Product Name: Nerinetide
Form: Free base
CAS No: 500992-11-0
Molar Mass: 2518.88
Chemical Formula: C105H188N42O30
Synonyms: Nerinetide, NA-1
Storage: Store at -20℃
Sequence: YGRKKRRQRRRKLSSIESDV
Target: NMDA Receptor, nNOS
Application:
Nerinetide (CAS: 500992-11-0) presents a groundbreaking opportunity in acute ischemic stroke treatment by addressing critical pathways involved in post-stroke neuronal injury and cell death. Through its unique mechanism, nerinetide intervenes in the interaction between postsynaptic density protein-95 (PSD-95) and the N-methyl-D-aspartate (NMDA) receptor, effectively mitigating excitotoxicity, a primary contributor to neuronal damage following ischemic stroke. Excitotoxicity arises from the excessive influx of calcium ions into neurons, triggering a cascade of events leading to cell death. By blocking the PSD-95/NMDA receptor interaction, nerinetide curtails this cascade, preserving neuronal integrity and function, particularly in the ischemic penumbra, the region surrounding the core infarct where salvageable tissue exists. Preclinical investigations have shown promising results, demonstrating nerinetide's ability to reduce infarct size, improve neurological outcomes, and enhance long-term functional recovery in animal models of ischemic stroke. Building upon these findings, early-phase clinical trials have provided encouraging insights into nerinetide's safety and potential efficacy in human stroke patients. These trials have highlighted its favorable safety profile and early indications of neuroprotective effects, positioning nerinetide as a promising adjunctive therapy to existing treatments. The development of nerinetide signifies a significant advancement in stroke care, offering a targeted approach to neuroprotection that addresses the intricate pathophysiology of ischemic stroke. If successful in larger-scale clinical trials, nerinetide could emerge as a transformative therapeutic option for acute ischemic stroke patients, complementing standard treatments such as thrombolytic therapy and mechanical thrombectomy. By preserving neuronal function and limiting brain injury, nerinetide has the potential to improve clinical outcomes, reduce disability, and revolutionize acute ischemic stroke management on a global scale. Ongoing research efforts continue to explore nerinetide's therapeutic potential and optimize its clinical utility in stroke care. Through rigorous clinical evaluation and further elucidation of its mechanisms of action, nerinetide aims to fulfill its promise as a game-changing intervention in the battle against acute ischemic stroke, a leading cause of morbidity and mortality worldwide.
Current Research:
Nerinetide is an experimental peptide-based therapeutic currently being investigated for its potential in treating neurological conditions, particularly those related to ischemic stroke and neurodegenerative diseases. Nerinetide, also known as NA-1, is designed to target the NMDA (N-methyl-D-aspartate) receptor and has shown promise in preclinical and early clinical studies for protecting brain tissue from damage caused by stroke and other acute neurological insults.
Mechanism of Action
Nerinetide works by modulating the NMDA receptor, a critical player in neuronal communication. Under normal conditions, the NMDA receptor plays an essential role in synaptic plasticity and learning. However, during an ischemic stroke, excessive activation of NMDA receptors leads to an influx of calcium ions, which triggers a cascade of neurotoxic events that result in neuronal cell death and tissue damage.
Nerinetide acts as a selective antagonist of the NMDA receptor, preventing the harmful overactivation of this receptor and thereby reducing the excitotoxic damage typically seen in ischemic conditions. By stabilizing the receptor and limiting calcium influx, Nerinetide helps to preserve neuronal integrity and promote cell survival in the affected brain regions. This mechanism has the potential to minimize the long-term neurological deficits caused by stroke or traumatic brain injury.
Current Research and Development
Nerinetide is currently undergoing clinical trials for ischemic stroke and other neurological disorders. In a significant Phase 3 clinical trial, ESCAPE-NA1, Nerinetide demonstrated promising results in patients with acute ischemic stroke, showing a reduction in the extent of brain damage and improving functional recovery when administered within 24 hours of stroke onset. The treatment was well tolerated, and patients who received Nerinetide showed improvements in neurological outcomes compared to those receiving standard care.
In addition to stroke, Nerinetide is being explored as a potential therapeutic for other neurodegenerative diseases, such as Alzheimer’s disease and traumatic brain injury. Early studies suggest that Nerinetide could offer neuroprotective benefits by mitigating excitotoxicity in these conditions, where similar mechanisms of neuronal damage are at play.
Advantages Over Traditional Therapies
One of the key advantages of Nerinetide is its neuroprotective effect with a specific action on the NMDA receptor, a target that has long been of interest in neurological disease research. Traditional stroke therapies, such as thrombolytics (e.g., tPA), focus on dissolving clots but do not address the underlying neuronal damage caused by excessive excitotoxicity. Nerinetide, on the other hand, offers a complementary approach by targeting the neurotoxic cascade directly, potentially improving long-term recovery.
Another advantage is the timing of administration. While the window for thrombolytic therapy is typically limited to a few hours following stroke onset, Nerinetide can be administered within a longer therapeutic window (up to 24 hours), providing a broader opportunity for treatment and increasing the likelihood of positive patient outcomes.
Future Directions
As research continues, Nerinetide's role in neuroprotective therapy is expected to expand beyond ischemic stroke. The ongoing clinical trials will assess its safety and efficacy in other acute and chronic neurological conditions. Additionally, combination therapies involving Nerinetide and other neuroprotective agents or rehabilitation strategies may be explored to enhance functional recovery and improve long-term quality of life for patients suffering from neurological impairments.
Given the growing global burden of stroke and neurodegenerative diseases, Nerinetide has the potential to make a significant impact in the field of neurology, offering patients a new avenue for protection against irreversible brain damage and improving outcomes in conditions that currently have limited treatment options.
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