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.
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.
Robert Zaczek, PhD
Chief Scientific Officer