Tirzepatide (CAS 2023788-19-2) is a unimolecular dual agonist of the GIP-R (Glucose-dependent Insulinotropic Peptide) and GLP-1R receptors, composed of 39 amino acids. Developed by Eli Lilly (LY3298176), it integrates into a single sequence the pharmacophores of both natural incretins, with Aib2 and Aib13 substitutions for DPP-4 resistance and C20 acylation (eicosanedioic acid) on Lys20 via γ-Glu-2×OEG linker, providing a plasma half-life of ~117 hours (≈ 5 days) and weekly administration.
Dual mechanism of action. GIP-R (EC50 ~0.07 nM) and GLP-1R agonism (EC50 ~5 nM, biased towards Gαs coupling) produces therapeutic synergy: GIP-R improves β-pancreatic function and adipocyte insulin sensitivity, while GLP-1R exerts classical effects (glucose-dependent insulinotropic, gastric emptying slowdown, central appetite reduction). Tirzepatide is described as biased towards GIP-R with GLP-1R activity ~5x weaker than native GLP-1, a profile seemingly contributing to its better gastrointestinal tolerability.
Clinical data. Approved by the FDA in May 2022 (Mounjaro® for type 2 diabetes) and November 2023 (Zepbound® for obesity), tirzepatide demonstrated HbA1c reduction of 2.07-2.58% at 15 mg/week in SURPASS trials (diabetes), and weight loss of 20.9% at 72 weeks in SURMOUNT-1 — superior to all previous peptide therapies. Digestive tolerability (nausea, vomiting, diarrhoea) remains dose-limiting however.
Research use. Tirzepatide is studied preclinically for NASH/NAFLD, heart failure with preserved ejection fraction (HFpEF), obstructive sleep apnoea (OSA) and neuroprotection. Several teams explore its effect on cognitive function, systemic inflammatory markers (CRP, IL-6, TNF-α) and cardio-renal biomarkers. Lab Peptides France distributes RUO tirzepatide in 10mg, 15mg, 20mg, 30mg and 60mg, with an HPLC ≥ 98% specification.
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Structure, mécanisme amyline, récepteur CTR + RAMP1/2/3, pharmacocinétique, programme REDEFINE (CagriSema), comparaison versus pramlintide Symlin, synergie GLP-1, protocoles de reconstitution RUO, stabilité et perspectives. Le pilier scientifique de référence sur le cagrilintide.
Structure, mécanisme triple agoniste, pharmacocinétique, programme TRIUMPH (1-4, Obesity, HFpEF, MASH), comparaison versus semaglutide et tirzepatide, protocoles de reconstitution RUO, stabilité et perspectives réglementaires. Le pilier scientifique de référence sur le retatrutide.