Tirzepatide

A dual receptor agonist engineered to simultaneously activate GLP-1 and GIP receptors. The first approved drug targeting two incretin receptors together, producing synergistic metabolic effects.

GLP-1R drives appetite suppression, glucose-dependent insulin secretion and gastric emptying delay. GIPR drives enhanced insulin sensitivity, potential mitigation of GLP-1 GI side effects, and adipose lipid metabolism promotion.

If semaglutide is one key turning one lock, tirzepatide turns two simultaneously. The second receptor, GIP, improves insulin sensitivity and may reduce side effects. In head-to-head trials it produced significantly greater weight loss than semaglutide, and it became the fastest-growing drug in US history by prescription volume within 12 months of launch.

• Percentage body weight reduction
• HbA1c change from baseline
• Insulin sensitivity indices
• Beta-cell function markers
• Liver fat fraction
• Waist circumference

• T2D SURPASS 1-6 trials
• Obesity SURMOUNT 1-4, up to 22.5 percent mean reduction
• Head-to-head vs semaglutide SURPASS-6 superior outcomes
• Cardiovascular SURPASS-CVOT ongoing
• Liver fat reduction in metabolic steatohepatitis
• Heart failure SUMMIT trial
• Insulin sensitivity and beta-cell function

Developed by Eli Lilly as the first dual incretin receptor agonist, approved as Mounjaro for type 2 diabetes and Zepbound for obesity.

Men and women 30-65 seeking superior weight loss, insulin resistance support, metabolic syndrome research, and those who want better results than semaglutide alone.

• Reconstitute with sterile or bacteriostatic water.
• Add diluent slowly down the vial wall and swirl gently.
• 5-day half-life supports weekly protocol modelling.
• Store reconstituted solution at 2-8C.
• Protect from light and avoid freeze-thaw cycles.

• Dual receptor profile differs mechanistically from single-agonist references.
• GI tolerability is dose-escalation dependent in human trials.
• Greater mean weight reduction than semaglutide in head-to-head data.
• Extensive published trial literature for protocol comparison.