disorders, today announced the successful completion of Phase 1 studies of NP10679, a highly potent and selective GluN2B subunit-specific NMDA (N-methyl-D-aspartate) receptor inhibitor. NeurOp is investigating NP10679 for several CNS disorders such as stroke, severe pain, subarachnoid hemorrhage and treatment-resistant depression, which are associated with over-activity of NMDA receptors.

The primary objective of the studies was to evaluate the safety and tolerability of NP10679 in healthy subjects. Secondary objectives included assessment of pharmacokinetics and pharmacodynamics.

The initial Phase 1 trial was a first-in-human randomized, placebo-controlled, single ascending dose (SAD) study that assessed NP10679 in healthy volunteers. The study included six single ascending dose cohorts (5 to 200 mg). The study enrolled 48 subjects, 36 of whom received study drug while the remaining 12 subjects received placebo. A second Phase 1 study employed a multiple ascending dose (MAD) design assessing the effects of NP10679 on 24 subjects in three cohorts (25, 50 and 100 mg once daily) over five days.

The pharmacokinetic profile of NP10679 in humans indicated clear dose linearity across the dose ranges tested and an excellent half-life of approximately 17 hours. The results from both studies also revealed a benign safety profile that should allow adequate dosing to test the molecule in a number of indications.

“Development of NP10679 rests on a foundation of outstanding science. Based on the encouraging safety profile and positive pharmacokinetics demonstrated in our Phase 1 clinical studies, we look forward to advancing NP10679 into Phase 2 trials for stroke,” said James McNamara, M.D., Executive Chairman of NeurOp. “We plan to initiate Phase 2 studies in early 2021.”

The phase 1 NP10679 program was conducted in collaboration with Pharmaron (Baltimore). Data collected from this study will inform dose and schedule for further development of NP10679.

About NP10679
NP10679 is being developed as subunit-specific NMDA receptor inhibitor for CNS disorders. NMDA receptors are activated by the neurotransmitter glutamate, the predominant excitatory transmitter in brain. Several neurological disorders, including pain, treatment-resistant depression, and brain damage resulting from acute brain injury, such as stroke or subarachnoid hemorrhage (SAH), are associated with over-activity of these receptors that leads to significant acidification in brain tissues. NP10679 is selective for a specific NMDA subtype, GluN2B, and has increased potency in acidic conditions. This enhanced selectivity and disease context-dependent target engagement may provide neuroprotection with fewer negative side effects than currently available NMDA inhibitors.

About NeurOp, Inc.
NeurOp, Inc. is a clinical-stage biopharmaceutical company based in Atlanta, Georgia that is developing small-molecule therapies for central nervous system disorders, including severe pain, subarachnoid hemorrhage (SAH) and stroke. Its proprietary compounds selectively inhibit the GluN2B subunit of neuronal NMDA receptors for potential therapeutic benefit with fewer side effects than currently available NMDA receptor antagonists. For more information, please visit www.neuropinc.com.

NeurOp Initiates Phase 1 Clinical Trial of NMDA Receptor Inhibitor NP10679

NeurOp, Inc., a clinical-stage biotechnology company, today announced the initiation of a Phase 1 clinical trial of NP10679, a highly potent and selective GluN2B subunit-specific NMDA (N-methyl-D-aspartate) receptor inhibitor. NeurOp is investigating NP10679 for several neurological disorders that are associated with over-activity of these receptors.

The randomized, placebo-controlled, single ascending dose study will assess the safety, pharmacokinetics and pharmacodynamics of NP10679 in healthy volunteers. The study is being conducted in collaboration with Pharmaron (Baltimore) and is currently enrolling subjects in the United States. Data collected from the study will inform dose and schedule for further development of NP10679 for potential use in severe pain and the prevention of ischemic damage following subarachnoid hemorrhage (SAH).

Certain areas of the brain become acidified by metabolic insufficiency or increased neuronal activity. This condition or “context” exists in severe pain and SAH and may also exist in brain areas that are undergoing seizures or involved in nicotine or opioid addiction.

“NP10679 is a first-in-class therapy as a context-dependent NMDA receptor inhibitor,” said NeurOp’s Chief Scientific Officer, Robert Zaczek, PhD. “Preclinical data demonstrate that NP10679 is different from other NMDA therapies, because of its selectivity, safety profile and potency at low pH, a condition found in a number of central nervous system disorders.”

“We have achieved a significant milestone for NeurOp now that NP10679 has advanced to the clinic,” said James McNamara, MD, Executive Chairman at NeurOp. “We look forward to moving this compound through clinical development and are particularly encouraged by its potential as a treatment for severe pain. With the opioid epidemic facing the nation, the need for effective and safe medications for severe pain is greater than ever.”

NP10679 is bioavailable either orally or by IV, and it is currently being evaluated in this study by the IV route. An IND for NP10679 was opened in 2016.

About NeurOp
NeurOp, Inc. is a clinical-stage biopharmaceutical company based in Atlanta that is developing small-molecule therapies for central nervous system disorders, including severe pain, subarachnoid hemorrhage (SAH) and catastrophic juvenile epilepsies. Its proprietary compounds selectively inhibit the GluN2B subunit of neuronal NMDA receptors for potential therapeutic benefit with fewer side effects than currently available NMDA receptor antagonists. For more information, please visit www.neuropinc.com.

NeurOp contact:
Robert Zaczek, PhD
Phone: 860.853.0427

NIH Awards NeurOp $3.5 Million to Support Phase 1 Clinical Trial of NMDA Inhibitor NP10679

NP10679 is in development to prevent brain ischemia during stroke or subarachnoid hemorrhage

NeurOp, Inc. today announced that it has received a $3.5 million award from the National Institute of Neurological Disorders and Stroke (NINDS), a division of the NIH, to begin clinical testing of the Company’s drug candidate NP10679, a GluN2B subunit-specific NMDA (N-methyl-D-aspartate) inhibitor. NeurOp is investigating NP10679 for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage (SAH).

“We designed NP10679 with great care to incorporate the attributes we believe differentiate this molecule from other NMDA inhibitors in development,” said Barney Koszalka, PhD, NeurOp CEO. “For example, the binding of the molecule is enhanced in an acidic environment, a property other NMDA inhibitors lack. This property of pH dependence improves the chance of achieving efficacy at dose levels devoid of side effects. We would like to partner with a pharmaceutical company in future trials to fully explore this advantage in an array of disorders such as stroke, treatment-resistant depression and neuropathic pain.”

NP10679 is bioavailable by either the oral or IV route, and it will initially be evaluated in a Phase 1 study in healthy human volunteers by the IV route. The study is expected to start in early 2018. Pre-clinical studies have shown efficacy in treating complications associated with SAH. An IND for NP10679 was opened in 2016.

NeurOp’s Chief Scientific Officer, Robert Zaczek, PhD, added, “The safety profile of NP10679 allows for prophylactic use in patients at risk for an ischemic event, such as those suffering an SAH. This is important because extensive data has shown that early intervention is key for robust efficacy of neuroprotective therapy. Our prophylactic intervention strategy will place NP10679 at its site of action before an SAH-driven delayed cerebral ischemia event takes place. This eliminates the time-of-dosing caveat that might, in part, have led to previous failures of clinical tests involving glutamatergic agents in stroke and head trauma.”

Note: Research reported in this news release is supported by the National Institute of Neurological Disorders and Stroke of the National Institutes of Health (NIH) under Award Number R44NS071657. The content is solely the responsibility of the authors and does not necessarily represent the official views of the NIH.

About NeurOp
NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia and Parkinson’s disease. Its research targets specific subunits of neuronal NMDA receptors to identify and evaluate small molecule modulators for potential therapeutic benefit. Multi-year funding from the NIH supports the Company’s research and development programs for NP10679 for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage. For more information, please visit www.neuropinc.com.

NeurOp contact:
Barney Koszalka, PhD, CEO

NeurOp’s Lee Latimer Elected to ACS 2016 Board of Directors

NeurOp, Inc. today announced that Lee H. Latimer, Ph.D., head of chemistry, has been elected as Director-at-Large for the American Chemical Society’s (ACS) 2016 Board of Directors. The Society announced election results on November 5.

Dr. Latimer has been a member of ACS since 1972 and became an ACS Fellow in 2012. He has held leadership positions at the local and national level of the organization and been recognized with a number of awards for his contributions.

“ACS is about opportunity for its members in so many ways. It has certainly been so for me. I enjoy meeting new challenges and colleagues in teams and applying my experience to make a difference,” said Latimer.

Dr. Latimer earned his Ph.D. in organic chemistry from the University of Wisconsin under the mentorship of B.M. Trost and held an NIH Fellowship with W.G. Dauben at the University of California at Berkeley and C.J. Sih at the University of Wisconsin at Madison. To learn more about Dr. Latimer’s extensive professional experience, click here.

About NeurOp
NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia, and Alzheimer’s and Parkinson’s diseases. Its research targets various subunits of neuronal NMDA receptors and their potential therapeutic benefit. The company has licensed its technology to Bristol-Myers Squibb for the development of a compound for treatment-resistant depression. Multi-year funding from the NIH supports the company’s research and development programs for schizophrenia, Alzheimer’s disease and NP10679, its drug candidate for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage. For more information, please visit www.neuropinc.com.

NeurOp contact:
Barney Koszalka, CEO
Phone: (919) 260-5595

NeurOp Announces Strategic Collaboration with Johnson & Johnson Innovation to Study Role of NMDA Receptors

NeurOp, Inc. today announced that it has entered into a research collaboration with Janssen Pharmaceuticals, Inc. to better understand how modulating the NMDA (N-methyl-D-aspartate) receptor impacts pathways related to different central nervous system disorders.

Under the agreement, which was facilitated by the Johnson & Johnson Innovation Center in Boston, NeurOp and Janssen will focus specifically on the modulation of the 2C and 2D subunits of the NMDA receptor and their potential to impact central nervous system disorders such as depression. Financial terms of the agreement were not disclosed.

“Glutamate signaling through NMDA receptors is one of the most important processes in normal brain function, particularly in emotional processing,” said Barney Koszalka, Ph.D., NeurOp CEO. “NeurOp and Janssen see this as a tremendous opportunity to investigate the use of NMDA modulators, which could lead to new treatments for patients afflicted with a number of central nervous system disorders.”

About NeurOp
NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia, and Alzheimer’s and Parkinson’s diseases. Its research targets various subunits of neuronal NMDA receptors and their potential therapeutic benefit. The company has licensed its technology to Bristol-Myers Squibb for the development of a compound for treatment-resistant depression. Multi-year funding from the NIH supports the company’s research and development programs for schizophrenia, Alzheimer’s disease and NP10679, its drug candidate for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage. For more information, please visit www.neuropinc.com.

NeurOp contact:
Barney Koszalka, Ph.D., CEO
Phone: (919) 260-5595

 

NeurOp Receives Milestone Payment as Bristol-Myers Squibb Nominates NMDA Receptor Compound as Drug Development Candidate

NeurOp, Inc. today announced that Bristol-Myers Squibb has selected an NR2B-specific N-methyl-D-aspartate (NMDA) receptor modulator as a drug development candidate for treatment-resistant depression. This decision triggers a milestone payment to NeurOp, which licensed its technology to Bristol-Myers Squibb in 2009. The compound can now advance into pre-IND studies.

“The team at Bristol-Myers Squibb has been a dedicated, insightful research partner as we have worked together for more than three years to identify and advance a new drug candidate,” commented Barney Koszalka, Ph.D., NeurOp president and CEO. “Reaching this clinical and financial milestone is important to NeurOp, because it will help support our R&D on additional subunits of the NMDA receptor as treatments for other central nervous system disorders.”

Under the terms of the agreement, Bristol-Myers Squibb agreed to pay NeurOp an upfront fee and fund a multi-year research collaboration. The direct research collaboration ended in December 2012, and the program was fully internalized at Bristol-Myers Squibb. NeurOp is eligible to receive additional milestone payments for the successful development of a compound and royalties on worldwide sales of commercialized compounds. Financial terms of the current milestone were not disclosed.

About Treatment-Resistant Depression
Unlike normal emotional experiences of sadness, loss or passing mood states, major depressive disorder (MDD) is persistent and can significantly interfere with thoughts, behavior, mood, activity and physical health. According to the National Institute of Mental Health, MDD is the leading cause of disability in the U.S. for people aged 15 to 44 and affects almost 15 million adults, or about 6.7 percent of the population in a given year. Up to 15 percent of people with MDD die by suicide. About one-third of people suffering from depression do not get relief from first-line antidepressant medications. Of significant concern is the fact that even when effective there is a delay in onset of action of two weeks or more, during which time patients are at increased risk of suicide.

About NeurOp
NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia, and Alzheimer’s and Parkinson’s diseases. Its research targets various subunits of neuronal NMDA receptors and their potential therapeutic benefit. The company has licensed its technology to Bristol-Myers Squibb for the development of a compound for treatment-resistant depression. Multi-year funding from the NIH supports the company’s research and development programs for schizophrenia, Alzheimer’s disease and NP10679, its drug candidate for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage. For more information, please visit www.neuropinc.com.

NeurOp contact:
Barney Koszalka, CEO
Phone: (919) 260-5595

 

NeurOp Awarded NIH Grant for Alzheimer’s Disease Drug Research

NeurOp, Inc. announced today that the National Institutes of Health (NIH) has awarded it a grant to support research on new Alzheimer’s disease treatments. NeurOp is investigating subunit-selective N-methyl D-aspartate (NMDA) receptor compounds as potential therapeutics. The grant is a one-year award and will be conducted in collaboration with Dr. Jon Johnson at the University of Pittsburgh.

“Alzheimer’s disease has devastating effects on patients and their families,” said Barney Koszalka, Ph.D., NeurOp president and CEO. “Our research suggests that targeting specific subunits of NMDA receptors may lead to a new generation of drugs that may enhance cognitive performance, as well as impact the progression of other diseases of the central nervous system. This is the third grant we’ve received from the NIH to fund research based on our NMDA receptor modulation platform, and we look forward to further exploring the potential it has for patients.”

This project is supported by the National Institute on Aging of the National Institutes of Health under award number R41AG048723.

About NeurOp
NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia, and Alzheimer’s and Parkinson’s diseases. Its research targets various subunits of neuronal NMDA receptors and their potential therapeutic benefit. The company has licensed its technology to Bristol-Myers Squibb for the development of a compound for treatment-resistant depression. Funding from the NIH supports the company’s research and development programs for schizophrenia, Alzheimer’s disease and NP10679, its drug candidate for the prevention of ischemic damage during a stroke or subarachnoid hemorrhage. For more information, please visit www.neuropinc.com.

NeurOp contact:
Barney Koszalka, CEO
Phone: (919) 260-5595

Lee H. Latimer Joins NeurOp to Manage Its Chemistry Operations

NeurOp, Inc. announces that Lee H. Latimer, Ph.D., has been appointed as its head of chemistry. He will oversee the company’s chemistry program to support its drug development initiatives for the treatment of depression, neuropathic pain, ischemia (stroke), schizophrenia and other central nervous system disorders.

Dr. Latimer was most recently a consultant to the pharmaceutical and biotechnology industries and provided expertise in process, analytical and medicinal chemistry. Prior to that, he was the senior director of process and analytical chemistry at Elan Pharmaceuticals. He successfully led in-house and outsourced oversight and development of GMP routes to five clinical candidates in its Alzheimer’s disease and multiple sclerosis programs. Dr. Latimer is also an inventor of semagacestat, which reached phase III clinical trials for Alzheimer’s disease in collaboration with Eli Lilly.

“Lee brings a wealth of development experience to NeurOp at a time when our internal programs are advancing into clinical development,” said Barney Koszalka, Ph.D., president and CEO at NeurOp. “His work in early-stage medical chemistry programs will also greatly contribute to our ongoing efforts to develop new modulators of the NMDA receptor through our collaboration with Emory University.”

Dr. Latimer earned his Ph.D. in organic chemistry from the University of Wisconsin under the mentorship of B.M. Trost and held an NIH Fellowship with W.G. Dauben at the University of California at Berkeley and C.J. Sih at the University of Wisconsin at Madison. He is an American Chemical Society Fellow.

About NeurOp

NeurOp, Inc. is an Atlanta-based biopharmaceutical company developing new medicines for central nervous system disorders, including depression, neuropathic pain, ischemia (stroke), schizophrenia, and Alzheimer’s and Parkinson’s diseases. Its research targets various subunits of neuronal NMDA receptors and their potential therapeutic benefit. The company has a research collaboration and licensing agreement with Bristol-Myers Squibb for the development of NeurOp’s compounds for the treatment of depression and neuropathic pain. Multi-year funding from the NIH supports the company’s research and development programs for schizophrenia and NP10679, its drug candidate for the prevention of ischemic damage. For more information, please visit www.neuropinc.com.

NeurOp contact:

Barney Koszalka, CEO
Phone: 404.941.2350

 

NeurOp Selects NP10679 as Development Candidate for SAH

NeurOp, Inc. has selected NP10679 as a development candidate for the prevention of ischemic damage and its consequences in persons receiving surgical treatment for subarachnoid hemorrhage (SAH). NP10679 is a GluN2B subunit-specific modulator designed to work at the site of ischemic insult.

NeurOp has begun late-stage preclinical development studies with this candidate with the goal to file an IND in 2015.

This news follows the publication of related research by NeurOp’s director of drug discovery, Scott J. Myers, Ph.D., in collaboration with a number of other scientists. In February, Neurocritical Care published their paper entitled “pH-Sensitive NMDA Inhibitors Improve Outcome in a Murine Model of SAH.”

The manuscript demonstrates that the use of a pH-dependent NMDA antagonist has the potential to work selectively in areas of ischemia known to undergo acidic pH shifts, which occur during SAH. Because of their regional selectivity, these NMDA antagonists may also be associated with fewer behavioral side effects than non-selective NMDA antagonists.

NeurOp contact:
Barney Koszalka, CEO
Phone: 404.941.2350