Drug intelligence / Profile preview

LY2409021 + metformin

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY2409021 + metformin is an investigational oral fixed-dose combination for type 2 diabetes that combines **LY2409021**, a selective small molecule **glucagon receptor antagonist** developed by Eli Lilly, with **metformin**, a widely used antihyperglycemic agent. LY2409021 blocks the hepatic glucagon receptor, suppressing glucagon-mediated glucose output and thereby lowering blood glucose[1][2]. When given with metformin, which primarily reduces hepatic gluconeogenesis and increases insulin sensitivity, the combination aims to synergistically improve glycemic control in type 2 diabetes. LY2409021 reduces HbA1c but has been associated with increased hepatic fat, liver enzymes, and small rises in blood pressure and cholesterol; all effects appear reversible after discontinuation[1][2]. Its development status as a fixed combination remains investigational, with no evidence of approval or broad market authorization.

02

Targets

GCGR (Glucagon receptor)ND1 (Mitochondrial electron transport chain complex I)

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