GliaMed began focusing on small molecule compounds called "immunophilin ligands" after it was shown that the immunosuppressive drug FK506 unexpectedly promoted and enhanced nerve regeneration in animal models of nerve injury. The company created small molecule compounds that retained the neuroregenerative properties of FK506 while eliminating its immunosuppressive activity. The discovery made by GliaMed’s founder was that these small molecules induced somatic cells to adopt a stem cell phenotype in vitro and that these induced stem cells could be made to differentiate into cells of different lineages, including muscle cells, neurons and glial cells. This class of small molecules has been termed “Regenerative Immunophilin Ligands” or RILs. Further research in animal models showed that administration of RILs in vivo by topical, oral or parenteral routes resulted in the generation of stem cell-like de-differentiated cells at the sites of trauma, and drove rapid and enhanced regeneration of a variety of tissues, including complex skin tissues, myocytes, bone and brain.

To date, GliaMed has shown compelling evidence in animal models that administration of GM1485 promotes:

  • Rapid regeneration of all components of skin following surgical wounding, resulting in complete wound healing with minimal scarring
  • Regeneration of cardiac tissue following induced myocardial infarction
  • Regeneration of CNS tissue after occlusive stroke with reperfusion injury

GliaMed has also shown that RILs induce the de-differentiation of adult human fibroblasts in vitro, and that when these cells are placed under appropriate culture conditions, they can be induced to differentiate into cells that express muscle-specific, neuron-specific or glial-specific markers. The mechanism of action involves induction of transcription factors such as Oct-4 and Sox-2, which are characteristic of stem cells.