12 March 2018 - - US-based brain and nervous system disorder treatment developer Aptinyx Inc. has presented preclinical and early-stage clinical data from studies of the company's lead product candidate, NYX-2925, at the 20th annual meeting of the American Society for Experimental Neurotherapeutics, the company said.
The presentation featured results from preclinical studies that further demonstrate efficacy and safety of NYX-2925, Aptinyx's novel modulator of the N-methyl-D-aspartate (NMDA) receptor, in several models of neuropathic pain.
In several preclinical models of neuropathic pain, NYX-2925 demonstrated reproducible and dose-dependent analgesic activity. At doses well in excess of the analgesic dose levels, NYX-2925 did not have adverse effects in safety-pharmacology and toxicology studies.
NYX-2925 had high oral bioavailability and the pharmacokinetics were reproducible and predictable across species.
The presentation also included Phase 1 clinical data outlining the safety, tolerability, and pharmacokinetics of NYX-2925 in healthy volunteers. Once-daily oral dosing with NYX-2925 for seven days produced linear, dose-proportional pharmacokinetics and minimal accumulation in 84 healthy adult volunteers.
NYX-2925 was generally well-tolerated, there were no serious adverse events reported, and no subjects discontinued due to adverse events. Additionally, evaluation of cerebrospinal fluid samples from study participants confirmed that NYX-2925 crosses the blood-brain barrier.
NYX-2925 is an oral, small-molecule NMDA receptor modulator that binds to a novel site on the NMDA receptor and enhances synaptic plasticity to restore normal neural cell function.
Aptinyx is a clinical-stage biopharmaceutical company discovering and developing transformative therapies for challenging disorders of the brain and nervous system.
The company has a proven platform for discovery of novel compounds that work through a unique mechanism to modulate -- rather than block or over-activate -- NMDA receptors and enhance synaptic plasticity, the foundation of neural cell communication.