- Mechanism
- Activates innate repair receptor (IRR)
- Typical research dose
- 2-4 mg/day subcutaneous (in trials)
- Route
- subcutaneous
- Half-life
- < 1 hour (biological effects last longer)
- Legal status
- Investigational / Clinical Trials
Overview
ARA-290 (Cibinetide) is a synthetic, non-hematopoietic peptide engineered from the structure of erythropoietin (EPO). It selectively binds to the innate repair receptor (IRR) to modulate immune responses, reduce inflammation, and promote tissue healing without stimulating red blood cell production. By targeting specific inflammatory pathways, the ARA-290 (Cibinetide) peptide offers significant therapeutic potential for managing neuropathic pain, protecting transplanted tissues, and addressing complications associated with diabetes and sarcoidosis.
Potential Benefits
- Neuropathic Pain Relief: Clinical trials demonstrate that ARA-290 significantly improves symptoms of small fiber neuropathy in patients with sarcoidosis and type 2 diabetes (Dahan A et al., 2013).
- Nerve Fiber Regeneration: Studies show the peptide can increase corneal nerve fiber density, indicating active nerve repair and regeneration (van Velzen M et al., 2014).
- Metabolic Control in Diabetes: Research indicates that ARA-290 improves metabolic control and reduces neuropathic symptoms in patients with type 2 diabetes (Brines M et al., 2015).
- Anti-Inflammatory Action: The peptide dampens innate immune cell functions and macrophage activation, showing efficacy in ameliorating experimental colitis (Nairz M et al., 2017).
- Tissue Protection and Engraftment: Cibinetide protects isolated human islets in stressful environments, preventing damage and improving engraftment success during transplantation (Yao M et al., 2021).
Where to Buy ARA-290 (Cibinetide)
Research compound. ARA-290 (Cibinetide) is a research chemical, typically not FDA-approved for human consumption. Sale or use for human consumption may be illegal in your jurisdiction.
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Verify third-party COAs and consult a qualified healthcare provider before using any compound.
Side Effects
Common side effects:
- Injection site redness or irritation
- Mild transient headache
- Nausea or gastrointestinal upset
- Fatigue
- Dizziness
Rare or serious side effects:
- Allergic reactions
- Unintended immune modulation
- Unpredicted drug interactions
ARA-290 (Cibinetide) is not FDA-approved and is intended for research purposes only. Consult a qualified healthcare provider before use.
Mechanism of Action
Innate repair receptor activation is the primary mechanism through which ARA-290 (Cibinetide) exerts its therapeutic effects. Unlike native erythropoietin, which binds to the homodimeric EPO receptor to stimulate red blood cell production, ARA-290 selectively targets the heteromeric innate repair receptor (IRR) composed of EPO and beta-common receptor subunits. This specific binding initiates a cascade of intracellular signaling pathways that suppress the production of pro-inflammatory cytokines while promoting cellular survival and tissue repair.
Modulation of nociception and immune response further explains the profound pain-relieving properties of the ARA-290 peptide. Research indicates that it relieves pathophysiological pain by targeting the TRPV1 channel, effectively integrating the immune system with pain signaling pathways (Zhang W et al., 2016). By inhibiting macrophage activation and dampening innate immune cell functions, Cibinetide creates a microenvironment conducive to nerve regeneration and reduced neuroinflammation.
Origin & History
Engineered from erythropoietin, ARA-290 was developed to harness the tissue-protective and anti-inflammatory properties of EPO without triggering unwanted erythropoiesis. Researchers synthesized this 11-amino acid peptide by mapping the specific domain of EPO responsible for binding to the innate repair receptor. This breakthrough allowed for the targeted treatment of inflammatory and neuropathic conditions without the cardiovascular risks associated with elevated hematocrit levels.
Clinical trial progression has marked the development of ARA-290 (Cibinetide) across multiple therapeutic areas. The peptide has been evaluated in Phase 2 trials for conditions such as sarcoidosis-associated small nerve fiber loss (NCT02039687) and type 2 diabetes (NCT01933529). While it remains an investigational compound without full FDA approval for widespread clinical use, its orphan drug designation for sarcoidosis highlights its significant potential in addressing unmet medical needs.