RETATRUTIDE VIAL (LYOPHILIZED POWDER)

WHAT IS RETATRUTIDE?

RETATRUTIDE (Pronounced Ret-uh-true-tide) is a once-weekly injectable investigational medication currently being studied for the treatment of obesity and type 2 diabetes.

It is a novel peptide that functions as a triple hormone receptor agonist, targeting the receptors for glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and glucagon.

By activating all three receptors, RETATRUTIDE aims to provide enhanced metabolic benefits compared to medications that target only one or two of these pathways.

HOW DOES RETATRUTIDE WORK?

GLP-1 RECEPTOR ACTIVATION:

INCREASED INSULIN SECRETION: RETATRUTIDE stimulates the pancreas to release insulin in response to elevated blood glucose levels, aiding in blood sugar regulation.

DECREASED GLUCAGON SECRETION: It suppresses the release of glucagon, a hormone that raises blood sugar levels, thereby contributing to better glycemic control.

APPETITE SUPPRESSION: Activation of GLP-1 receptors in the brain leads to reduced appetite and increased feelings of fullness, promoting weight loss.

SLOWED GASTRIC EMPTYING: It delays the rate at which food leaves the stomach, helping to prevent rapid spikes in blood sugar after meals.

GIP RECEPTOR ACTIVATION:

ENHANCED INSULIN RELEASE: GIP works synergistically with GLP-1 to stimulate insulin secretion from the pancreas in a glucose-dependent manner.

IMPROVED INSULIN SENSITIVITY: It may enhance the body's responsiveness to insulin, facilitating better glucose uptake by tissues.

GLUCAGON RECEPTOR ACTIVATION:

INCREASED ENERGY EXPENDITURE: Activation of glucagon receptors promotes the breakdown of stored fats (lipolysis) and stimulates thermogenesis (heat production), leading to increased calorie burning.

WEIGHT LOSS: By enhancing fat breakdown and energy expenditure, retatrutide contributes to significant weight reduction beyond appetite suppression alone.

LIVER EFFECTS: While glucagon can stimulate glucose production in the liver, the balanced activation in retatrutide aims to mitigate adverse effects on blood sugar levels.

POTENTIAL HEALTH BENEFITS

SIGNIFICANT WEIGHT LOSS: Clinical trials have shown that retatrutide can lead to substantial weight reduction. Participants experienced an average weight loss of 24% over 48 weeks, surpassing the results of existing weight-loss medications.

IMPROVED GLYCEMIC CONTROL: Retatrutide has been effective in lowering blood sugar levels, making it a promising treatment for individuals with type 2 diabetes. In studies, participants achieved reductions in HbA1c levels, indicating better blood glucose management.

ENHANCED CARDIOVASCULAR HEALTH: The medication has been associated with improvements in cardiovascular risk factors, including reductions in blood pressure and lipid levels. These changes contribute to a decreased risk of heart disease.

REDUCTION IN LIVER FAT: Retatrutide has shown potential in reducing liver fat content, which is beneficial for individuals with non-alcoholic fatty liver disease (NAFLD). This effect may help mitigate the progression of liver-related conditions.

POTENTIAL SIDE EFFECTS

GASTROINTESTINAL ISSUES: These are common and can include nausea, vomiting, diarrhea, and constipation. These symptoms often occur at the beginning of treatment and may lessen over time.

DECREASED APPETITE: While this can be a beneficial effect for weight loss, it may lead to reduced food intake that some individuals may find difficult to manage.

POTENTIAL HYPOGLYCEMIA: Especially when used with other glucose-lowering medications, there may be a risk of low blood sugar levels.

INJECTION SITE REACTIONS: Some participants in trials reported mild to moderate reactions at the injection site, such as redness or irritation.

DIZZINESS AND HEADACHES: These were noted in some trial participants, usually occurring when the body adjusts to the medication.

POTENTIAL GALLBLADDER ISSUES: As with other weight-loss drugs, significant weight loss can increase the risk of gallstones and other gallbladder-related problems.

ELEVATED HEART RATE: Some participants have reported an increase in heart rate, which may need monitoring, especially in those with pre-existing heart conditions.

SKIN EFFECTS: Significant weight loss may cause sagging skin and more pronounced wrinkles. This is not specific to GLP-1 medications. ANYTHING that causes significant weight loss will cause more pronounced wrinkles and sagging skin because the underlying supporting structure of your skin has been stretched out from being overweight. The more overweight you are, the more pronounced this effect is when you lose weight.

If you develop intolerable nausea or vomiting, go back to the previous dose for a few more weeks and try to increase it again later. You do not have to increase to the maximum dose. If you are losing weight and not having significant side effects, you can maintain at that dose. If you develop severe constipation or abdominal pain, stop the medication and get evaluated by your PCP or Emergency Dept ASAP. If you develop swelling in your neck or difficulty swallowing, get evaluated by your PCP or Emergency Dept.

DOSAGE GUIDELINES

Retatrutide is given as a weekly subcutaneous injection. The starting dose is 1mg weekly, and the maximum dose is 8mg weekly. Very few individuals require the maximum dosage. The optimal dosage is one in which you are losing weight and don’t have intolerable side effects. This is different for each individual.

If you experience intolerable side effects, like nausea and vomiting, go back to the dose you were at before for a week or two and try increasing it again. If intolerable nausea or vomiting persists, just stay at the dose you tolerate.

RETATRUTIDE is an investigational drug in Phase 2 clinical trials at Lilly. It is currently only available as a research peptide.

RECONSTITUTION INSTRUCTIONS

18mg Vial (10mg)

Inject 1.8 ml of bacteriostatic water into the vial of powder (1.8ml = 180 units).

36mg Vial (20mg)

Inject 3.6 ml of bacteriostatic water into the vial of powder (3.6ml= 360 units)

STORAGE AND STABILITY FOR RESEARCH PEPTIDES

AS LYOPHILIZED POWDER vials, requiring no refrigeration during shipping.

In LYOPHILIZED Form:

Stable for up to 3 years in the freezer and 2 years in the refrigerator.

Protect from light.

ONCE RECONSTITUTED:

Stable for 6 weeks.

Must be refrigerated and kept away from light.

Avoid placing vials in the refrigerator door to prevent degradation from frequent temperature changes.

IMPORTANT DISCLOSURES

These statements have not been evaluated by the US Food and Drug Administration (FDA).

Not intended to diagnose, treat, cure, or prevent any disease.

Research peptides and some compounded drugs are not FDA-approved but are produced under strict quality control measures.

QUALITY ASSURANCE

The manufacturer ensures quality, safety, and efficacy, complying with regulatory standards.