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Drug intelligence / Profile preview
GCGR-A
- Development stage
- Preclinical
- Lead developer
- Mitsubishi Tanabe
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GCGR-A is a novel, orally active small molecule glucagon receptor (GCGR) antagonist developed by Mitsubishi Tanabe Pharma. It acts by inhibiting glucagon binding to the glucagon receptor, thereby suppressing glucagon-induced cyclic AMP (cAMP) production and lowering blood glucose levels. In preclinical studies, GCGR-A demonstrated significant glucose-lowering effects in hyperinsulinemic and relatively insulin-deficient diabetic mouse models (such as ob/ob and db/db mice) without altering plasma insulin levels, suggesting its efficacy is independent of pancreatic beta-cell function.
02
Targets
GCGR (Glucagon receptor)
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