tirzepatide — Dual GIP/GLP-1 receptor agonist

Dual incretin agonism — activates both GIP and GLP-1 receptors, producing greater insulin sensitivity, enhanced glucose-dependent insulin secretion, reduced glucagon, slowed gastric emptying, and central appetite suppression exceeding single-agonist effects.

Overview

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Compound Class

Dual GIP/GLP-1 receptor agonist

Mechanism of Action

Dual incretin agonism — activates both GIP and GLP-1 receptors, producing greater insulin sensitivity, enhanced glucose-dependent insulin secretion, reduced glucagon, slowed gastric emptying, and central appetite suppression exceeding single-agonist effects.

Regulatory Status

FDA approved (Mounjaro for T2DM, Zepbound for weight management)

Evidence Level

High — SURMOUNT and SURPASS Phase 3 trials