TIRZEPATIDE
Tirzepatide is a synthetic peptide that acts as a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Its ability to interact with two incretin signaling pathways has made it an important compound in research examining glucose regulation, energy balance, appetite signaling, and metabolic function.
GIP and GLP-1 are naturally occurring incretin hormones involved in the body's response to nutrient intake. Both participate in glucose-dependent insulin signaling, while GLP-1 signaling is also associated with mechanisms involving food intake and gastric emptying. Tirzepatide was engineered to activate both receptor systems within a single molecule.
Laboratory and clinical research has investigated tirzepatide's effects on glucose metabolism, insulin response, body weight, appetite-related pathways, and broader metabolic regulation. Research into its molecular pharmacology has also shown that its activity is not identical at the two receptors, with relatively greater engagement of the GIP receptor and distinctive signaling characteristics at the GLP-1 receptor.
The SURPASS clinical research program extensively evaluated tirzepatide in people with type 2 diabetes. In the randomized Phase 3 SURPASS-1 trial, researchers observed changes in measures including HbA1c, fasting glucose, and body weight across the studied tirzepatide groups compared with placebo.
Tirzepatide itself is an active ingredient in approved prescription medicines for specific medical indications. However, the research product offered here is not an approved medication and should not be represented or used as a substitute for an approved pharmaceutical product.
For laboratory research purposes only. Not for human consumption.
Willard et al., 2020, JCI Insight: Great mechanistic reference for the description. It examines tirzepatide as a dual GIP/GLP-1 receptor agonist and its distinctive signaling at the two receptors.
Rosenstock et al., 2021, The Lancet, SURPASS-1: Phase 3 randomized clinical trial examining tirzepatide in people with type 2 diabetes, including glucose control, body weight, safety and tolerability.
Jastreboff et al., 2022, New England Journal of Medicine, SURMOUNT-1: A major Phase 3 trial involving 2,539 adults with overweight or obesity without diabetes, investigating tirzepatide and body-weight outcomes over 72 weeks.
Review of the SURPASS clinical program: Useful background covering tirzepatide's development, incretin biology and the broader clinical research program.
