Hormonal
Tirzepatide, a dual GIP and GLP-1 receptor agonist, produces superior glycemic control and weight loss compared to selective GLP-1 receptor agonists by improving beta-cell function, enhancing insulin sensitivity independent of weight loss, and modulating central appetite regulation.
Tirzepatide is a once-weekly injection that works by mimicking two gut hormones (GIP and GLP-1). It is highly effective for lowering blood sugar and reducing body weight, often outperforming older GLP-1 drugs. It improves insulin sensitivity directly, not just through weight loss. Common side effects like nausea may be less severe due to the GIP component. It is prescribed for Type 2 Diabetes and Obesity.
Across the SURPASS clinical development program, tirzepatide demonstrated clinically meaningful and superior glycated hemoglobin (HbA1c) reductions compared not only with placebo but also with multiple active comparators, including a selective GLP-1RA... tirzepatide treatment is also associated with improvement in insulin sensitivity... Preclinical studies in obese mice suggest that tirzepatide may improve insulin sensitivity independently of weight reduction by enhancing glucose disposal in white adipose tissue, an effect mediated by GIPR activation in white adipose tissue.
Why this rating
Based on multiple phase 3 clinical trials (SURPASS, SURMOUNT) and mechanistic studies.
Source
Insights into the Mechanism of Action of Tirzepatide: A Narrative Review
Rodolfo J. Galindo et al. · Diabetes Therapy · 2025
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