Cibinetide

Name:  Lynn
Wechat：  15914422644

Tel：+86  15914422644

Whatsapp: +852 6252 8290

Email：    guangsheng 5   @zgguangsheng.com

1. Core Molecular & Physicochemical Specifications

2. Mechanism of Action

1. IRR Selective Activation: Binds EPOR/CD131 heterodimer (IRR) without activating EPOR homodimers, avoiding erythropoiesis and associated risks like hypertension or thrombosis.
2. Anti - Inflammatory Signaling: Inhibits pro - inflammatory cytokines (IL - 1β, TNF - α) and NF - κB pathway; antagonizes TRPV1 to reduce neurogenic inflammation and pain hypersensitivity.
3. Tissue Protection & Regeneration: Triggers PI3K/Akt and MAPK pathways, enhancing anti - apoptosis, promoting angiogenesis, and stimulating stem cell migration for tissue repair.
4. Metabolic & Skeletal Benefits: Improves glucose tolerance; inhibits osteoclastogenesis to increase bone mineral densityNational Center for Biotechnology Information.

3. Efficacy & Clinical Applications

3.1 Core Preclinical & Clinical Outcomes

3.2 Clinical Applications

• Target Populations: Patients with diabetic neuropathy, sarcoidosis, ischemia - related organ damage, and metabolic bone disorders, where anti - inflammation and tissue repair are prioritized without hematopoietic side effects.
• Key Advantages: No erythropoiesis - related adverse events; multi - tissue protective effects; potential for combination with standard therapies to enhance efficacy.

4. Production & Quality Control

4.1 Manufacturing Process

1. Solid - Phase Peptide Synthesis (SPPS): Assembles the 11 - amino acid sequence; purified via RP - HPLC to ≥98% purity.
2. Lyophilization: Produces stable powder; vacuum - sealed to ensure long - term stability at - 20°C.
3. Batch Testing: Each lot undergoes HPLC purity, mass spectrometry identity, and LAL endotoxin screening before release.

4.2 Quality Testing Standards

5. Administration, Safety & Regulatory Status

5.1 Administration Routes (Clinical/Research)

• Subcutaneous Injection: Weekly dosing (0.5 - 2.0 mg) for systemic effects; preferred for chronic conditions like neuropathy.
• Intravenous Infusion: For acute conditions (e.g., ischemia - reperfusion injury) to achieve rapid tissue exposure.
• Local Delivery: Intravitreal injection for retinal disorders (e.g., diabetic macular edema).

5.2 Safety Profile

• Common AEs: Mild injection - site reactions (pain/redness, <5%); transient fatigue/headache (phase 2, <10%).
• Rare AEs: No hematological abnormalities (no increased hemoglobin/hematocrit); no organ - specific toxicity reported in phase 1 - 2 trials.
• Contraindications: Hypersensitivity to peptide components; use in pregnancy/lactation only with ethical approval (limited data).

5.3 Regulatory Status

• Development Phase: Multiple phase 2 trials ongoing (neurosarcoidosis, diabetic macular edema); discontinued for depression indication.
• Regulatory Filings: No FDA/EMA/NMPA approval yet; available for research use (RUO) from peptide manufacturers.

6. Key Advantages & Limitations

6.1 Advantages

1. IRR - Specific Targeting: Avoids EPO’s hematopoietic side effects, expanding therapeutic window.
2. Multi - Tissue Protection: Acts on nerves, blood vessels, bones, and organs, suitable for comorbid conditions.
3. Favorable Safety: No dose - limiting hematological toxicity, enabling long - term use.

6.2 Limitations

1. Clinical Data Gaps: Limited long - term efficacy/safety data; phase 3 trials pending for key indications.
2. Delivery Constraints: Requires injection (no oral formulation); patient adherence may be affected.
3. Regulatory Uncertainty: Approval timeline unclear; access restricted to clinical trials/research settings.