Tirzepatide is a synthetically modified analog of gastric inhibitory polypeptide (GIP) with affinity at the glucagon-like peptide-1 (GLP-1) receptor. It was recently approved in the US to help type 2 diabetes patients better manage blood sugar. Tirzepatide is under active study as a weight loss agent and for its cardioprotective and anti-inflammatory properties
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Tirzepatide (LY3298176) is a synthetic peptide agonist of both the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. With a length of 39 amino acids, tirzepatide is primarily based on human GIP and modified with a C20 fatty di-acid moiety to extend its duration and thus allow for once-weekly subcutaneous administration [1, 2].
GIP is an incretin that is secreted from K cells in the upper small intestine in response to food, and is responsible for the majority of the insulinotropic incretin effect in man. GLP-1 is also an incretin, but which also inhibits glucagon secretion in the hyperglycaemic and normoglycaemic states. The hormone slows gastric emptying, promotes satiety, and reduces food intake, and GLP-1 analogs like semaglutide have had their own success as type 2 diabetes treatments [1, 2, 3, 4].
Research indicates that tirzepatide’s activation of both the GLP-1 and GIP receptors produces a synergistic effect to exert greater insulin and glucagonostatic responses, compared to administering GIP or GLP-1 alone. This makes the peptide a powerful tool in the treatment of both type 2 diabetes and obesity [1, 3].
Following completion of clinical trials in type 2 diabetes patients, tirzepatide became roundly acknowledged as a potent glucose lowering and weight loss agent with a comparable safety profile to other GLP-1 receptor agonists [5, 6, 7, 8, 9].
In May 2022, the US Food and Drug Administration approved tirzepatide as an adjunct treatment of type 2 diabetes, available by prescription under brand name Mounjaro [10].
Licensed researchers may also buy tirzepatide online as a reference material for laboratory experimentation only.
Tirzepatide has already been demonstrated as an effective treatment of type 2 diabetes, and is additionally being investigated as an obesity treatment and for its cardioprotective effect.
While a number of clinical trials involving tirzepatide are pending through at least 2024, here is a summary of the published results to date.
Through its activation of GIP receptors in fat cells, tirzepatide works to decrease adipose inflammation while increasing adiponectin, thus reducing fat cell differentiation and increasing energy expenditure, leading to weight loss [11].
In late 2022, Eli Lilly commenced SURMOUNT, a development program comprising four global phase 3 trials to assess the efficacy and safety of tirzepatide as an adjunct treatment of chronic weight management in adults with a BMI of 27 or greater [12].
Numbering over 2,500 participants, the first trial confirmed the efficacy of tirzepatide in inducing weight loss in the obese and overweight patients, with average weight reductions of tirzepatide 16% on 5mg/weekly, 21.4% on tirzepatide 10mg/weekly, and 22.5% on tirzepatide 15 mg/weekly, administered for a duration of 72 weeks. Results for the remaining trials are expected to be published in 2023 [12, 13].
As mentioned, animal research has shown that tirzepatide regulates hypothalamic feeding centers via GIP signaling, resulting in improved glucose handling and reduced food intake [11].
Tirzepatide has demonstrated superiority to diabetes treatments like dulaglutide and semaglutide in terms of glycemic control and obesity reduction. In one study, researchers found that tirzepatide was more effective than semaglutide at reducing hemoglobin A1c and inducing weight loss in type 2 diabetes patients [6, 14].
Based on its superior effectiveness compared to these other diabetes therapies in clinical studies, tirzepatide was approved by the US Food and Drug Administration as an adjunct treatment to improve blood sugar control in adults with type 2 diabetes [10].
Through its selective targeting of GLP-1 receptors, tirzepatide plays a role in abating inflammation, a condition that contributes to the initiation and progression of atherosclerosis [4]. Tirzepatide also increases adiponectin, and researchers have found a correlation between high levels of adiponectin and a reduced risk of coronary heart disease [15].
In a 26-week study on patients with type 2 diabetes, researchers found that once-weekly tirzepatide injections improved lipoprotein biomarkers associated with insulin resistance and cardiovascular risk while lowering triglycerides, suggesting a net lowering of the patients’ risk of of heart disease [16].
A pending cardiovascular outcomes study is expected to provide a clearer picture on the cardiovascular benefit of tirzepatide, compared to treatment with the GLP-1 receptor agonist dulaglutide [17]. Learn more about the benefits of Tirzepatide here.
Clinical trial data indicates that tirzepatide is generally well tolerated and is not associated with serious adverse effects in obese patients with or without type 2 diabetes [5, 6, 7, 8, 9, 13].
There are minor side effects linked with tirzepatide administration, and these generally subside with discontinuation of treatment or an adjustment of the total weekly tirzepatide dose.
Tirzepatide may induce the following side effects, most of which are GI tract related [5, 6, 7, 8, 9, 13]:
Due to its gastric emptying effect and lack of data in patients with severe gastrointestinal disease, researchers are advised against administering tirzepatide to subjects with serious gastroparesis [18].
Based on extensive clinical study (the SURPASS program), the US Food and Drug Administration has deemed tirzepatide safe for use in adults with type 2 diabetes [5, 6, 7, 8, 9, 10].
For example, in the phase 3 SURPASS-1 trial, the investigators deemed that tirzepatide had a safety profile consistent with that of other GLP-1 receptor agonists, while in the phase 3 SURPASS-4 trial, the investigators ruled out excess cardiovascular risk as a safety concern in administering tirzepatide to type 2 diabetes patients [5, 6].
While safety studies for other indications are still pending, studies into using tirzepatide as a treatment of obesity in adults (the SURMOUNT program), have already yielded positive outcomes [12, 13].
As a research chemical, tirzepatide is intended to be handled strictly by professional researchers and their authorized assistants, bearing in mind that the peptide has only been approved for use as a type 2 diabetes treatment to date.
To see information on the safe and effective administration of tirzepatide, researchers may refer to the Mounjaro (tirzepatide) package insert published by Eli Lilly. Here are some noteworthy points regarding the safe administration of tirzepatide [18]:
There are no set guidelines for dosing tirzepatide in a research setting, as the peptide may be studied for a range of applications.
On the other hand, reference may be made to the dosing schedules followed in both the Mounjaro (tirzepatide) package insert and clinical trials involving the peptide [5, 6, 7, 8, 9, 13, 18].
Based on the aforecited sources, researchers may refer to the following tirzepatide dosing protocol for weight loss in obese subjects:
Qualified researchers and laboratory professionals may legally buy tirzepatide online for in vitro testing.
Researchers are advised to avoid purchasing tirzepatide from online peptide vendors who do not clearly state that their peptides are intended for research purposes only, or similar.
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Tirzepatide that is provided in lyophilized (freeze-dried) powder form must be reconstituted with bacteriostatic water. To reconstitute tirzepatide, extract the correct amount of bacteriostatic water from its vial and insert into the tirzepatide vial, letting the water slowly enter before swirling the solution until dissolved.
Tirzepatide is intended to be delivered subcutaneously, into the fatty tissue beneath the research subject’s skin, typically in the abdomen.
Tirzepatide should be administered once weekly at a dose ranging from 2.5mg to 15mg, depending on the study phase, research objective, and test subject.
Tirzepatide is a novel, FDA-approved medication that acts on both the GIP and GLP-1 receptors to improve insulin sensitivity, induce weight loss, and favorably impact the lipid profiles of type 2 diabetes patients.
It is now targeted as an obesity treatment, with positive data from the SURMOUNT clinical trial program already published and further results pending.
The overall safety data and relative lack of adverse effects further support the use of this dual GIP/GLP-1 receptor agonist in a range of clinical applications.
Licensed researchers who wish to buy tirzepatide online for investigation should head over to our top-rated research peptides vendor today.
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