Three Recent Preclinical Publications Highlight NMDA Receptor Activation Facilitated by Aptinyx’s NYX-2925
September 26 2019 - 8:07AM
Aptinyx Inc. (Nasdaq: APTX), a clinical-stage biopharmaceutical
company developing transformative therapies for the treatment of
brain and nervous system disorders, today announced that
preclinical data from the company’s novel NMDA receptor modulator,
NYX-2925, has been published in three scientific journals. The
published data demonstrate the effects of NYX-2925 on NMDA receptor
trafficking in vitro and on sleep, mood, and EEG biomarkers in
rodent models. Taken together, these data provide key insights into
the mechanism of NYX-2925 and its enhancement of synaptic
plasticity processes in the brain.
“The data published in these journals are
reflective of our in-depth understanding of the activity of
NYX-2925, garnered through evaluations across numerous molecular
and behavioral preclinical models,” remarked Norbert Riedel, Ph.D.,
president and chief executive officer of Aptinyx. “NYX-2925 and
other compounds in our pipeline are highly selective to the NMDA
receptor and exhibit a unique modulatory mechanism of action on
this receptor. We are very pleased to have these data published
across these high-caliber peer-reviewed journals to enhance the
understanding of this novel mechanism, which is highly relevant in
the treatment of chronic centralized neuropathic pain as well as
other neurologic conditions caused by aberrant synaptic plasticity
processes.”
The first publication is titled “NYX‐2925 induces
metabotropic NMDAR signaling that enhances synaptic NMDAR and
AMPAR” and has been published in the Journal of Neurochemistry. The
data published in this paper detail the NYX-2925 treatment-mediated
increases in NMDA receptor GluN2B trafficking and long-term
potentiation-related signaling. The findings demonstrate the
facilitation of synaptic plasticity processes resulting from
administration of different concentration levels of NYX-2925.
The second publication is titled “NMDAR activation
regulates the daily rhythms of sleep and mood” and has been
published in Sleep. The data presented in this paper demonstrate
the positive activity exhibited by NYX-2925 on various elements of
sleep architecture. Administration of NYX-2925 enhanced sleep
quality, as measured by an increase in the non-REM component of
sleep. NYX-2925 facilitated an increase in sleep-bout duration and
decreased drowsiness during wake, as measured by delta power.
NYX-2925 also reversed sleep deprivation-induced deficits in a
learning task and improved mood. Aptinyx has also conducted a
translational sleep study in humans based on these observations on
sleep parameters and NYX-2925 demonstrated significant effects on
multiple sleep measures, including an increase in non-REM sleep, in
that study as well. NMDA receptor-dependent synaptic plasticity
processes are critical for sleep regulation and disrupted sleep is
known to occur in a number of disorders, including chronic pain.
These data support continued exploration of the effect of positive
NMDA receptor modulation on sleep quality and associated downstream
behavioral changes in both preclinical and clinical models.
The third publication is titled “A translational
EEG-based approach to assess modulation of long-lasting
NMDAR-dependent synaptic plasticity” and has been published in
Psychopharmacology. Oral administration of NYX-2925 enhanced alpha
power, increased NMDA receptor-dependent auditory LTP, and
facilitated NMDA receptor-dependent mismatch negativity. The
published studies are the first in vivo demonstration of the
long-lasting effects of positive NMDA receptor modulation on
synaptic plasticity processes using non-invasive EEG techniques.
Aptinyx has also conducted a translational EEG study in healthy
human volunteers in which NYX-2925 was shown to facilitate mismatch
negativity and enhance synaptic plasticity, demonstrating that the
mechanistic activity observed preclinically is consistent with the
activity observed in the human brain.
About NYX-2925NYX-2925 is a novel
oral NMDA receptor modulator currently in Phase 2 clinical
development for the treatment of chronic pain. In clinical studies,
NYX-2925 has been shown to have activity that affects central pain
processing, resulting in alleviation of pain and other symptoms
associated with chronic pain conditions. In Phase 1 and Phase 2
clinical studies, NYX-2925 has exhibited a favorable safety and
tolerability profile across a wide dose range. In preclinical
models of numerous neuropathic pain conditions, NYX-2925 has shown
robust activity with a favorable tolerability profile. The U.S.
Food and Drug Administration has granted Fast Track designation to
Aptinyx’s development of NYX-2925 for the treatment of neuropathic
pain associated with DPN.
About AptinyxAptinyx Inc. is
a clinical-stage biopharmaceutical company focused on the
discovery, development, and commercialization of proprietary
synthetic small molecules for the treatment of brain and nervous
system disorders. Aptinyx has a 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. The company has three product candidates in clinical
development in central nervous system indications, including
chronic pain, post-traumatic stress disorder, and cognitive
impairment associated with Parkinson’s
disease. Aptinyx is also advancing additional compounds
from its proprietary discovery platform, which continues to
generate a rich and diverse pipeline of small-molecule NMDA
receptor modulators with the potential to treat an array of
neurologic disorders. For more information,
visit www.aptinyx.com.
Forward-Looking
StatementsStatements contained in this press release
regarding matters that are not historical facts are
“forward-looking statements” within the meaning of the Private
Securities Litigation Reform Act of 1995. Because such statements
are subject to risks and uncertainties, actual results may differ
materially from those expressed or implied by such forward-looking
statements. Such statements include, but are not limited to,
statements regarding the company’s business plans and objectives,
therapeutic effects of the company’s product candidates,
expectations regarding the design, implementation, timing, and
success of its current and planned clinical studies, and
expectations regarding its uses and sufficiency of capital. Risks
that contribute to the uncertain nature of the forward-looking
statements include: the success, cost, and timing of the company’s
product candidate development activities and planned clinical
studies; the company’s ability to execute on its strategy; positive
results from a clinical study may not necessarily be predictive of
the results of future or ongoing clinical studies; regulatory
developments in the United States and foreign countries; as well as
those risks and uncertainties set forth in the company’s most
recent Annual Report on Form 10-K and subsequent filings with the
Securities and Exchange Commission. All forward-looking statements
contained in this press release speak only as of the date on which
they were made. Aptinyx undertakes no obligation to update such
statements to reflect events that occur or circumstances that exist
after the date on which they were made.
Investor & Media Contact:Nick
SmithAptinyx Inc.ir@aptinyx.com or
corporate@aptinyx.com847-871-0377
Source: Aptinyx Inc.
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