Preclinical Analyses of TGR-63 Demonstrate Blood-Brain Barrier Permeability and Safety Profile
IGC Pharma, Inc. today announced preclinical data demonstrating TGR-63’s potential as an effective treatment for Alzheimer’s disease. Analysis of the partition coefficient and mass spectrometry of brain tissue in Alzheimer’s murine models both indicate that TGR-63 has the potential to cross the blood-brain barrier in humans. These findings build on earlier results demonstrating TGR-63’s efficacy in reducing amyloid plaque in Alzheimer's mouse models.
Ensuring effective drug delivery to the brain is a major challenge in treating Alzheimer’s disease. The preclinical studies on TGR-63 included an analysis of the partition coefficient in an aoctanol-water assay the partition coefficient calculated as Log Poctanol/water, indicated that LogP=0.1, which suggests that TGR-63 possesses favorable properties for penetrating the blood-brain barrier, a critical step in accessing brain tissue. Additionally, mass spectrometry analysis of brain tissue samples from TGR-63-treated mice confirmed the presence of the compound in the brain, validating its ability to cross the blood-brain barrier in mice and potentially in humans.
Furthermore, the safety profile of TGR-63 was evaluated through extended studies in mice. Mice received daily doses of TGR-63 for eight months without exhibiting any adverse effects. Comprehensive examinations of major organs, including the liver, heart, spleen, and kidneys, revealed no signs of toxicity, inflammation, or cell death, indicating biocompatibility and safety. IGC continues to progress TGR-63 towards clinical trials, representing a significant advancement in Alzheimer's treatment research.
Ram Mukunda, CEO of IGC, commented, “These preliminary findings underscore TGR-63’s potential as a safe and effective treatment for Alzheimer’s disease. As we forge ahead with this amyloid-targeting drug, we are encouraged by its potential to offer an improved safety profile compared to currently approved treatments. This strategic approach should allow us to offer a diverse portfolio of Alzheimer’s-focused drugs that prioritize patient safety and efficacy. In addition to the focus on Alzheimer’s, we are training sophisticated AI models to analyze potential efficacy of targeting other receptors such as GLP-1, CB1, among others. We have four platforms, IGC-AD1, TGR, IGC-C, IGC-M and LMP. These platforms allow us to modify the core molecule and potentially target other receptors that could impact other diseases and conditions. We are very excited with the possibilities."
July 12, 2024
