This product is a box of 10 vials.
What is ARA-290?
ARA-290 is a version of erythropoietin that reduces inflammation through paracrine signaling and innate repair receptors. Studies show it can lower HbA1c levels, improve cholesterol, ease neuropathic pain, and promote wound healing.
ARA-290 is a small peptide that comes from the helix beta part of erythropoietin (EPO). For a long time, EPO has been recognized for doing more than just boosting red blood cell production in the bone marrow. This glycoprotein, produced in the kidneys, also encourages blood vessel growth, helps cells survive, changes blood pressure, and offers protective effects for nerves in diabetic neuropathy. ARA-290 provides the nerve-protecting and pain-relieving benefits of EPO without increasing red blood cell production. It has finished phase II trials and is getting ready for phase III trials to treat conditions related to diabetes and the autoimmune disease sarcoidosis. Currently, researchers are focusing on its potential to manage neuropathic pain. They are also exploring it as a way to speed up wound healing in long-term diabetes, as an immune-modulating drug, and as a possible therapy for systemic lupus erythematosus (also known as lupus or SLE).
Sequence:Â ZEQLERALNSS
Molecular Formula:Â C51H84N16O21
Molecular Weight:Â 1257.3 g/mol
PubChem CID:Â 91810664
CAS No:Â 1208243-50-8
Synonyms:Â cibinetide, PH-BSP
Blood Vessel Health
Retinal ischemia stems from various diseases and ranks as a top cause of blindness in developed countries. Protecting retinal epithelial cells from damage or aiding their regrowth after injury could greatly lessen the impact of these conditions. In mouse studies, ARA-290 shields endothelial colony-forming cells from inflammation's harmful effects. This action extends cell life and assists these cells in repairing and rebuilding blood vessels.
Additional research in mice reveals that ARA-290 boosts the growth, movement, and survival of endothelial colony-forming cells across the blood vessels. It seems to improve their ability to home in on damaged areas that need repair. Experts hope this feature could enhance the work of the body's own cells and make transplanted ones more effective at fixing blood vessels and restoring flow to oxygen-deprived tissues. If it works well with cell transplants, ARA-290 might open doors to new treatments. These could involve successfully transplanting functional cells for tasks like tissue repair, hormone creation, protein production, and beyond.
Reducing Inflammatory Cytokines
Mouse studies demonstrate that ARA-290 can support the survival of transplanted islet cells by blocking macrophage activation. For decades, endocrinologists have dreamed of treating diabetes by transplanting healthy insulin-producing islet cells. Unlike injected insulin, these cells offer more natural blood sugar control and cut down on complications that arise even in well-managed diabetes. Sadly, transplanted islet cells often don't last long, leading to the approach being mostly set aside. But ARA-290's development might shift that trend. Research in mice indicates the peptide's power to curb inflammatory cytokines such as IL-6, IL-12, and TNF-alpha, which greatly extends islet cell survival. ARA-290's skill in guarding against typical inflammatory reactions likely comes from its attachment to the tissue-protective receptor (TPR). This boosts tissue defense and aids in balancing the immune system. EPO binds to the TPR too, but it brings unwanted side effects related to the heart, blood, and other areas, making it unsuitable for many uses. By linking to the TPR without triggering EPO's other effects, peptides like ARA-290 lower cell death and reduce harmful inflammatory cytokines. Overall, this leads to better tissue protection and regeneration. Such benefits result in lower illness and death rates, quicker wound healing, less scarring, and faster recovery of function after injuries.
Tissue Protection
Studies in mice indicate that ARA-290 supports the survival of transplanted islet cells by curbing macrophage activation. Endocrinologists have long viewed transplanting healthy insulin-producing islet cells as the ideal diabetes treatment. These cells provide more natural blood sugar regulation than external insulin, which helps avoid complications common in even tightly controlled diabetes. However, islet cells rarely survive long after transplant, so the method has largely been dropped. ARA-290's emergence could change this. Mouse research shows the peptide suppresses inflammatory cytokines like IL-6, IL-12, and TNF-alpha, leading to much longer survival for transplanted islet cells. The way ARA-290 defends against standard inflammatory responses appears tied to its binding with the tissue-protective receptor (TPR). This enhances tissue safeguarding and helps manage the immune system. While EPO also connects to the TPR, its various heart-related and blood-forming side effects make it impractical for widespread use. Peptides like ARA-290, by attaching to the TPR without those extra effects, decrease cell death and limit damaging inflammatory cytokines. In the end, this promotes tissue protection and better regeneration, which means less severe illness, faster healing of wounds, reduced scars, and quicker return to normal function after harm.
Immune System
The TPR appears on various immune cells, such as macrophages, dendritic cells, mast cells, and lymphocytes (especially T-cells). Growing evidence points to ARA-290 and similar peptides binding to this TPR on immune cells, directly influencing how they work.
For macrophages, ARA-290's stimulation of the TPR sharply cuts the release of proinflammatory cytokines like TNF-alpha and IL-6. Even though this toned-down immune response can slow pathogen removal in some cases, it eases disease intensity and stops chronic issues from taking hold. Studies also reveal that TPR activation limits macrophage chemokine pathways, reducing inflammatory cytokine influx while encouraging resident macrophages to gather at injury sites. The outcome tends to be stronger tissue repair with fewer inflammatory drawbacks.
Further studies suggest ARA-290 could change how dendritic cells present antigens, affecting adaptive immunity that builds lasting defense against known pathogens. At first glance, this might seem harmful, but keep in mind that adaptive immunity drives much of the rejection in organ and tissue transplants. Fine-tuning this process could lower rejection risks in procedures like kidney, heart, or bone marrow transplants, as well as experimental ones.
ARA-290 holds promise as an immune modulator in several areas, including colitis. This condition can arise from infections or chronic autoimmune issues, like those in Crohn's disease and ulcerative colitis. Right now, treatments for autoimmune colitis mainly involve injections with many side effects. More targeted immune modulators like ARA-290 could relieve the burden for people with inflammatory bowel disease.
Another promising use for ARA-290's immune effects is treating systemic lupus erythematosus (SLE). In mouse models, giving ARA-290 lowers autoantibodies (such as ANA and anti-dsDNA), which mark SLE and signal its severity. It also reduces kidney harm, a common cause of health problems and death in SLE. These results hint that ARA-290 could become the first focused therapy for this condition.
Pain Perception
Experts have known for years that the immune system influences how we feel pain (nociception), but creating regulators for this has proven tough. The immune system plays a key role in neuropathic pain, like the kind from diabetes. This type of pain resists control, yet studies show targeting the innate repair receptor (IRR) can reduce inflammation and ease it. ARA-290 interacts with this receptor, and recent work suggests it also blocks TRPV1 channel activity. Known as the capsaicin receptor, TRPV1 handles heat sensation and the burning pain linked to neuropathy. ARA-290's effect on this receptor might help treat pain from diabetes, multiple sclerosis, chemotherapy, and amputations.
Small nerve fiber loss often happens in autoimmune diseases like sarcoidosis and diabetes. Called small fiber neuropathy, it occurs when skin fibers for sensing temperature and pain break down. Symptoms vary in strength but might feel like pins and needles or sand in your shoe. The pain tends to come and go sharply, hitting several times daily. In severe cases, it turns constant and feels like burning. Studies on people with small fiber loss show ARA-290 boosts small nerve fiber numbers and cuts pain a lot. This implies it could effectively treat nerve damage in sarcoidosis, diabetes, thyroid issues, celiac disease, HIV, and similar conditions.
Orphan Drug
In 2016, Araim Pharmaceuticals shared that the FDA gave orphan drug status to explore daily cibinetide for treating painful sarcoid neuropathy. The next year, Chief Science Officer Michael Brines and colleagues published findings on ARA-290's benefits for peripheral and small fiber nerve pain.
Dr. Brines and his team noted that ARA-290 (cibinetide) is heading into phase 3 trials for neuropathy. This peptide could help the about 87 million Americans with nerve damage and related issues. It even shows promise in speeding up slow wound healing in diabetic mice, which might prevent amputations and chronic ulcers that many diabetics face later.
Summary
ARA-290 has drawn main interest for its unique way of handling neuropathic pain, but it also stands out for immune modulation, wound repair stimulation, and potential protection of blood vessels during low-oxygen events. Research is most advanced in its role for modulating neuropathic pain. The peptide is now in phase II and III trials for diabetic neuropathy and sarcoid neuropathy. There's growing curiosity about using it for systemic lupus erythematosus and pain from multiple sclerosis, HIV, celiac disease, and more. Interest is also rising in ARA-290 as a way to alter disease in inflammatory bowel conditions.
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