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What is Retatrutide Peptide?

Retatrutide is a peptide modified from the GIP peptide skeleton. Retatrutide containing 39 amino acids, which can achieve triple agonist activity on GCGR, GIPR and GLP-1R. Retatrutide participates in GCGR in vivo and improves glucose tolerance in ipGTT via GIP or GLP-1 receptors.

Retatrutide can also be used in obesity research. Retatrutide causes significant weight loss and increases energy expenditure through glucagon receptor activation. 

Development of Retatrutide

The average half-life of retatrutide in humans is up to 6 days, and the half-life in mice is 21 hours (0.47mg/kg). Its peptide backbone sequence contains three non-coding amino acids at positions 2, 20 and 13.

Among them, Aib2 helps improve stability against the degradation of DPP4. Aib20 helps optimize GIP activity. αMeL13 helps optimize GCG and GIP activity. The backbone is coupled to the C20 fatty diacid moiety via a linker located at lysine 17th. It can extending half-life through albumin binding while providing the desired pharmacological properties.

Retatrutide Clinical Trials

The latest clinical trial data of Retatrutide in the treatment of obesity and NAFLD was announced at the 83rd ADA Academic Meeting. On the same day, the NEJM published online the results of the phase 2 clinical trial of Retatrutide in the treatment of obesity.

1. Retatrutide achieves record weight loss results

This randomized, double-blind, phase 2 clinical trial evaluated the weight loss efficacy and safety of placebo and varying doses of retatrutide after 48 weeks of treatment.

The study included adults with a BMI of ≥30 kg/m2 or a BMI of 27 to <30 kg/m2 and at least one weight-related disease (except diabetes), followed by a 2:1:1:1:2:2. Proportions were randomly assigned and received retatrutide injection treatment at doses of 1 mg, 4 mg (initial dose 2 mg), 4 mg (initial dose 4 mg), 8 mg (initial dose 2 mg), 8 mg (initial dose 4 mg), 12 mg ( Initial dose 2 mg).

The primary endpoint of the clinical trial was the percentage change in body weight from baseline to 24 weeks. Secondary endpoints include percent weight change from baseline to 48 weeks, proportion of weight loss ≥5%, ≥10%, ≥15%, and safety of treatment.

The average age of the 338 patients enrolled was 48.2 years old, and 51.8% were male. There were no differences in baseline characteristics between different treatment groups.

2. Retatrutide weight loss effect

Retatrutide treatment at all doses demonstrated clinically meaningful weight loss compared to placebo, with greater weight loss in women.

With weekly injections of Retatrutide dosage 12 mg, patients lost an average of 24.2% of their weight after 48 weeks, which is the best effect of drug weight loss so far. nearly half of patients can achieve weight loss ≥ 25%. 1/4 of patients can achieve weight loss ≥ 30%. At a weekly injection dose of 8 mg, all patients achieved >5% weight loss after 48 weeks regardless of dose.

3.Greater Liver Fat Reduction

Retatrutide showed greater liver fat reduction and great improvements in NASH-related biomarkers (K-18 and Pro-C3).

At the doses of 8 mg and 12 mg, the average relative liver fat reduction rate of patients was >80%.

At the doses of 8 mg and 12 mg, more than 80% of patients achieved a fat loss rate of ≥70%.

At the doses of 8 mg and 12 mg, >85% of patients lost liver fat at 48 weeks.

At the highest dose of retatrutide (12 mg size), more than 90% of obese and NAFLD patients achieved great effect of liver fat. This suggests that the addition of GCG agonism to GlP and/or GlP-1  may have a beneficial effect on NAFLD / NASH patients. It have more powerful strong effects as far as we know. 

The current pilot lab data, as well as the weight loss results from the main Phase 2 trial data, provide further evaluation of retatrutide in patients with NASH.

Adverse Reactions of Retatrutide 

Adverse events were reported by 70% of patients in the placebo group. 73% to 94% of patients in the retatrutide group reported adverse events, and the incidence of adverse events was higher in the 8 mg and 12 mg groups. The most common adverse events leading to discontinuation were mild to moderate gastrointestinal reactions, occurring primarily during dose increases.

The most common adverse events in the retatrutide group were mild to moderate gastrointestinal reactions and were dose-related. In short, in adult obese patients, retatrutide showed superior weight loss and was well tolerated.

The findings were published online the same day in NEJM. NEJM also wrote in its tweet: "The weight loss achieved by this drug is very large compared with other weight loss drugs and is comparable to bariatric surgery."

Retatrutide vs Tirzepatide

According to current clinical data released by various drugs, Tirzepatide can reduce weight by 26.6% after 84 weeks.

Restarutide reduced the average weight of the subjects by 24.2% in just 48 weeks. According to industry media STAT, this is the drug that has achieved the highest weight loss rate so far. If Retatrutide is finally approved for marketing, it may break the weight loss record set by Tirzepatide.

Omizzur Retatrutide Peptide for Sale - Buy 5/10mg in stock

About Omizzur Ltd

Omizzur ltd is a company engaged in peptide. We providing professional and strong support to pharma companies, drug R&D institutions and universities all of the world. Most of our clients come from the USA, Europe, India and other countries. We try best to help you complete your R&D project with the same high-quality products at a lower price.

Most commonly used products are in stock. Some special products require custom-made (it depending on the difficulty and quantity of product, the deliver time is about 2-4 weeks). For product details please get in touch with our customer services for help.

About TFA removal in Retatrutide:

During the peptide synthesis process, some salt needs to be added. But there are many types of salts, and the peptides made from different types of salts are different and have different effects. So today we mainly choose the appropriate type of peptide salt in peptide synthesis.

TFA: This is a salt commonly used in peptide products. But due to the toxicity of TFA, some experiments need to avoid using this salt. The peptides synthesized by the company are generally in the form of TFA salts. If residual TFA will affect your experiments, we generally recommend conversion to other salts such as AC and HCL forms. 

These salt forms of the peptide typically cost 20% to 30% more than TFA salts because some of the peptide is lost during the salt transfer process and it will need more raw materials. TFA can cause many problems. Therefore, we can remove TFA salts and avoid them in the first step.

Shipping

Usually we arrange shipping within 24 hours of receiving the order (except Sundays). We ship by Fedex, DHL and other methods for global shipping. Most countries can deliver goods within 7 days.

If there are customs clearance issues, it may be delayed for 2-3 days. It depending on the customs processing speed of each country. We will provide support for your local customs to complete this process as soon as possible.

Storage

When peptides are received, please make sure they are kept in a cool, dark place. For best storage, store them under fridge at 4°C or colder, away from bright light. Solid peptides are stable at room temperature for a few weeks. For long-term storage, -20°C is best.

Contamination with moisture will greatly decrease long term storage of solid peptides. Every time you use some of them, remove the container from cold storage and allow it to equilibrate to room temperature or slightly warmer before opening it. It will reduce the uptake of moisture from the air onto the cold surface of the solid peptide or the inside of the container. 

After removing the required quantity, re-seal the container, preferably under an atmosphere of dry nitrogen. This can be achieved by blowing a gentle stream of dry nitrogen into a plastic bag housing the container. taking great care to avoid blowing the peptide powder right out of the container. After the air is displaced, quickly cap the container, and then return it to cold storage. This procedure will minimize the oxidation of air-sensitive peptides as discussed later.

Customer Service Center

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References:

[1] Chalasani N, et al. Hepatology, 2018;67:328-357.

[2] Flint A, et al. Hepatology, 2020;72:1036A.

[3] Hartman ML, et al. Diabetes Care, 2020;43:1352-1355.

[4] Gastaldelli A, et al. Lancet Diabetes Endocrinol, 2022;10:393-406.

[5] Newsome PN, et al. N Engl J Med, 2021;25:1113-1124.

[6] Abdelmalek MF. J Hepatol, 2020;73:S124.

[7] Flint A, et al. Aliment Pharmacol Ther, 2021:54:1150-1181.

[8] Harrison SA, et al. Nat Med, 2021;27:1262-1271.