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Retatrutide Guide

Reference asset · April 2026

The GLP-1 receptor map: which drugs hit which receptors

Every approved and late-stage investigational drug in the GLP-1 class, mapped against its molecular targets. The canonical reference for journalists, clinicians, and patients trying to make sense of a fast-moving drug class.

Editorially reviewed April 2026Updated April 28, 2026Independent medical reviewer onboarding

Receptor map · GLP-1 drug class

Which drugs activate which gut-hormone receptors

ApprovedPhase 3Phase 2
GLP-1-class drugs and the gut-hormone receptors each one activates: GLP-1, GIP, glucagon, and amylin.
DrugGLP-1GIPGlucagonAmylinStatus
LiraglutideSaxenda · VictozaNovo Nordisk
Approved
SemaglutideOzempic · Wegovy · RybelsusNovo Nordisk
Approved
DulaglutideTrulicityEli Lilly
Approved
ExenatideByetta · BydureonAstraZeneca
Approved
TirzepatideMounjaro · ZepboundEli Lilly
Approved
Orforglipron (oral)Eli Lilly
Phase 3
SurvodutideBoehringer / Zealand
Phase 3
MazdutideInnovent / Lilly
Phase 3
CagriSema (cagrilintide + semaglutide)Novo Nordisk
Phase 3
RetatrutideEli Lilly
Phase 3
Receptor activity is the molecular target each drug binds and activates. "Daily" or "oral" descriptors are included where the route differs from the once-weekly subcutaneous norm. Combination therapies (e.g., CagriSema) are shown with the union of their components' receptors.

How to read this map

Each column is a hormone receptor. Each row is a drug. A filled circle means the drug is a meaningful agonist (activator) at that receptor. We do not show partial antagonists, allosteric modulators, or receptor binding that is not pharmacologically active at clinical doses.

Why it matters

The history of obesity drugs over the last fifteen years can be told as a story of receptors stacked in a single molecule:

  • 1 receptor (GLP-1 only): exenatide (2005), liraglutide (2010), semaglutide (2017). Approximate weight loss: 5–15%.
  • 2 receptors (GLP-1 + GIP): tirzepatide (2022). Approximate weight loss: ~21%.
  • 2 receptors (GLP-1 + glucagon): survodutide, mazdutide. ~14–19%.
  • 2 mechanisms via combination (GLP-1 + amylin): cagrilintide + semaglutide. ~22%.
  • 3 receptors (GLP-1 + GIP + glucagon): retatrutide. ~24% in Phase 2.

The pattern isn't guaranteed — adding receptors does not always add efficacy linearly, and side-effect burden tends to rise alongside. But it is the central design hypothesis driving the next wave of obesity drugs.

What the map doesn't show

  • Receptor selectivity ratios. Two drugs that both hit GLP-1 and glucagon may have very different potency balances. Survodutide and mazdutide are not identical even though their map row looks the same.
  • Pharmacokinetics. Daily-injected liraglutide and once-weekly semaglutide both target only GLP-1, but their dosing cadence and patient experience differ substantially.
  • Earlier-stage candidates. Phase 1 and preclinical molecules are not on this map. New rows appear here when a drug enters Phase 2.

Update history

  • April 2026 — Added orforglipron Phase 3 status. Refreshed CagriSema designation.
  • February 2026 — Added mazdutide GLORY-1 Phase 3.
  • October 2025 — Initial publication.

Sources

Primary sources cited on this page

  1. Coskun T, et al.. LY3437943 (retatrutide), a novel triple glucagon, GIP, and GLP-1 receptor agonist. Cell Metabolism. 2022. Source ↗
  2. U.S. Food and Drug Administration. Orange Book: Approved Drug Products. FDA. 2026. Source ↗
  3. ClinicalTrials.gov. GLP-1, GIP, glucagon, and amylin receptor agonist program registries. NLM. 2026. Source ↗