Imunofan
Imunofan (Arg-Asp-Lys-Val-Tyr-Arg) is a synthetic hexapeptide derived from a modified thymopoietin fragment, developed in Russia as an immunomodulator with antioxidant and hepatoprotective properties. It is used clinically as an adjunct in HIV, cancer, and chronic hepatitis.
Imunofan is a synthetic hexapeptide with the sequence Arg-Asp-Lys-Val-Tyr-Arg, derived from a structurally modified fragment of thymopoietin (residues 32-36 with additional modifications). Developed at the Institute of Immunology in Moscow by V.V.
Overview
Imunofan represents a second-generation approach to thymic peptide therapy. Rather than using natural thymic extracts, it was rationally designed as a modified fragment of thymopoietin with improved stability and broader pharmacological activity. The peptide has been studied in over 100 clinical investigations in Russia and has accumulated a substantial body of clinical evidence within the Russian medical literature, though Western peer-reviewed data remains limited.
The drug is notable for its three-phase action profile: a fast phase (2-3 hours) involving antioxidant enzyme activation, an intermediate phase (2-3 days) involving immune cell activation and cytokine modulation, and a slow phase (up to 4 months) involving sustained immunoregulatory effects including normalization of immunoglobulin levels.
Mechanism of Action
Imunofan operates through a multi-phase mechanism that distinguishes it from other thymic peptides:
Phase 1 — Antioxidant (0-3 hours): Within minutes of administration, Imunofan activates the ceruloplasmin-transferrin antioxidant system. It increases ceruloplasmin catalytic activity by 30-40%, enhances the activity of catalase and glutathione peroxidase, and reduces lipid peroxidation. This rapid antioxidant response provides cytoprotection and reduces oxidative damage to immune cells.
Phase 2 — Immune correction (2-3 days): Imunofan stimulates phagocytic activity of neutrophils and macrophages, enhances NK cell cytotoxicity, and promotes the differentiation and functional maturation of T lymphocytes. It increases the production of IL-2 by T-helper cells and modulates the expression of CD4 and CD8 markers, helping restore the helper/suppressor ratio in immunodeficient patients.
Phase 3 — Immunoregulation (7 days to 4 months): The peptide normalizes the production of immunoglobulins, particularly IgA and IgG, and stabilizes the balance between Th1 and Th2 cytokine profiles. This phase is responsible for the sustained clinical benefit observed after treatment courses.
Hepatoprotective effects: Imunofan activates hepatic antioxidant defenses and reduces inflammation-mediated liver damage, making it useful as an adjunct in chronic hepatitis. It enhances the detoxification capacity of the liver by upregulating cytochrome P450 enzymes and glutathione-S-transferase activity.
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Research
Vaccine Adjuvant Effects
Research has explored Imunofan as a vaccine adjuvant, particularly for improving immune responses in immunocompromised populations. When co-administered with hepatitis B vaccine in immunodeficient patients, Imunofan significantly increased seroconversion rates and antibody titers compared to vaccine alone.
HIV Adjunct Therapy
Clinical studies in HIV-positive patients demonstrated that Imunofan courses (administered alongside antiretroviral therapy) improved CD4+ T-cell counts, reduced viral load, and decreased the frequency of opportunistic infections. The peptide was particularly effective in patients with CD4 counts between 200-500 cells/mm3, where it helped delay progression to AIDS-defining illness. These results have been published primarily in Russian-language journals.
Chronic Hepatitis
In patients with chronic hepatitis B and C, Imunofan administered as suppositories (100 mcg daily for 20 days) reduced serum aminotransferase levels, decreased markers of oxidative stress, and improved histological activity scores on liver biopsy. The hepatoprotective effects were attributed to both direct antioxidant action and modulation of the immune-mediated hepatocyte damage characteristic of viral hepatitis.
Antioxidant Properties and Cytoprotection
Studies on the antioxidant effects of Imunofan demonstrated that a single dose can increase ceruloplasmin activity by 30-40% within 2-3 hours, with concurrent reductions in malondialdehyde (a marker of lipid peroxidation). In models of ischemia-reperfusion injury, Imunofan pretreatment significantly reduced tissue damage and inflammatory cell infiltration, suggesting a protective role against oxidative stress in clinical settings (Lebedev et al., 1999).
NK Cell Activation and Cancer Adjunct
In patients with solid tumors undergoing chemotherapy, Imunofan administration (1 mL of 0.005% solution subcutaneously, every other day for 10 injections) restored NK cell cytotoxicity to near-normal levels and improved the CD4/CD8 ratio. A study in patients with gastric cancer showed that Imunofan adjunct therapy reduced postoperative infectious complications by 2.5-fold and improved 2-year survival compared to chemotherapy alone (Pokrovsky et al., 2002).
Safety Profile
Imunofan has been administered to tens of thousands of patients in Russia since its registration in 1996, with a well-documented safety profile in the Russian medical literature. Side effects are rare and generally mild, including occasional transient pain at the injection site and, rarely, mild allergic reactions. No cases of immunosuppression, autoimmune disease exacerbation, or serious adverse events have been reported in the published literature. The peptide does not cause hyperstimulation of the immune system, which differentiates it from some other immunomodulators. Formal Western regulatory safety studies have not been conducted.
Pharmacokinetic Profile
Imunofan — Pharmacokinetic Curve
Subcutaneous, intramuscular, intranasal, rectal (suppository)Quick Start
- Route
- Subcutaneous, intramuscular, intranasal, rectal (suppository)
Molecular Structure
- Formula
- C36H61N13O10
- Weight
- 836 Da
- CAS
- 130513-78-1
- PubChem CID
- 15788399
- Exact Mass
- 835.4664 Da
- LogP
- -7.8
- TPSA
- 421 Ų
- H-Bond Donors
- 14
- H-Bond Acceptors
- 14
- Rotatable Bonds
- 28
- Complexity
- 1450
Identifiers (SMILES, InChI)
InChI=1S/C36H61N13O10/c1-19(2)28(33(57)48-25(17-20-10-12-21(50)13-11-20)31(55)46-24(34(58)59)9-6-16-44-36(41)42)49-30(54)23(8-3-4-14-37)45-32(56)26(18-27(51)52)47-29(53)22(38)7-5-15-43-35(39)40/h10-13,19,22-26,28,50H,3-9,14-18,37-38H2,1-2H3,(H,45,56)(H,46,55)(H,47,53)(H,48,57)(H,49,54)(H,51,52)(H,58,59)(H4,39,40,43)(H4,41,42,44)/t22-,23-,24-,25-,26-,28-/m0/s1
UIPUKCRNGDAFKO-BIVGDOEESA-NResearch Indications
Tissue Repair
In vitro studies in human fibroblast and keratinocyte cell lines demonstrated statistically significant pro-proliferative activity, suggesting potential for wound healing applications. Clinical validation ongoing.
Investigated as adjunct therapy in type 2 diabetes patients with diabetic foot syndrome. Immunomodulatory and antioxidant properties may support healing in compromised tissue.
Immunomodulation
Hexapeptide (RDKVYR) derived from thymopoietin positions 32-37. Restores disturbed cellular and humoral immunity to reference values through a three-phase mechanism over 2 hours to 4 months. Approved in Russia for 25+ years.
Indicated for cytomegalovirus, herpes, toxoplasmosis, chlamydia, pneumocystosis, and cryptosporidiosis. Enhances phagocytosis and intracellular killing of bacteria and viruses during the middle phase (days 2-10).
Hepatoprotection & Detoxification
Prevents hepatic cytolysis, reduces transaminase activity and bilirubin concentration. Enhances antioxidant defense by stimulating ceruloplasmin, lactoferrin production, and catalase activity within 2-3 hours.
Research Protocols
intranasal Injection
Administered via intranasal.
| Goal | Dose | Frequency | Duration |
|---|---|---|---|
| Patients with chronic hepatitis B and C | 100 mcg | Daily | 20 days |
subcutaneous Injection
NK Cell Activation and Cancer Adjunct In patients with solid tumors undergoing chemotherapy, Imunofan administration (1 mL of 0.005% solution subcutaneously, every other day for 10 injections) restored NK cell cytotoxicity to near-normal levels and improved the CD4/CD8 ratio.
| Goal | Dose | Frequency | Duration |
|---|---|---|---|
| Patients with chronic hepatitis B and C | 100 mcg | Daily | 20 days |
intramuscular Injection
Administered via intramuscular injection.
| Goal | Dose | Frequency | Duration |
|---|---|---|---|
| Patients with chronic hepatitis B and C | 100 mcg | Daily | 20 days |
Interactions
Peptide Interactions
Imunofan has been used clinically in Russia to mitigate cyclophosphamide-induced immunosuppression. It restores T-cell function and antioxidant capacity (ceruloplasmin, catalase activity) reduced by alkylating chemotherapy, without interfering with the cytotoxic antitumor mechanism (Lebedev et al., 1999).
Both imunofan and thymalfasin are immunomodulatory peptides that enhance T-cell function. Imunofan (a thymopentin derivative) and thymalfasin activate overlapping immune pathways. Concurrent use may produce excessive immune stimulation; clinical monitoring of immune markers is advisable (Khaitov & Pinegin, 2000).
What to Expect
What to Expect
Effects begin within hours of administration based on half-life of ~2-3 hours
Imunofan operates through a multi-phase mechanism that distinguishes it from other thymic peptides: Phase 1 — Antioxidant (0-3 hours): Within minutes...
Phase 2 — Immune correction (2-3 days): Imunofan stimulates phagocytic activity of neutrophils and macrophages, enhances NK cell cytotoxicity, and...
Phase 3 — Immunoregulation (7 days to 4 months): The peptide normalizes the production of immunoglobulins, particularly IgA and IgG, and stabilizes...
In patients with chronic hepatitis B and C, Imunofan administered as suppositories (100 mcg daily for 20 days) reduced serum aminotransferase levels,...
Quality Indicators
Red flags
- Significant side effect risk noted
- Liver toxicity concerns reported
Frequently Asked Questions
References (4)
- [1]Lebedev VV et al Imunofan — regulatory peptide in the therapy of infectious and noninfectious diseases Immunologiya (1999)
- [2]Pokrovsky VS et al Immunomodulatory therapy in oncology Bull Exp Biol Med (2002)
- [3]Lebedev VV Imunofan is a synthetic peptide analogue of thymopoietin: pharmacological and immunological properties Immunologiya (1999)
- [4]Tutel'ian AV et al Immunomodulatory properties of imunofan Vestn Ross Akad Med Nauk (2005)
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