Tirzepatide

FDA-approved dosing starts at 2.5 mg subcutaneously once weekly for 4 weeks, then increases to 5 mg weekly. May be titrated in 2.5 mg increments every 4 weeks to a maximum of 15 mg weekly. Available strengths: 2.5, 5, 7.5, 10, 12.5, and 15 mg. Injected subcutaneously in the abdomen, thigh, or upper arm with rotation of sites. Minimum 72 hours between doses if changing injection day.

Acts as a dual agonist at both GIP and GLP-1 receptors, combining the metabolic benefits of both incretin pathways. Demonstrates high affinity for GIP receptors and moderate affinity for GLP-1 receptors.

Stimulates first- and second-phase insulin secretion in a glucose-dependent manner, reducing risk of hypoglycemia while effectively lowering blood glucose.

Reduces glucagon levels in a glucose-dependent manner, decreasing hepatic glucose output and fasting/postprandial glucose levels.

Promotes satiety through central appetite regulation and delays gastric emptying, contributing to reduced caloric intake and weight loss.

Significantly lowers HbA1c levels with maximum reductions of ~2.24% in clinical trials (SURPASS program). FDA-approved for T2DM as Mounjaro.

Promotes substantial weight loss of up to 11.2 kg (and higher at maximum doses in obesity trials ~20-25% body weight). FDA-approved for obesity as Zepbound.

Reduces LDL cholesterol, triglycerides, and blood pressure, improving overall cardiovascular risk profile.

FDA-approved for treating obstructive sleep apnea in adults with obesity, likely through weight reduction mechanisms.

Emerging evidence shows tirzepatide alleviates metabolic dysfunction-associated fatty liver disease through effects on lipid metabolism and inflammation.

Obesity increases the risk of heart failure with preserved ejection fraction. Tirzepatide, a long-ac...

The New England journal of medicine · Milton Packer, Michael R Zile, Christopher M Kramer, Seth J ...

Obesity is a chronic disease and causal precursor to myriad other conditions, including type 2 diabe...

The New England journal of medicine · Ania M Jastreboff, Carel W le Roux, Adam Stefanski, Louis J ...

Tirzepatide, a dual incretin agonist of the glucagon-like peptide-1 and glucose-dependent insulinotr...

The New England journal of medicine · Stephen J Nicholls, Imre Pavo, Deepak L Bhatt, John B Buse, ...

Heart failure with preserved ejection fraction (HFpEF) is a major cause of hospitalization, often oc...

JAMA · Nils Krüger, Sebastian Schneeweiss, Kenshiro Fuse, Sofiya Ma...

Obstructive sleep apnea is characterized by disordered breathing during sleep and is associated with...

The New England journal of medicine · Atul Malhotra, Ronald R Grunstein, Ingo Fietze, Terri E Weav...