CAS number:2023788-19-2
Molecular Formula:
C225H348N48O68
Molecular Weight:
4813.45g/mol
Brief Introduction:
Tirzepatide is a novel dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist approved for the treatment of type 2 diabetes mellitus (T2DM) and chronic weight management. Clinical trials from the SURPASS and SURMOUNT series have demonstrated its superior efficacy in glycemic control and weight reduction compared to existing GLP-1 receptor agonists (Khurana et al., 2024). It has shown significant weight loss outcomes, with patients achieving up to 20.9% reduction in body weight at higher doses (Jastreboff et al., 2022, cited in Khurana et al., 2024). Additionally, tirzepatide has been effective in managing hypothalamic obesity, a condition typically refractory to standard treatments, as evidenced by a case report where a patient lost 9 kg over 4 months (Brijmohan & Mullally, 2025). Despite its benefits, tirzepatide is associated with gastrointestinal adverse effects such as nausea, vomiting, and pancreatitis, which are common but generally manageable (Khurana et al., 2024). Its safety profile continues to be monitored in real-world settings to ensure optimal therapeutic outcomes.
Properities:
Type | Dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist [4, 5] |
Administration | Subcutaneous injection once per week [4] |
Approved for | Type 2 diabetes (US, May 2022) [4]; Obesity or overweight (US, November 2023) [4] |
Doses (Clinical Trials) | 5 mg, 10 mg, 15 mg [4] |
Common Doses (Real-world) | 2.5 mg (initiation), 5 mg, 7.5 mg (by sixth prescription fill) [3] |
Effects on Weight | Significant weight reduction: 5% to 20.9% across different trials in a dose-dependent manner over 72 weeks [4]; Mean weight reduction of 12.9% at 6-months post-index in real-world use [5]; 22.5% mean bodyweight reduction at week 72 (15mg dose) in SURMOUNT-1 [4]; 21.1% mean bodyweight reduction over 72 weeks (10 or 15 mg) in SURMOUNT-3 [4]; 20.9% mean bodyweight reduction during 36-week lead-in, with an additional 6.7% over 52 weeks in SURMOUNT-4 [4]. |
Effects on Body Composition | Lost body weight may be primarily due to fat mass reduction [4]; Associated with favorable changes in muscle fat infiltration and reductions in muscle volume [1]. |
Effects on Appetite | Significantly decreased food intake, reduced overall appetite scores, and increased fasting visual analog scale scores for satiety and fullness [4]. |
Effects on Glycemic Control | Favorable effects, with notable reductions in HbA1c levels ranging from 20.4 mmol/mol (5 mg dose) to 28.2 mmol/mol (15 mg dose) following 40-52 weeks of treatment [4]. |
Effects on Lipid Profile | Beneficial impact, including reductions in total cholesterol, low-density lipoprotein cholesterol, and triglyceride levels, while increasing high-density lipoprotein cholesterol concentrations [4]. |
Adverse Effects | Associated with gastrointestinal adverse effects, requiring dose escalation strategies for tolerability [4]; Mild to moderate adverse events are commonly reported at higher doses [4]; Discontinuation rates due to adverse events range from 4% to 10% across different dosages [4]. |
Persistence (Real-world) | Ranged from 60.6% to 75.7% across databases over 6 months [3]. |
Marketed under the brand name | Mounjaro [5] |
References:
[1] Real-world use and effectiveness of tirzepatide among people without evidence of type 2 diabetes in the United States. Diabetes & MetabolismMay 2025.
[2] Consistent improvements in liver histology across subgroups in a post hoc analysis of the SYNERGY-NASH trial with tirzepatide. JHEP ReportsAvailable online 6 June 2025.
[3] Tirzepatide and muscle composition changes in people with type 2 diabetes (SURPASS-3 MRI): a post-hoc analysis of a randomised, open-label, parallel-group, phase 3 trial. The Lancet Diabetes & EndocrinologyJune 2025.
[4] The promise of tirzepatide: A narrative review of metabolic benefits. Primary Care DiabetesJune 2025.
[5] Characteristics and Treatment Patterns of People Without Type 2 Diabetes Diagnoses Who Use Tirzepatide in the United States. Clinical TherapeuticsAvailable online 6 June 2025.
Tirzepatide is a synthetic peptide composed of 39 amino acids.
As a peptide, Tirzepatide contains multiple amide (peptide) bonds.
Tirzepatide is a dual GLP-1 receptor and GIP receptor agonist.
Tirzepatide is used clinically to lower blood glucose in type 2 diabetes.
Chemtoo
Chemical Procurement Assistant