Tirzepatide (LY3298176)

Tirzepatide hydrochloride (LY3298176 hydrochloride) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes [1] .

In HEK293 cells, Tirzepatide induces internalization of the GIPR and has a propensity toward partial agonism, and this ultimately reflects in signaling bias toward the cAMP pathway versus β-arrestin recruitment. [1] LY3298176 shows glucose-dependent insulin secretion and improves glucose tolerance by acting on both GIP and GLP-1 receptors in mice.