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Retatrutide (LY3437943) is a 39-amino-acid synthetic peptide built on a GIP backbone and conjugated to a C20 fatty-diacid side chain, which extends its plasma half-life to roughly six days and supports once-weekly subcutaneous administration.

It is the first single molecule to act as a balanced agonist at three incretin and glucose-regulatory receptors simultaneously: the glucose-dependent insulinotropic polypeptide receptor (GIPR), the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR). Reported in-vitro binding gives EC50 values of approximately 0.064 nM at GIPR, 0.78 nM at GLP-1R and 5.79 nM at GCGR. The added glucagon-receptor arm is the mechanistic point of difference from dual GIP/GLP-1 agents, and is associated in the published literature with increased energy expenditure alongside the appetite and gastric-emptying effects contributed by GLP-1 signalling.

Retatrutide is an investigational compound in late-stage clinical development. It has not been granted marketing authorisation by the FDA, EMA or CDSCO. Supplied in a 3 mL pre-filled pen at 10 mg/mL (30 mg total peptide).