Pipeline

Aptinyx’s Development Pipeline

Aptinyx’s proprietary chemistry platform has yielded numerous small-molecule modulators of N-methyl-D-aspartate (NMDA) receptors. A number of these molecules have advanced into clinical development as drug candidates for the treatment of various brain and nervous system disorders. In studies to date, they have demonstrated high oral bioavailability, diverse NMDA receptor subtype binding profiles and differentiated efficacy. Aptinyx’s small-molecule compounds bind to a distinct, recently discovered site on the NMDA receptor to modulate NMDA-receptor channel opening and enhance synaptic plasticity. This mechanism is distinct from any other therapies, emerging or marketed, for multiple challenging neurologic disorders.

Pipeline of novel oral NMDA receptor modulators discovered from Aptinyx’s proprietary chemistry platform
Compound
Indication
Pre-IND
Phase 1
Phase 2
Phase 3
Painful Diabetic
Peripheral Neuropathy
Fibromyalgia
(Exploratory)
Post-Traumatic Stress Disorder

NYX-2925

NYX-2925 is a novel, oral, small-molecule NMDA receptor modulator in clinical development as a therapy for neuropathic pain.

NYX-2925 has demonstrated robust efficacy in preclinical models of numerous neuropathic pain conditions with a favorable safety profile. In a Phase 1 clinical study in healthy human subjects, NYX-2925 was well tolerated across a wide dose range, including dose levels well in excess of the expected therapeutic levels.

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. Two Phase 2 clinical studies of NYX-2925 are currently ongoing in subjects with painful DPN and in subjects with fibromyalgia.

See the Clinical Studies page to learn more about ongoing studies with NYX-2925.

NYX-783

NYX-783 is an NMDA receptor modulating small molecule in clinical development as a therapy for post-traumatic stress disorder (PTSD).

As learning processes are involved in fear extinction, NYX-783’s mechanism of enhancing synaptic plasticity and facilitating learning is highly relevant in PTSD. NYX-783 has demonstrated robust and long-lasting efficacy in preclinical models of depression, learning, and fear extinction, as well as a favorable safety profile. These findings suggest NYX-783 may target the underlying cause of PTSD, not simply palliate its symptoms.

NYX-783 is currently in a Phase 1 study to establish safety and tolerability. The U.S. Food and Drug Administration has granted Fast Track designation to Aptinyx’s development of NYX-783 for the treatment of PTSD.

Platform

Aptinyx has a robust and growing chemistry platform, enabling discovery and design of small-molecule compounds that elegantly modulate the NMDA receptor. The company has developed a discovery screening and profiling process to rapidly assess the binding and functional properties of these NMDA receptor modulators. To date, Aptinyx compounds have shown efficacy in a number of preclinical models of depression, neuropathic pain, migraine, PTSD, neuroprotection, cognitive function and impairment, and sleep, among others. Aptinyx is rapidly progressing the most promising of these drug candidates in preclinical and clinical development.