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RETATRUTIDE

Potential Health Benefits of Retatruide

- Aids in Weight Reduction

- Improves Blood Glucose Levels

- Improves Blood Pressure

What is Retatrutide?

Retatrutide, a new medication developed by Eli Lilly, holds significant promise for treating obesity and diabetes. Also referred to as GGG Tri-agonist, GLP-1/GIP/glucagon tri-agonist, or LY3437943, this injectable treatment is similar to existing weight loss options like tirzepatide and semaglutide, but with enhanced effectiveness. When paired with a balanced diet, regular exercise, and lifestyle changes, retatrutide can improve weight loss results and address comorbidities associated with obesity, such as diabetes and hypertension.

Key Takeaways of Retatrutide

1. Retatrutide shows promise as one of the best weight loss medications currently available, outperforming popular options like Semaglutide (Ozempic, Wegovy, Rybelsus) and Tirzepatide (Mounjaro). Developed by Eli Lilly, retatrutide was designed to address obesity and diabetes. 

2. It targets specific biological pathways related to metabolism, appetite regulation, and fat storage, resulting in weight reduction. Clinical trials have demonstrated that retatrutide can lead to significant weight loss when incorporated into a comprehensive weight management program.

3. In addition to weight loss, retatrutide may provide further health benefits, including improved insulin sensitivity, better cardiovascular risk factors, and enhanced overall quality of life. 

4. Before starting retatrutide for obesity treatment, it's important to consult with a healthcare professional. Regular monitoring, adherence to prescribed dosages, and healthy lifestyle changes are crucial for achieving and maintaining the desired results.

Chemical Structure of Retatrutide

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How Retatrutide Works?

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Retatrutide Clinical Trials

Weight Reduction

Trial results indicate that retatrutide shows significant potential for treating obesity and weight-related conditions:

1. In a phase 2 trial published in the New England Journal of Medicine on June 26, 2023, 338 obese adults participated. The primary endpoint was the percentage change in body weight over 24 weeks, with secondary endpoints including weight change at 48 weeks and achieving weight loss of 5%, 10%, or 15%. After 48 weeks, participants receiving weekly retatrutide injections experienced notable weight reductions: -8.7% for the 1-mg group, -17.1% for the 4-mg group, -22.8% for the 8-mg group, and -24.2% for the 12-mg group, compared to -2.1% in the placebo group. Improvements were also noted in LDL cholesterol, triglycerides, fasting glucose, insulin levels, and blood pressure.

2. In adults aged 20-70 with type 2 diabetes, retatrutide doses of 3/6/9/12 mg led to an average weight loss of 17% over nine months, demonstrating an acceptable safety profile. Its combined action on glucagon, GIP, and GLP-1 receptors may explain its strong weight loss effects.

3. In animal studies, retatrutide reduced body weight and blood sugar levels in high-fat-fed mice and improved energy expenditure in obese mice. In healthy subjects, the highest doses resulted in significant weight loss maintained for up to 43 days. Overall, retatrutide proved effective in reducing appetite and body weight, outperforming other GIPR and GLP-1R agonists, while also showing favorable safety in patients with type 2 diabetes and obesity.

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Retatrutide Dosage

Retatrutide is a new obesity treatment currently under development by Eli Lilly. The starting dose is 0.5 mg, administered subcutaneously once a week. After four weeks, the dose may be increased to 1 mg, 2 mg, or 4 mg based on the patient’s response, with a maximum dose of 12 mg per week.

Starting with a low dose is crucial for minimizing the risk of side effects. If the initial dose is well tolerated, it can be gradually increased. However, if the patient experiences significant side effects, the dose should be reduced or the medication discontinued.

Improves Blood Sugar Levels

Retatrutide helps regulate blood sugar levels by influencing the hormones insulin and glucagon. Insulin lowers blood sugar, while glucagon raises it to maintain balance. As a GLP-1 agonist and GR agonist, retatrutide promotes insulin release from the pancreas and reduces glucagon secretion, supporting healthy blood sugar levels.

Evidence from clinical trials indicates that retatrutide can positively impact blood sugar levels in individuals with diabetes:

1. In adults aged 20-70 with type 2 diabetes for at least three months, retatrutide at doses of 3/6/9/12 mg led to significant reductions in blood sugar levels, with an acceptable safety profile compared to placebo. 

2. In high-fat-fed mice, administering retatrutide twice daily for 21 days lowered nonfasting blood sugar levels by increasing circulating insulin. 

 

3. In obese mice, retatrutide improved blood sugar control and enhanced energy expenditure, effects that lasted for up to 43 days.

4. In 45 healthy human subjects, the three highest doses of subcutaneous retatrutide resulted in increased mean fasting insulin and C-peptide levels, peaking at 24 and 48 hours, which corresponded with reduced blood sugar levels. 

5. In diet-induced obese mice, retatrutide lowered both blood sugar and insulin levels, indicating improved insulin sensitivity. 

6. In patients with type 2 diabetes, 12 weeks of subcutaneous retatrutide administration decreased glycated hemoglobin (HbA1c), a key measure of blood sugar, while maintaining a favorable safety and tolerability profile.

Improves Blood Pressure

As a weight loss medication, retatrutide can help lower blood pressure by addressing obesity. By reducing energy intake and increasing energy expenditure, retatrutide promotes fat loss, which is linked to blood pressure reduction. This suggests that retatrutide may be advantageous for individuals with hypertension.

Research supports the blood pressure-lowering effects of retatrutide:

1. In a Phase 1 clinical trial, the safety and tolerability of single-ascending doses of retatrutide were assessed in forty-five healthy subjects, who were randomly assigned to receive varying doses of the medication or a placebo. Throughout the study, vital signs, electrocardiograms (ECGs), laboratory data, and adverse events were monitored. Results indicated that participants receiving retatrutide experienced significant weight loss, increased insulin levels, and decreased systolic blood pressure, which returned close to baseline by Day 29.

2. Another Phase 1 proof-of-concept study evaluated the safety and tolerability of multiple ascending doses of retatrutide in patients with type 2 diabetes. In this trial, seventy-two diabetic patients were randomized to receive either retatrutide or placebo. After 12 weeks, those who received retatrutide showed reductions in blood pressure, along with a better safety and tolerability profile compared to the placebo group.

Associated Side Effects of Retatrutide

Side effects from retatrutide are quite rare. While some patients have reported issues while using the drug, these side effects have not been definitively linked to retatrutide and may have occurred by coincidence. Nevertheless, they are noted as potential side effects, even though they are uncommon.

Possible side effects of retatrutide may include:

- Chest pain
- Depression
- Difficulty breathing
- Dizziness
- Dry mouth
- Fatigue
- Headache
- Irregular heartbeat
- Swelling in the hands and feet

In terms of safety, the most frequently reported adverse events were related to the gastrointestinal system. These side effects are generally mild and tend to resolve on their own. Overall, the safety and tolerability profile of retatrutide is consistent with other incretin-based therapies, which are hormones produced by the gut that help regulate blood sugar levels.

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