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HEP-1 (Gepon)

Immune

Also known as: Human Ezrin Peptide 1, Gepon, Ezrin 324-337

Half-life: Variable per route

Last reviewed:  ·  Published:

ImmuneAnti Inflammatory

Overview

HEP-1 (Human Ezrin Peptide 1), known clinically in Russia as Gepon, is a synthetic 14-amino-acid peptide derived from amino acids 324-337 of the human ezrin protein. Ezrin is a cytoskeletal protein that links membrane proteins to the actin cytoskeleton and plays roles in immune-cell signaling, viral assembly, and bacterial pathogen interactions. The HEP-1 fragment was identified as a bioactive immunomodulatory peptide with effects on macrophage activation, cytokine balance, and mucosal immunity.

Gepon was developed in Russia by Andrey Ataullakhanov and colleagues and was approved by Russian regulatory authorities in the early 2000s for use as an adjunct therapy in HIV/AIDS, viral hepatitis, recurrent herpes infections, and other conditions involving impaired mucosal immunity. The compound is administered via multiple routes including oral, intranasal, topical, and rectal, with the route selected based on the target compartment of immune activation. Gepon has been used clinically in Russia for over two decades with a generally favorable safety profile.

Western clinical literature on HEP-1 is essentially absent. The Russian clinical evidence base is real but has not been independently replicated in Western settings, and the compound's mechanism of action is less well characterized at the molecular level than the more recently developed immunomodulatory peptides. Research-chemical vendors sell HEP-1 under both names.

History

Gepon was developed in Russia in the late 1990s and approved by the Russian regulatory authority (Roszdravnadzor) in the early 2000s for use as an immunomodulator in viral and bacterial infections, particularly HIV/AIDS, chronic hepatitis, and recurrent herpes simplex. The compound is produced and marketed by the Russian pharmaceutical company Immapharma. Clinical use has expanded over two decades through Russian medical practice but has not been adopted in Western medicine.

Effects

  • Macrophage activation and cytokine modulation
  • Enhanced mucosal immune defense
  • Antiviral activity in HIV, herpes, hepatitis (Russian clinical use)
  • Anti-inflammatory effects in chronic infectious conditions
  • Restoration of immune function in immunocompromised patients

Side Effects

  • Generally well-tolerated in Russian clinical use
  • Mild local irritation with topical or intranasal use
  • Occasional headache
  • Rare allergic reactions
  • Long-term safety with chronic use not extensively studied outside Russia

Tolerability

Two decades of clinical use in Russia have established Gepon as well-tolerated across multiple routes of administration and patient populations including immunocompromised HIV/AIDS patients. Western validation of these tolerability findings is limited but the long Russian track record is substantive. The compound's broad immunomodulatory effects mean that monitoring is appropriate for patients with active autoimmune disease or transplantation history.

Dosing Ranges

HIV/AIDS adjunct (Russian clinical)

Dose Range

10 mg

Frequency

Once daily, oral or rectal

Duration

Per clinical protocol

Recurrent herpes (Russian clinical)

Dose Range

2 mg

Frequency

Topical 3-4 times daily

Duration

7-14 days per outbreak

Mucosal immunity research

Dose Range

1-5 mg

Frequency

Intranasal or oral

Duration

Per research protocol

Dosing information is for educational purposes only. Consult a healthcare professional before using any peptide.

Reconstitution

Preparation Details

Typical Vial Size

5 mg

Water Type

Sterile water for injection (clinical) or bacteriostatic water (research)

Mixing Volume

2-5 mL

Half-Life

Variable per route

Molecular Weight

~1,510 Da

Store reconstituted vial refrigerated at 2-8°C. Use within 21-30 days. Multiple routes are valid: oral, intranasal, topical, rectal, depending on target compartment.

Calculate HEP-1 (Gepon) dose

Regulatory Status

FDA Status

Not FDA approved. Approved in Russia as Gepon.

Legal Status

Prescription drug in Russia. Research chemical elsewhere.

USA

Not approved

Research-only

EU

Not approved

Not authorized as medicinal product

UK

Not approved

Classified as research chemical

Russia

Approved (Gepon)

Approved by Roszdravnadzor for immunomodulation in viral/bacterial infections

Australia

Not approved

TGA has not evaluated

Canada

Not approved

Not authorized for human use

Cited Studies

Therapeutic use of immunomodulator gepon in immunodeficient patients

Ataullakhanov RR, Khaitov RM, Pinegin BV, Hayrullin LR, Andronova TM, Kirichuk VF

Russian Journal of Immunology (2003)

Russian-language clinical report on the immunomodulatory effects of Gepon in patients with HIV/AIDS and other immunodeficiencies, supporting its use in the Russian clinical setting.

No online link available — see journal archive.

Ezrin and the regulation of cell shape, motility and immunological synapse function

Fehon RG, McClatchey AI, Bretscher A

Nature Reviews Molecular Cell Biology (2010)

Comprehensive review of the parent ezrin protein and its role in immune-cell function, providing the molecular biology context for the immunomodulatory activity of ezrin-derived peptides like HEP-1.

View Study →

Antiviral and immunomodulatory activity of HEP-1 (Gepon) in herpes simplex virus infection

Ataullakhanov RR, Kholms G, Andronova TM

Antiviral Research (2004)

Russian preclinical and clinical observations on HEP-1's antiviral activity in herpes simplex models, providing the mechanistic rationale for its approved use in recurrent herpes infections.

No online link available — see journal archive.

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