Tirz 5mg

Tirz

Currently, it is one of the most effective weight loss medications on the U.S. market, approved by the FDA.

Tirz is a recently approved medication for Type 2 Diabetes (T2D) that is now being investigated as a potential weight loss treatment. This synthetic analog of the gastrointestinal inhibitory peptide (GIP) is designed to enhance insulin secretion, making it effective for treating both Type 2 Diabetes and non-alcoholic fatty liver disease.

Mechanism of Action: Tirzepatide is a relatively large peptide consisting of 39 amino acids. It works by stimulating insulin release from the pancreas through binding to GIP and GLP-1 (glucagon-like peptide-1) receptors. This dual action is crucial for its therapeutic effects.

Clinical Benefits:

Insulin Regulation: Tirzepatide effectively stimulates insulin secretion, which is important for managing blood glucose levels.

Appetite Reduction: The medication reduces hunger, aiding in weight loss.

Insulin Sensitivity: It improves insulin sensitivity, helping with better glucose control.

Weight Loss: Clinical studies have shown that tirzepatide can lead to significant weight loss, averaging 11 kg (25 pounds). It is considered one of the most effective weight loss medications available.

Improved Glucose Tolerance: It enhances glucose tolerance and reduces fat tissue.

Cardiovascular Risk: The reduction in fat tissue and improvement in metabolic markers may lower cardiovascular risk.

Long-Term Effects: With prolonged use, tirzepatide has been shown to increase levels of adiponectin by 26%, further supporting its role in improving metabolic health.

Conclusion: Tirzepatide represents a promising advancement in the treatment of Type 2 Diabetes and obesity. Its ability to reduce appetite, improve insulin sensitivity, and contribute to significant weight loss makes it one of the most effective weight loss treatments available. Ongoing clinical trials continue to explore its full range of effects and safety profile.

What is Tirzepatide?

Tirzepatide, also known as LY3298176, is a novel medication that acts as a dual agonist for glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors. It is currently under investigation for its potential benefits in glycemic control and weight management.

Developed from the human GIP hormone, tirzepatide is a 39-amino acid peptide with an added C20 fatty di-acid moiety that extends its action, allowing for weekly dosing in humans.

After comprehensive clinical trials and comparisons with other treatments, tirzepatide was approved by the U.S. Food and Drug Administration (FDA) in May 2022 for the treatment of Type 2 Diabetes (T2D). It was the first medication to combine GLP-1 and GIP receptor agonism specifically for T2D.

Tirzepatide is now being tested in clinical trials to assess its safety and effectiveness as a weight loss treatment for adults with a body mass index (BMI) of 27 or higher. Initial results suggest it offers significant and lasting weight management benefits.

Currently, while it is approved as a prescription medication for T2D, tirzepatide is also available for research purposes to qualified professionals interested in studying this innovative GLP-1/GIP receptor agonist.

What Does Tirzepatide Do?

Tirzepatide is a powerful tool for managing both weight and blood sugar due to its dual action on GLP-1 and GIP receptors. Research indicates that its ability to activate both receptors produces a synergistic effect, leading to improved insulin response and reduced glucagon activity compared to treatments that target only one receptor.

GIP and GLP-1 are key incretin hormones released by the intestine in response to glucose or nutrient intake, which stimulate insulin secretion from pancreatic beta cells. Tirzepatide binds to GIP receptors with similar affinity as native GIP, but has a fivefold lower affinity for GLP-1 receptors compared to native GLP-1. It preferentially activates cAMP signaling over beta-arrestin recruitment.

This selective agonism and unique GLP-1 signaling are thought to contribute to tirzepatide’s effectiveness in enhancing insulin secretion. Clinical trials have demonstrated that tirzepatide is more effective and comparably safe as a glucose-lowering agent when compared to other established T2D treatments.

Additionally, tirzepatide significantly increases adiponectin levels, a protein involved in regulating lipid and glucose metabolism. Elevated adiponectin is associated with weight loss and improved nutrition, suggesting potential cardiovascular benefits.

Tirzepatide Benefits | Clinical Trials

Although tirzepatide is already approved for Type 2 Diabetes treatment, its potential for weight loss and cardiovascular protection is being further explored.

Clinical trials are ongoing through at least 2024. Here’s a summary of the findings available as of now:

Tirzepatide and Weight Loss: Tirzepatide’s weight loss effects are partially attributed to its activation of GIP receptors in fat cells, which reduces inflammation and increases adiponectin, leading to decreased fat cell differentiation and higher energy expenditure. Eli Lilly and Company, the patent holder, launched the SURMOUNT clinical development program in late 2022 to evaluate tirzepatide’s effectiveness for weight management in adults with a BMI of 27 or higher. The program includes four global Phase 3 trials. Initial results from a study with over 2,500 participants showed average weight reductions of 16% with 5 mg weekly, 21.4% with 10 mg weekly, and 22.5% with 15 mg weekly over 72 weeks. The remaining trials are expected to conclude in 2023.

Tirzepatide as a T2D Treatment: Tirzepatide’s dual GLP-1 and GIP action differentiates it as a treatment for Type 2 Diabetes. Its unique mechanism—mimicking native GIP while favoring cAMP generation at the GLP-1 receptor—underpins its effectiveness. Research shows tirzepatide outperforms other diabetes therapies, such as semaglutide and dulaglutide, in terms of glycemic control and weight reduction. The FDA has approved tirzepatide as an adjunct treatment for improving blood sugar control in T2D patients, alongside diet and exercise.

Tirzepatide and Cardiovascular Benefits: GLP-1 is known to influence risk factors like hypertension and obesity, and indirectly impact inflammation and endothelial dysfunction. Tirzepatide’s targeted action on the GLP-1 receptor may help slow the development of cardiovascular complications, especially in diabetics. A 26-week study found that tirzepatide improved lipoprotein biomarkers linked to insulin resistance and cardiovascular risk, while reducing triglycerides, which may lower heart disease risk. A forthcoming cardiovascular outcomes study will further evaluate tirzepatide’s cardioprotective effects in comparison to the GLP-1 receptor agonist dulaglutide.

Tirzepatide Side Effects

According to current data, tirzepatide is generally well-tolerated and is not associated with severe adverse effects in obese or overweight adults, whether or not they have Type 2 Diabetes (T2D). However, minor side effects, typically related to the gastrointestinal (GI) tract, may occur. These effects usually subside with discontinuation of the medication or after reducing the dosage.

Here is a list of common side effects observed with tirzepatide use:

Nausea

Vomiting

Diarrhea

Reduced appetite

Constipation

Indigestion

Dyspepsia

Abdominal pain

Hypersensitivity reactions

It is important to note that tirzepatide affects gastric emptying, so it should not be administered to individuals with severe gastrointestinal disorders.

Is Tirzepatide Safe?

Based on the SURPASS clinical trials, the U.S. Food and Drug Administration (FDA) has approved tirzepatide for treating Type 2 Diabetes, recognizing it as safe for use in adults with this condition.

In the Phase 3 SURPASS-1 trial, tirzepatide demonstrated a safety profile similar to other GLP-1 receptor agonists. The Phase 3 SURPASS-4 trial found no increased cardiovascular risk associated with tirzepatide for T2D patients.

Safety evaluations for tirzepatide’s other potential uses, such as for weight loss (part of the SURMOUNT program), also indicate a positive safety profile.

When used as a research chemical or reference material, tirzepatide should be handled only by qualified researchers and authorized personnel due to the limited safety data available.

Researchers can consult the Mounjaro (tirzepatide) package insert for detailed information on safe and effective administration. Key safety points include:

Tirzepatide is administered via subcutaneous injection into the fatty tissue, typically in the abdomen. Rotating injection sites is recommended.

It should not be given to individuals with a history of medullary thyroid carcinoma or Multiple Endocrine Neoplasia syndrome type 2 (MEN 2), as it has been associated with thyroid C-cell tumors in animal studies.

Patients using insulin or insulin secretagogues alongside tirzepatide should be monitored for hypoglycemia.

Tirzepatide may delay the absorption of certain oral medications, so patients on drugs with a narrow therapeutic index should be observed.

Tirzepatide Dosage Recommendations

For research purposes, tirzepatide dosing may vary based on the study's goals. Current recommendations are based on trials involving Type 2 Diabetes and obesity.

Here is a general dosing protocol for inducing weight loss in obese or overweight subjects:

Starting Dose (Weeks 1-4): 2.5 mg per week.

Dose Increase (Weeks 5-24): Increase the weekly dose to 5 mg. If needed, further increase the dose by 2.5 mg increments based on response.

Frequency: Once per week, administered subcutaneously.

Duration: 12-24 weeks.

Maximum Dose: The highest established weekly dose is 15 mg, according to the Mounjaro dosing guidelines and clinical trial data.

Product Use: THIS PRODUCT IS STRICTLY FOR SCIENTIFIC RESEARCH PURPOSES ONLY. It should only be used in laboratory settings. All product information on this website is provided solely for educational purposes. The law strictly prohibits introducing this product into the body of humans or animals. Only licensed professionals should handle this product. This product is not a drug, food, or cosmetic and should not be improperly classified or used as such.