Retatrutide is a special type of medication that works on three different receptors in the body: GCGR, GIPR, and GLP-1R. It’s made up of a fatty acid attached to a single peptide, which is a molecule made of amino acids. This medication is designed based on a modified version of a peptide called GIP. The modification allows retatrutide to stick to a protein called albumin in the blood. Because of this, the medication stays in the bloodstream for a long time, meaning people only need to take it once a week for it to work.
This medication has a broad range of effects because it can attach to different receptors. Here’s how it works on each of them:
- Gastric Inhibitor Peptide Receptor (GIPR): This receptor, also known as the glucose dependent insulinotropic polypeptide receptor, is found in the brain and throughout the digestive system. It seems to be important for controlling hunger and telling the brain when the stomach is full.
- Glucagon-like Peptide Receptor-1 (GLP-1R): When this receptor is activated, it slows down how fast the stomach empties. Slower stomach emptying signals the brain to eat less, helping to manage weight. Drugs targeting this receptor were first made to treat type 2 diabetes, but they’ve been found to help with weight loss and reduce the risk of certain heart problems. Scientists are also looking into whether they could be used to treat depression, alcoholism, and other conditions.
- Glucagon Receptor (GCGR): This receptor is mostly found in the liver and kidneys. Changes in this receptor are linked to some types of type 2 diabetes. When retatrutide attaches to this receptor, it boosts the production of glucagon, a hormone that helps break down stored energy like fat and sugar. This increases the body’s basic metabolism, even when sleeping, which leads to overall weight loss and specifically burns fat.
BENEFITS OF RETATRUTIDE
- Helps induce weight loss
- Helps slow food leaving your stomach
- Helps prevent your liver from making too much sugar
- Helps the pancreas produce more insulin when your blood sugar levels are high
- Helps control blood glucose
- Can reduce hyperglycemia, especially after meals
- Can reduce fasting insulin and fasting glucose
- Can reduce hemoglobin A1c
- Can decrease appetite and caloric intake, while inhibiting weight gain
- Has been shown to lower triglyceride levels and oxidative stress from high LDL
- Helps decrease leptin and increase leptin sensitivity
- Can increase the conversion of white fat to brown fat
- May improve blood pressure
Retatrutide Dosage for Weight Loss
Studies suggest that retatrutide is one of the most effective weight loss medications based on incretins. In human phase 2 trials, retatrutide significantly reduced body weight. Participants given the highest dose lost around 20 pounds in 12 weeks, and others lost inches from their waist in 6 months. Weight loss with retatrutide varied with the dose over 48 weeks, with higher doses leading to more weight loss.
In a study reported in the New England Journal of Medicine, the amount of weight lost with retatrutide varied depending on the dose over the 48-week trial period. Those who received the lowest dose lost 8.7% of their total body weight, while those on the highest dose lost more than 24%. Similar findings were also reported in a JAMA article.
Retatrutide and Diabetes
Retatrutide has also shown promise in reducing glycated hemoglobin levels, which is important for managing diabetes and preventing its complications. Its effects on heart health are still being studied, but research suggests that it might improve heart rate and blood pressure.
In phase 2 trials, retatrutide has been found to significantly lower levels of glycated hemoglobin (HbA1c). Hemoglobin is a protein in the blood that carries oxygen, but when it combines with sugar, it forms glycated hemoglobin. High levels of this type of hemoglobin are usually due to consistently high blood sugar levels, which are characteristic of diabetes. Monitoring HbA1c levels is important for managing diabetes because keeping them low not only helps control blood sugar effectively but also reduces the risk of long-term complications like heart disease, nerve damage, kidney problems, and eye issues.
Retatrutide and Heart Health
Although the direct impact of retatrutide on heart health in humans hasn’t been studied, research has been conducted.
Supporting this idea is the fact that several incretin agonists like semaglutide and liraglutide have been linked to improvements in heart health among people with diabetes. Because of this, these peptides are now being studied for potential direct use in treating heart disease. Retatrutide is expected to yield even better outcomes due to its broader impact on glucagon levels. However, the exact effects will need further investigation through detailed clinical and benchtop trials. These findings suggest that retatrutide and similar molecules could be beneficial for repairing the cardiovascular system and preventing heart disease in the first place.
Final Thoughts
Retatrutide represents an exciting new development in the world of weight loss medications, offering a multi-faceted approach that targets fat loss while preserving muscle mass. Its once-weekly injection, reduced nausea, and muscle-sparing properties make it a potentially better option than some of the current weight loss drugs on the market, particularly for people with obesity who are also managing blood sugar levels and blood pressure.
Like any medication, the effectiveness of Retatrutide will vary from person to person. While it seems to offer more benefits, especially for people with obesity looking for sustainable weight loss, it is essential to consult with a healthcare professional to determine if it’s the right fit for you.