TMG-123 / Teijin - LARVOL DELTA

Quantitative prediction of human metabolites formed from the oxidation of the alcohol group of the glucokinase activator, TMG-123, using chimeric mice with humanized livers. (PubMed, J Pharm Sci) - "The main enzyme that metabolizes TMG-123 to GDI-1202 was found to be alcohol dehydrogenase (ADH)/aldehyde dehydrogenase (ALDH). Therefore, chimeric mice are effective animal models for predicting the PK of metabolites formed via the action of non-cytochrome P450 enzymes in humans."

Journal • Preclinical

Managing Post-Transplant Diabetes Mellitus after Kidney Transplantation: Challenges and Advances in Treatment. (PubMed, Pharmaceuticals (Basel)) - "New opportunities are offered by hypoglycemic drugs still in clinical trials, including glucokinase activators, such as dorzagliatin, ADV-1002401, LY2608204, TMG-123, imeglimine, amycretin and pramlintide. Although many therapeutic options are currently available, PTDM often creates uncertainty about the most appropriate treatment strategy. Therefore, more research is needed to individualize therapeutic plans and monitor these patients."

Journal • Post-transplantation • Review • Chronic Kidney Disease • Diabetes • Infectious Disease • Metabolic Disorders • Transplant Rejection • Transplantation

Disruptions in hepatic glucose metabolism are involved in the diminished efficacy after chronic treatment with glucokinase activator. (PubMed, PLoS One) - "For the mechanism analysis, we conducted a hepatic enzyme assay and liver perfusion study in Goto-Kakizaki rats after chronic treatment with MK-0941 and TMG-123, and revealed that, only in the MK-0941-treated group, the activity of glucose-6-phosphatase was increased, and hepatic glucose utilization was decreased compared to the non-treated group. These data indicate that disruptions in hepatic glucose metabolism are involved in the diminished efficacy of glucokinase activators."

Journal • Diabetes • Metabolic Disorders • Type 2 Diabetes Mellitus

A novel glucokinase activator TMG-123 causes long-lasting hypoglycemia and impairs spermatogenesis irreversibly in rats. (PubMed, J Toxicol Sci) - "However, there were no abnormalities in the copulation or fertility rate. These results suggest that long-lasting hypoglycemia in rats is harmful to spermatogenesis and the testicular damage does not recover."

Journal • Hypoglycemia