IRT-103 LODONAL exerts its effects on humans via at least two distinct receptor mechanisms. The first receptor mechanism is the blocking of the opiate receptor for a short period time. This results in a reactive increase in the production of opioid receptors on immune cells, an increase in circulating levels of endorphins and enkephalins. Increased levels of beta-endorphin and enkephalins have been shown to stimulate the immune system, promoting an increase in the number and functions of T lymphocytes and natural killer (NK) cells. The increase in the T-cell and NK cell numbers and functions appears to restore a more normal balance of the immune cells such that effects of disease are significantly reduced.
It has been demonstrated in phase II clinical trials for Crohn’s Disease, HIV/AIDS, Fibromyalgia, MS, Autism and Cancer that in the presence of LDN, the numbers of T-cells, both CD4+ helper T cells and CD8+ cytotoxic T cells, may increase by more than 300%.
In addition to the antagonist effect on mu-opioid and other opioid receptors, naltrexone simultaneously has an antagonist effect on non-opioid receptors (Toll-like receptor 4 or TLR4 or TRL-9 as well as the p receptors) that are found on macrophages such as microglia. In this process IRT-103 is able to shift Th1 to Th2 to reduce inflammation