Tirzepatide is a synthetic analog of gastric inhibitory polypeptide (GIP) with affinity at glucagon-like receptor-1 (GLP-1). It is a linear polypeptide made of 39 amino acids modified with a C20 fatty diacid moiety through a linker at lysine-20. This particular modification extends its durations and allows for weekly subcutaneous dosing. It is approved for type 2 diabetes management and is under active study for its weight loss and cardioprotective effects

From Pubchem

Synonyms: Mounjaro, LY3298176
Molecular Formula: C225H348N48O68
Molecular Weight: 4813 g/mol
CAS number: 2023788-19-2
PubChem CID: 163285897

Eli Lilly and the company first developed tirzepatide and applied for patent in 2016. After the successful completion of clinical trials in type 2 diabetes patients, the company applied for FDA approval in October 2021 with the priority review voucher. In May 2022, tirzepatide was approved for the adjunct treatment of type 2 diabetes under the brand name, Mounjaro. At Pinnacle Peptides, tirzepatide for sale is exclusively available for research

Tirzepatide has a greater affinity to GIP receptors than GLP-1 receptors. GIP is an incretin that is released from the upper small intestine in response to food. It is the main incretin responsible for the insulinotropic effects. GLP-1 is also an incretin that is involved in promoting insulin release, inhibiting glycogen secretion, delaying gastric emptying time and reducing appetite. Tirzepatide’s dual action at GLP-1 and GIP receptors produces a synergistic effect and causes greater hyperglycemic reduction than a selective GLP-1 agonist alone.

1. Cardioprotective Effects

Research shows that tirzepatide might offer cardioprotective effects. One study found that tirzepatide alleviated cardiac dysfunction induced by lipopolysaccharide and suppressed the inflammatory response in mice. Additionally, it reduced the risk of ventricular arrhythmia and cardiac apoptosis through inhibition of the TLR4/NF-kB/NLRP3 pathway [1].

A follow-up analysis of the SURPASS clinical program found that patients treated with TZP experienced a decrease in systolic blood pressure due to its impact on weight loss [2]. Furthermore, another study discovered that individuals who received TZP had greater reductions in triglyceride levels and LDL-C compared to those given insulin glargine [3]

2. Diabetes

The FDA approved Tirzepatide for type 2 diabetes following a series of successful phase 3 clinical trials conducted in the SURPASS program. These trials provided substantial evidence showcasing tirzepatide's superior effectiveness when compared to a placebo and other medications.

Results from the SURPASS 3 trials have demonstrated that Tirzepatide (TZP) outperforms Insulin Degludec in terms of efficacy. Notably, patients treated with TZP who achieved an HbA1c level of <5.7% over 52 weeks displayed more favorable outcomes in TIT, TTIT, and glycemic variability compared to those who did not reach this target [4].

Furthermore, another study indicates that when combined with insulin glargine, TZP leads to improved glycemic control in patients who were previously unresponsive to insulin glargine [5].

The SURPASS 6 trial has revealed that TZP is more effective in enhancing HbA1c levels and improving the health-related quality of life (HRQoL) in diabetic patients when compared to insulin lispro [6].

3. Weight Loss

The SURPASS 1-5 trials, which investigated the anti-diabetic effects of tirzepatide, have also demonstrated a significant impact of TZP on weight loss. A meta-analysis of these trials reveals that 43% of patients who received TZP lost more than 15 kilograms of body weight [7].

In the SURAMOUNT trial 1, researchers assessed the safety and effectiveness of tirzepatide in obese individuals. They enrolled 2539 participants in the study and randomly assigned them to receive subcutaneous TZP (at doses of 5mg, 10mg, or 15mg) or a placebo for 72 weeks. The findings indicated that the percentage of participants achieving more than a 5% reduction in weight was 85% for 5mg, 89% for 10mg, and 91% for 15mg. These stats clearly indicate TZP’s superior efficacy compared to the placebo [8].

Furthermore, SURAMOUNT trial 2 found that 79-83% of individuals treated with TZP experienced more than 5% weight loss, in contrast to the control group where only 32% achieved this level of weight reduction [9].

Tirzepatide is an FDA-approved drug for the adjunct treatment of type 2 diabetes. Further clinical trials under SURAMOUNT program are underway to establish the safety and efficacy of tirzepatide for weight loss. Pinnacle peptides offer the option to purchase tirzepatide for research purposes only, not for human consumption. We encourage you to buy tirzepatide from us only if you are an authorized researcher.

1. Kellerer, Liu, Q., et al., Tirzepatide attenuates lipopolysaccharide-induced left ventricular remodeling and dysfunction by inhibiting the TLR4/NF-kB/NLRP3 pathway. International Immunopharmacology, 2023. 120: p. 110311.
2. Lingvay, I., et al., Systolic blood pressure reduction with tirzepatide in patients with type 2 diabetes: insights from SURPASS clinical program. Cardiovascular Diabetology, 2023. 22(1): p. 66.
3. Kahn, S., et al., IDF2022-0918 Tirzepatide Reduces Serum Triglyceride Irrespective of Fibrate Use in People With T2D at High CV Risk (SURPASS-4). Diabetes Research and Clinical Practice, 2023.
4. BERGENSTAL, R.M., et al., 764-P: Time in Range and Time in Tight Range in Tirzepatide-Treated Patients Achieving Normoglycemia in the SURPASS-3 CGM Substudy. Diabetes, 2023. 72(Supplement_1).
5. Dahl, D., et al., Effect of Subcutaneous Tirzepatide vs Placebo Added to Titrated Insulin Glargine on Glycemic Control in Patients With Type 2 Diabetes: The SURPASS-5 Randomized Clinical Trial. Jama, 2022. 327(6): p. 534-545.
6. BOYE, K., et al., 753-P: Tirzepatide Improves HRQoL Compared with Insulin Lispro in Poorly Controlled Basal Insulin–Treated Adults with Long-Standing T2D (SURPASS-6). Diabetes, 2023. 72(Supplement_1).
7. Malecki, M., et al., IDF2022-0369 Predictors of Achieving Weight Loss ≥15% With Tirzepatide in People With Type 2 Diabetes From SURPASS 1-4. Diabetes Research and Clinical Practice, 2023.
8. Jastreboff, A.M., et al., Tirzepatide Once Weekly for the Treatment of Obesity. New England Journal of Medicine, 2022. 387(3): p. 205-216.
9. Garvey, W.T., et al., Tirzepatide Once Weekly for the Treatment of Obesity in People With Type 2 Diabetes (SURMOUNT-2): A Double-Blind, Randomised, Multicentre, Placebo-Controlled, Phase 3 Trial. The Lancet, 2023.