Tirzepatide Pharmacokinetics
Tirzepatide half-life, absorption, routes of administration, and clearance.
Dual-Agonist Pharmacokinetics: The 5-Day GIP/GLP-1 Profile
Tirzepatide's pharmacokinetic engineering builds on GLP-1 agonist acylation principles but applies them to a GIP-backbone peptide, producing a dual-receptor agonist with a 5-day half-life. The result is once-weekly dosing with balanced GIP and GLP-1 receptor engagement throughout the dosing interval.
Physicochemical and PK profile
- Molecular Formula
- C225H348N48O68
- Molecular Weight
- 4813.45 g/mol
- CAS Number
- 2023788-19-2
- Half-Life
- Approximately 5 days (120 hours)
- Sequence
- Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys(γGlu-γGlu-C20 diacid)-Ile-Ala-Gln-Lys-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser
- Solubility
- Formulated as ready-to-use solution for injection
- Storage
- Store at 2-8°C. May be stored at room temperature for up to 21 days if needed.
References
- Tirzepatide Once Weekly for the Treatment of Obesity · Jastreboff AM, et al. · 2022
- Frías JP, et al. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes (SURPASS-2). N Engl J Med. 2021;385(6):503-515. · Frías JP, Davies MJ, Rosenstock J, Pérez Manghi FC, Fernández Landó L, Bergman BK, Liu B, Cui X, Brown K · 2021
- Comparison of tirzepatide and dulaglutide on major adverse cardiovascular events in participants with type 2 diabetes and atherosclerotic cardiovascular disease: SURPASS-CVOT design and baseline characteristics. · Nicholls SJ, Bhatt DL, Buse JB et al. · 2024
- Tirzepatide - StatPearls - NCBI Bookshelf
- Jastreboff AM, et al. Tirzepatide Once Weekly for the Treatment of Obesity (SURMOUNT-1). N Engl J Med. 2022;387(3):205-216. · Jastreboff AM, Aronne LJ, Ahmad NN, Wharton S, Connery L, Alves B, Kiyosue A, Zhang S, Liu B, Bunck MC, Stefanski A · 2022
- Cardiovascular Outcomes with Tirzepatide versus Dulaglutide in Type 2 Diabetes. · Nicholls SJ, Pavo I, Bhatt DL et al. · 2025
- Garvey WT, et al. Tirzepatide once weekly for the treatment of obesity in people with type 2 diabetes (SURMOUNT-2). Lancet. 2023;402(10402):613-626. · 2023
- Mounjaro FDA Label
- Rosenstock J, et al. Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1). Lancet. 2021;398(10295):143-155. · 2021
- Effects of tirzepatide versus insulin glargine on kidney outcomes in type 2 diabetes in the SURPASS-4 trial: post-hoc analysis of an open-label, randomised, phase 3 trial. · Heerspink HJL, Sattar N, Pavo I et al. · 2022
- FDA Approves First Medication for Obstructive Sleep Apnea
- Nauck MA, D'Alessio DA. Tirzepatide, a dual GIP/GLP-1 receptor co-agonist for the treatment of type 2 diabetes with unmatched effectiveness. Cardiovasc Diabetol. 2022;21(1):66. · Liu HX, Ma JZ, Ye YS, Zhao JJ, Wan SJ, Hu XY, Xu G · 2022