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Research Monograph

ARA-290 (Cibinetide / EPO-Derived Tissue-Protective Peptide)

Also Known AsCibinetide · ARA 290 · pHBSP

Molecular Weight1257.35 g/mol
Discovered2004
Citations4 peer-reviewed
Research Areas5 domains
Background

Developed by Araim Pharmaceuticals based on the tissue-protective domain of erythropoietin (EPO). ARA-290 is a linear 11-amino acid peptide derived from the B-helix surface of EPO that selectively activates the innate repair receptor (IRR), a heterodimer of EPOR and beta common receptor (betaCR/CD131), without stimulating erythropoiesis. This separation of tissue protection from red blood cell production addresses the thrombotic risk of full-length EPO.

Amino Acid SequenceGln-Glu-Gln-Leu-Glu-Arg-Ala-Leu-Asn-Ser-Ser
Mechanisms of Action

How ARA-290 Works

01

Innate Repair Receptor (IRR) Activation

ARA-290 selectively binds the innate repair receptor, a heterocomplex of EPOR and betaCR (CD131) expressed on damaged and inflamed tissues. Unlike full-length EPO, it does not activate the classical homodimeric EPOR responsible for erythropoiesis. IRR activation triggers JAK2-STAT5 signaling in a tissue-protective rather than erythropoietic context.

EPOR/betaCR heterodimerCD131JAK2STAT5
02

Anti-Inflammatory Cytokine Modulation

IRR signaling suppresses NF-kappaB-dependent pro-inflammatory gene transcription, reducing TNF-alpha, IL-1beta, and IL-6 production. Simultaneously, it upregulates anti-inflammatory mediators including IL-10 and TGF-beta, promoting resolution of inflammation in damaged tissues.

NF-kappaBTNF-alphaIL-1betaIL-6IL-10
03

Small Nerve Fiber Repair

ARA-290 promotes regeneration of intraepidermal nerve fibers (IENFs) through IRR-mediated signaling on Schwann cells and dorsal root ganglion neurons. Clinical studies demonstrated increased corneal nerve fiber density and skin biopsy nerve fiber counts in neuropathy patients.

intraepidermal nerve fibersSchwann cellsdorsal root ganglion neuronscorneal nerves
04

Anti-Apoptotic Signaling

IRR activation induces PI3K/Akt-dependent cell survival signaling, upregulating Bcl-XL and inhibiting caspase-3 activation in metabolically stressed cells. This protects neurons, cardiomyocytes, and renal tubular cells from ischemia-reperfusion and inflammatory injury.

PI3K/AktBcl-XLcaspase-3
Evidence-Graded Research Areas

Published Research

Strong
Moderate
Emerging
Preclinical

Diabetic Neuropathy & Small Fiber Neuropathy

Strong

Phase II clinical trials in type 2 diabetic patients with small fiber neuropathy demonstrated statistically significant improvements in corneal nerve fiber density, neuropathic pain scores (NRS), and patient-reported quality of life after 28 days of subcutaneous ARA-290. Intraepidermal nerve fiber regeneration was confirmed by serial skin biopsy.

Sarcoidosis-Associated Neuropathy

Moderate

A phase II trial in sarcoidosis patients with small fiber neuropathy demonstrated reduced neuropathic symptoms, decreased fatigue scores (FAS), and improved corneal nerve fiber morphology. The anti-inflammatory and nerve-regenerative dual mechanism addresses both the underlying granulomatous inflammation and the neuropathic sequelae.

Metabolic Syndrome & Insulin Sensitivity

Moderate

Clinical studies report improvements in HbA1c, insulin sensitivity (HOMA-IR), and cholesterol profiles in diabetic patients treated with ARA-290. The metabolic benefits may be secondary to reduced systemic inflammation and improved autonomic nerve function regulating metabolic homeostasis.

Myocardial Ischemia-Reperfusion Injury

Preclinical

Preclinical models demonstrate reduced infarct size, improved ejection fraction, and decreased cardiomyocyte apoptosis with ARA-290 administration peri-infarction. The IRR is upregulated on stressed cardiomyocytes, providing a therapeutic window for intervention after ischemic insult.

Chronic Kidney Disease

Preclinical

Early preclinical data show renoprotective effects of ARA-290 in ischemia-reperfusion and cisplatin-induced nephrotoxicity models. Renal tubular cell apoptosis was reduced, and inflammatory infiltration was attenuated. The IRR is constitutively expressed on renal tubular epithelium, supporting tissue-specific therapeutic potential.

Safety Profile

ARA-290 has been well tolerated in multiple phase I/II clinical trials involving over 300 subjects. No erythropoietic stimulation (hemoglobin/hematocrit changes) has been observed, confirming selectivity for the IRR over the classical EPOR. Injection-site reactions were the most common adverse event. No thrombotic events, cardiovascular adverse events, or dose-limiting toxicities were reported.

Handling & Storage

Reconstitute with bacteriostatic water. Direct gentle stream along vial wall — do not shake. Store reconstituted solution at 2-8°C and use within 28 days. Lyophilized powder stable at -20°C for 24+ months. ARA-290 is chemically stable and does not require light protection.

References & Citations

Peer-Reviewed Literature

  1. 1

    Nonerythropoietic, tissue-protective peptides derived from the tertiary structure of erythropoietin

    Brines M, Patel NSA, Villa P, et al.

    Proceedings of the National Academy of Sciences, 2008PubMed 18765816DOI
  2. 2

    ARA 290, a nonerythropoietic peptide engineered from erythropoietin, improves metabolic control and neuropathic symptoms in patients with type 2 diabetes

    Brines M, Dunne AN, van Bruggen N, et al.

    Molecular Medicine, 2015PubMed 25387184DOI
  3. 3

    ARA 290 improves symptoms in patients with sarcoidosis-associated small nerve fiber loss and increases corneal nerve fiber density

    Dahan A, Dunne A, Swartjes M, et al.

    Molecular Medicine, 2013PubMed 23887688DOI
  4. 4

    The receptor that tames the innate immune response

    Brines M, Cerami A.

    Molecular Medicine, 2012PubMed 22231731DOI
Frequently Asked Questions

ARA-290 FAQ

What is ARA-290?

ARA-290 (also known as cibinetide) is an 11-amino acid peptide engineered from the tissue-protective domain of erythropoietin (EPO). It selectively activates the innate repair receptor (EPOR/betaCR heterodimer) without stimulating red blood cell production, providing tissue-protective and nerve-regenerative properties without the thrombotic risks of full-length EPO.

How does ARA-290 differ from EPO?

Full-length EPO activates both the classical homodimeric EPOR (driving erythropoiesis) and the heterodimeric innate repair receptor (driving tissue protection). ARA-290 selectively activates only the innate repair receptor. This means it provides neuroprotective and anti-inflammatory effects without increasing hemoglobin, hematocrit, or thrombotic risk.

What clinical evidence exists for ARA-290 in neuropathy?

Phase II trials demonstrated improved corneal nerve fiber density, reduced neuropathic pain scores, and increased intraepidermal nerve fiber counts in patients with diabetic and sarcoidosis-associated small fiber neuropathy. These are the first clinical demonstrations of nerve fiber regeneration in neuropathy patients.

What is the purity of G26x Peptides ARA-290?

Our ARA-290 is 99%+ purity, independently verified by Janoshik Analytical with a full Certificate of Analysis (COA) available for each batch. It is supplied as a lyophilized powder manufactured under GMP-adjacent conditions.

How should ARA-290 be stored?

Lyophilized ARA-290 should be stored at -20°C for long-term storage (stable for 24+ months). Once reconstituted with bacteriostatic water, store at 2-8°C and use within 28 days. ARA-290 is chemically stable and does not require special light protection.

Available for Research

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All compounds 99%+ purity, verified by Janoshik Analytical. GMP-manufactured lyophilized powder.

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Disclaimer: This monograph is provided for educational and research purposes only. G26x Peptides products are sold exclusively as research chemicals. They are not intended for human consumption, therapeutic use, or as dietary supplements. All research should be conducted in compliance with applicable laws and institutional review board protocols. Information presented here is sourced from published peer-reviewed literature and does not constitute medical advice.