An innate immunity receptor agonist
What is Licopid (GMDP)?
Licopid is an immunomodulator of the last generation containing full synthetic analogue of the natural peptidoglycan (GMDP or glucosaminylmuramyldipeptide), being the minimal biologically active fragment of bacterial cell wall structure. Once in the body, Licopid imitates the natural discovery process of peptidoglycan fragments of bacteria. Therefore, effect of this drug is as close as possible to the natural immunoregulation process implemented in the body under the effect of pathogenic bacteria.
CLASSIFICATION OF MICROBIAL IMMUNOMODULATORS
Classification of microbial immunomodulators under Kozlov I.G. (Head of Laboratory of Experimental Immunology and Immunopharmacology of the Federal Scientific and Clinical Center for Pediatric Hematology, Oncology and Immunology, Vice President of the Russian Scientific Society of Immunologists) 2005.
0 generation — Living bacteria
- I generation — Lysates of microorganisms
II generation — Partially refined components
- Nucleic acids
III generation — Minimal biologically active fragments
- Glucosaminylmuramyldipeptide (GMDP) — (Licopid)
- CpG oligonucleotides
WHAT IS GMDP?
Each microbial cell “wears” external safety coating called “cell wall”, significant part of which is formed by a peptidoglycan. The latter consists of recurrent fragments forming a frame. From the one side, peptidoglycan, its structural components, protect bacterial cell, whereas, from the other side, they “yield up” its affiliation with microbial world.
Effective substance of Licopid is GMDP (glucosaminylmuramyldipeptide), being the fully synthetic analogue of recurrent fragment of peptidoglycan of Gram+ and Gram- bacteria.
In the body, GMDP is naturally formed under the effect of various hydrolytic enzymes breaking down the bacterial cell wall.
HOW DOES LICOPID WORK?
Licopid® (GMDP) is one of immunomodulators with known and predictable effect, providing it a clear advantage.
Pharmacologic activity of drug is achieved by binding of its effective agent – GMDP with intracellular receptor of innate immunity NOD2 (Girardin S.E., 2003; Meshcheryakova E., 2007). GMDP binding with the receptor results in a series of intracellular events ending by activation of nuclear factor (NF) and production of a series of key cytokines— IL-1, IL-6, IL-12, TNF-α, interferon-gamma, and colony-stimulating factors (CSF).
By influence on key molecular target (receptor) in immune system, GMDP as part of Licopid imitates the natural discovery process of peptidoglycan fragments in bacteria.
Discovery of innate immunity receptors and description of the methods operation of innate immunity was awarded the Nobel Prize in Physiology and Medicine in 2011. Further information on main operating principles of innate immunity in view of modern representations could be found in article “Nobel Prize or Ode to Innate Immunity”.
HOW LICOPID EFFECTS HUMAN BODY?
Licopid® increases functional activity (bactericide, cytotoxic) of “main” cells of innate immune system, professional “killers” of everything alien — phagocytes. Licopid strengthens their presentation by antigens, proliferation of Т- and В-lymphocytes, increases synthesis of specific antibodies, and promotes normalization of Th1/Th2-lymphocytes towards Th1 predominance. Licopid® (GMDP) stimulates leucopoiesis and recovery of granulocyte count by activation of production of colony-stimulating factors (CSF).
There are also other useful properties of GMDP evolved from experimental studies — antitumor and antimethastatic effects, adjuvant properties (higher production of antibodies at immunization, which is especially important at introduction of killed or “weakened” antigens).
WHY LICOPID IS CALLED THE NATURAL IMMUNOREGULATOR?
GMDP is not alien molecules; our body meets them daily fighting off the attacks of “pathogenic” microbes by processing of “worn-out” useful bacteria bearing GMDP in their cell walls, i.e. potentially different analogues could become “molecule” of the drug – activator of innate immunity, upon clinical proof of its safety.
WHAT ARE LICOPID EFFECTS?
Muramylpeptides are natural activators of innate immune system through innate immunity receptor NOD-2.