Description
What is ARA-290 (Cibinetide)?
ARA‑290 (cibinetide) is a synthetic 11‑residue peptide mimicking the surface of helix B of erythropoietin (EPO). EPO’s tissue‑protective effects are mediated by a heterodimeric “innate repair receptor” (IRR) composed of the EPO receptor plus the CD131 common β‑chain, pharmacologically separable from the classical erythropoietic EPO homodimer receptor. ARA‑290 selectively engages the IRR, retaining EPO’s neuroprotective and anti‑inflammatory activity without raising hemoglobin or thrombotic risk.
Mechanism of Action
- Selective agonist at the heterodimeric EPO receptor / CD131 innate repair receptor (IRR)
- No binding at the classical EPOR‑homodimer → no erythropoiesis or prothrombotic risk
- Reduces pro‑inflammatory cytokine production (TNF‑α, IL‑6)
- Neuroprotective in preclinical models of peripheral neuropathy and ischemic injury
- Rapid plasma clearance (~2 min half‑life) with durable tissue effect (allosteric receptor modulation)
Compound Properties
- Sequence: pyro‑Glu‑Glu‑Gln‑Leu‑Glu‑Arg‑Ala‑Leu‑Asn‑Ser‑Ser (11‑aa)
- Molecular weight: ~1257.3 g/mol
- Form: Lyophilized powder
- Unit size: 10 mg / vial
- Source: Solid‑phase peptide synthesis; ≥98% purity by HPLC
Research‑Reference Dosing
Published research‑reference ranges in clinical literature:
- Brines et al., Molecular Medicine (2008): foundational IRR/ARA‑290 pharmacology.
- Dahan et al., Anesthesiology (2013): ARA‑290 in sarcoidosis‑associated small‑fiber neuropathy — 8 mg SC daily reduced neuropathic pain scores.
- Heij et al., Molecular Medicine (2012, 2017): diabetic neuropathy Phase 2 studies.
- Brines, Drugs in R&D: IRR biology and cibinetide program review.
Research Findings
- Improved neuropathic pain scores and corneal nerve fiber density in sarcoidosis small‑fiber neuropathy (Dahan 2013)
- Improved metabolic and neuropathic endpoints in Type 2 diabetic neuropathy Phase 2 (Heij 2017)
- No effect on hemoglobin or thrombotic markers across trials
- Investigated for DPN, sarcoidosis, optic neuritis, and macular disease
Known Side Effects Reported in Research/Trials
- Injection‑site reactions
- Transient mild headache
- Generally very well tolerated; key differentiator is the absence of EPO‑class hematologic/thrombotic risk
- Long‑term safety data beyond Phase 2 timeframes is limited
Storage & Handling
- Lyophilized (unreconstituted) vials: store at −20°C long‑term; short‑term 2–8°C acceptable.
- After reconstitution with bacteriostatic or sterile water: store at 2–8°C; use within 14–28 days per standard peptide stability guidance.
- Protect from light, heat, and repeated freeze‑thaw cycles. Handle in a sterile laboratory environment.
Certificate of Analysis
A Certificate of Analysis (COA) confirming identity and purity by HPLC / MS is available upon request. Contact Lonestar Peptides for lot‑specific documentation.
Summaries reference peer‑reviewed preclinical and clinical literature available as of early 2025. Newer findings may not be reflected. Researchers should consult current literature and conduct their own due diligence. Lonestar Peptides makes no claim of therapeutic benefit.
