Retatrutide 5mg

Retatrutide (LY3437943) is a peptide drug targeting GLP-1R/GCGR/GIPR developed based on the GIP peptide sequence. Its average half-life in humans is up to 6 days, and its half-life in mice is 21hr (0.47mg/kg).

 

Retatrutide is a single peptide modified from the GIP peptide backbone, containing 39 amino acids, which can achieve triple agonist activity in GCGR, GIPR and GLP-1R. Its peptide backbone sequence contains three non-coding amino acid residues at positions 2, 20 and 13. Among them, Aib2 (α-aminoisobutyric acid) helps to improve stability against degradation by dipeptidyl peptidase-4 (DPP4); Aib20 helps to optimize GIP activity, pharmacokinetic properties and developability; αMeL13 (α-methyl-L-leucine) helps to optimize glucagon (GCG) and GIP activity. The backbone is coupled to a C20 fatty diacid moiety via a linker located at a lysine residue at position 17, which extends the half-life via albumin binding while providing the desired pharmacological properties.

 

A total of 338 adult obese patients were enrolled in this Phase II clinical trial to explore the weight loss effects of three doses of 4mg, 8mg, and 12mg and different starting doses.

The results showed that at 24 weeks of treatment, Retatrutide (1mg, 4mg, 8mg or 12mg) achieved the primary endpoint of efficacy evaluation in obese or overweight (excluding diabetes) adult patients, with an average weight loss of 17.5%.

In terms of secondary endpoints, at 48 weeks of treatment, the average weight loss of subjects receiving weekly injections of 12mg Retatrutide was 24.2%.

 

Is retatrutide the same as Ozempic?

 

What does the drug retatrutide do?

Lowering blood sugar: Liraglutide can promote the secretion of insulin and inhibit the secretion of glucagon, thereby lowering blood sugar levels. It is widely used to treat type 2 diabetes to improve blood sugar control.

Weight loss: Liraglutide can also help lose weight. It helps control weight by increasing satiety and reducing appetite. Therefore, it is also used to treat obesity111213.

Improving cardiovascular function: Liraglutide can improve cardiovascular function, such as lowering blood pressure and improving blood lipid metabolism, thereby reducing the risk of cardiovascular disease.

Protecting the kidneys: Liraglutide can also reduce kidney damage, improve kidney function, and has a certain protective effect on diabetic nephropathy.

Relieving arthritis symptoms: Liraglutide also shows certain potential in the treatment of knee arthritis and can relieve arthritis symptoms. It should be noted that as a glucagon-like peptide-1 (GLP-1) receptor, the specific mechanism of action of liraglutide is to simulate the action of the GLP-1 hormone produced in the human body to produce the above effects.

 

Is retatrutide FDA approved?

No yet

Is retatrutide better than tirzepatide?

Retatrutide is an active compound called retatrutide released by Eli Lilly in June 2023. It is a triple (GLP-1/GIP/Gcg) agonist based on the GLP/GI dual receptor agonist Tirzepatide through a hybrid glucagon (GlucagonGcg) related structure, and is a drug for the treatment of obesity and type 2 diabetes. This active compound can activate receptor agonists in our body, which helps control blood sugar and manage weight loss. Its sequence is H-Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Ile-Ala-Gln-{20diacid-gamma-Glu-(AEEA)2-Lys}-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

 

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