Tirzepatide ILE12NVA (NVA-ILE) substituents - Biofargo

Description

Background Introduction

Tirzepatide, a groundbreaking dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors, has set a new standard in the treatment of type 2 diabetes (T2DM) and obesity. As one of the most effective GLP-1 receptor agonists (GLP-1RAs), tirzepatide has demonstrated superior efficacy in reducing HbA1c levels (-2.10%) and fasting plasma glucose concentrations (-3.12 mmol/L), offering unmatched glycemic control. It also provides significant benefits in weight management, with an average reduction of -8.47 kg, making it a powerful tool for addressing the ""twin epidemics"" of diabetes and obesity. Approved by the FDA under the brand name Mounjaro, tirzepatide uses innovative acylation technology to extend its half-life, allowing for once-weekly subcutaneous injections.

While it delivers substantial improvements in glycemic and metabolic outcomes, gastrointestinal side effects such as nausea, vomiting, and diarrhea, particularly at high doses, remain important considerations. Tirzepatide’s remarkable efficacy and safety profile have made it a frontrunner among incretin-based therapies, offering transformative benefits in the management of cardiometabolic disorders. This novel therapy highlights the evolving potential of GLP-1RAs and dual incretin receptor agonists in improving the lives of individuals with T2DM and related conditions.