Tirzepatide

Tirzepatide is a dual GLP-1 and GIP receptor agonist that improves glucose control, reduces appetite, and supports cardiovascular and lipid health in diabetes and obesity.

- Reduce appetite and improve glycemic and metabolic health

Mechanism of Action

How this peptide works in the body

Insulin Secretion and Glucagon Suppression:

Tirzepatide activates GLP-1 and GIP receptors on pancreatic β-cells, stimulating the cAMP/PKA pathway, which enhances glucose-dependent insulin secretion. Simultaneously, it binds to GIP receptors on α-cells, suppressing glucagon secretion and reducing hepatic gluconeogenesis and glycogenolysis, leading to improved blood sugar control.

Appetite Regulation:

Tirzepatide modulates hypothalamic appetite centers by stimulating POMC neurons and inhibiting AgRP/NPY neurons in the arcuate nucleus (ARC), reducing hunger signals. Additionally, it enhances adiponectin secretion in adipocytes via GIP receptor activation, reducing chronic adipose inflammation and promoting lipid oxidation.

Weight Loss:

Tirzepatide slows gastric emptying by delaying pyloric sphincter relaxation, reducing postprandial glucose spikes and extending satiety. By activating GLP-1 receptors in vagal afferents, it enhances signals to the nucleus of the solitary tract (NTS) in the brainstem, further suppressing appetite and reducing caloric intake.

Cardiometabolic Benefits:

Tirzepatide improves lipid metabolism by downregulating hepatic sterol regulatory element-binding proteins (SREBP-1c, SREBP-2), lowering triglyceride and LDL cholesterol synthesis, while increasing HDL cholesterol levels. It reduces systemic inflammation by suppressing NF-κB and IL-6/TNF-α cytokine production, decreasing cardiovascular disease risk.