Weight Loss Blockbuster Development: A Role for Unimolecular Polypharmacology

Sep 11, 2024Annual review of pharmacology and toxicology

Developing Powerful Weight Loss Drugs That Target Multiple Body Systems in One Molecule

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Abstract

More than 2.5 billion adults worldwide are affected by obesity and type 2 diabetes mellitus (T2DM).

  • Unimolecular polypharmacology designs single molecules to target multiple receptors or pathways.
  • Tirzepatide and retatrutide have shown superior efficacy in managing obesity and T2DM compared to traditional single agonists.
  • Tirzepatide has been noted for its effectiveness in weight loss and glycemic control, along with additional cardiovascular and renal benefits.
  • Challenges with these therapies include gastrointestinal side effects, patient compliance issues, and weight rebound after treatment cessation.
  • The development of these agents highlights the potential of unimolecular polypharmacology in treating metabolic diseases.

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