Tirzepatide

Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Tirzepatide potently activates the GLP-1R signaling pathway to stimulate glucose-dependent insulin secretion through activity at the GIP receptor (GIPR) or the GLP-1R.
Tirzepatide is a synthetic peptide with glucose-lowering effects. It is an antidiabetic agent against type 2 diabetes (T2D), stimulating insulin and suppressing glucagon secretion in a glucose-dependent manner. Tirzepatide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake and reduce body weight in patients with type 2 diabetes.

Tirzepatide comprises a 39 amino acid linear synthetic peptide conjugated to a C20 fatty diacid moiety through a hydrophilic linker at the lysine residue at position 20. Due to this moiety, the compound is highly bound to albumin in the plasma which prolongs its half-life. It contains two non-coded amino acid residues (Aib, α-amino isobutyric acid) at positions 2 and 13).