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  • Retatrutide

Retatrutide

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Main characteristics All specifications
CAS Number:: 2381089-83-2
Molecular Formula:: C221H342N46O68

Retatrutide

Manufacturer: Hilma Biocare

Package: 10 mg 

Common Names: Retatrutide, LY-3437943

Info: Retatrutide is a triple receptor agonist targeting GLP-1, GIP, and glucagon receptors. It is a synthetic peptide based on incretin hormone pathways designed to regulate metabolic activity, appetite, and energy expenditure. The molecule is a modified peptide engineered to enhance receptor affinity, prolong stability in circulation, and improve pharmacokinetic properties for once-weekly administration.

Effects

Retatrutide activates GLP-1 and GIP receptors while also stimulating the glucagon receptor, resulting in a broader metabolic effect compared to dual agonists. Through GLP-1 and GIP activity, it enhances glucose-dependent insulin secretion and improves glycemic control. The glucagon receptor activation contributes to increased energy expenditure and fat oxidation, which may support greater reductions in body weight. The compound also influences appetite regulation through central nervous system pathways, leading to reduced caloric intake. Clinical data indicate significant improvements in insulin sensitivity, lipid metabolism, and body weight reduction, with dose-dependent responses observed over time.

After administration, retatrutide shows a prolonged absorption phase consistent with weekly dosing and reaches steady-state concentrations after several weeks of continuous use. Its pharmacokinetic profile supports sustained receptor engagement and gradual metabolic adaptation. Clearance is slow, contributing to its extended duration of action. No dose adjustment is typically required for mild renal or hepatic impairment based on current available data, and clinically significant drug interactions remain under investigation.

Side Effects

Common side effects of Retatrutide are mainly gastrointestinal, including nausea, vomiting, diarrhea, constipation, and abdominal discomfort, especially during dose escalation periods. Other possible effects include decreased appetite, fatigue, and mild dehydration. In clinical observations, more serious adverse events are uncommon but may include pancreatitis, gallbladder-related disorders, hypoglycemia (particularly when combined with other glucose-lowering agents), and potential thyroid-related risks. Any persistent or severe symptoms should be evaluated by a healthcare professional.

Dosage Range and Duration of Use

Retatrutide is administered via subcutaneous injection, typically on a once-weekly schedule. Treatment is generally initiated at a low introductory dose of around 1 mg, with gradual escalation over time to improve tolerability and reduce gastrointestinal side effects. Depending on individual response and tolerability, the dose may be increased stepwise toward higher maintenance levels, reaching up to 12 mg in clinical study settings. A common titration approach follows a structured schedule: Weeks 1-4 at 1 mg, Weeks 5-8 at 2 mg, Weeks 9-12 at 4 mg, Weeks 13-16 at 6 mg, and from week 17 onward increasing to a maintenance range of 8-12 mg. Adjustments should always be individualized and guided by clinical response and tolerability.

Combination with Other Drugs

Retatrutide is not recommended for individuals with a history of medullary thyroid carcinoma or multiple endocrine neoplasia type 2. Caution is advised in patients with a history of pancreatitis or severe gastrointestinal disease. When combined with insulin or other antidiabetic medications, the risk of hypoglycemia may increase. It may also affect the absorption of orally administered medications due to delayed gastric emptying. Patients should inform their healthcare provider of all concurrent medications and supplements before starting therapy to avoid potential interactions.

MAIN FEATURES
CAS Number:
2381089-83-2
Molecular Formula:
C221H342N46O68

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Tags: Retatrutide, LY-3437943