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Retatrutide

Retatrutide structure

CAS No:
2381089-83-2
Formula:
C221H342N46O68
Chemical Name:
Retatrutide
Synonyms:
Retatrutide;GIPR/GLP-1R;LY3437943Retatrutide;Retalutide;Retatrutide (sodium salt);Retatrutide RT5;retatrutide 5mg;Retatratide
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Retatrutide is a novel triple agonist peptide of the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR) and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits human GCGR, GIPR and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively and mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively. It is an important tool for obesity research.Retatrutide potently activates the GLP-1R signaling pathway to stimulate glucose-dependent insulin secretion through activity at the GIP receptor (GIPR) or the GLP-1R.Retatrutide is a synthetic peptide with glucose-lowering effects. It is an antidiabetic agent against type 2 diabetes (T2D), stimulating insulin and suppressing glucagon secretion in a glucose-dependent manner.Retatrutide was also shown to delay gastric emptying, lower fasting and postprandial glucose concentration, decrease food intake and reduce body weight in patients with type 2 diabetes.

Retatrutide Basic Attributes

Molecular Weight：

4731.33

EC Number：

200-001-8

Color/Form：

White lyophilized

Characteristics

Water Solubility：

Soluble in water (5mg/ml).

Storage Conditions：

-20°C

Critical Temperature & Pressure：

-20°C

Drug Information

Drug Indication：

Investigated for the treatment of type 2 diabetes mellitus (T2DM), obesity, and overweight in adults. Additional potential indications under clinical evaluation include non-alcoholic fatty liver disease (NAFLD), metabolic dysfunction-associated steatohepatitis (MASH), and cardiovascular risk reduction.

LiverTox Summary：

No significant hepatotoxicity has been reported in clinical trials to date. However, periodic monitoring of liver enzymes (ALT, AST) is recommended, especially in patients with pre-existing liver conditions or during long-term therapy.

Drug Classes：

Triple agonist of GLP-1, GIP, and GLP-2 receptors; peptide-based antidiabetic and anti-obesity agent.

Drug Transformations：

Subcutaneously administered; metabolized via enzymatic degradation in liver and kidneys; eliminated renally and fecally.

Therapeutic Uses：

Glycemic control in type 2 diabetes and chronic weight management in obesity or overweight with comorbidities.

Drug Warnings：

Risk of GI adverse effects, hypoglycemia (with insulin/sulfonylureas), pancreatitis, gallbladder disease, and acute kidney injury; contraindicated in personal/family history of MTC or MEN 2; not for use in pregnancy.

Reported Fatal Dose：

Human lethal dose not established; preclinical data suggest a wide safety margin.

Drug Tolerance：

Generally well tolerated; most adverse events are mild-to-moderate gastrointestinal symptoms that improve over time.

Pharmacology：

Long-acting triple receptor agonist that enhances insulin secretion, suppresses glucagon, delays gastric emptying, promotes satiety, and may support gut integrity via GLP-2 activity.

MeSH：

GLP-1 Receptor Agonists; GIP Receptor Agonists; Peptide Hormones; Hypoglycemic Agents; Anti-Obesity Agents

Absorption：

Slow SC absorption (Tmax ～4–6 h); high plasma protein binding (～95%); primarily degraded by peptidases; excreted in urine and feces; half-life ～3.5 days enabling once-weekly dosing.

Metabolism/Metabolites：

Inactive or low-activity peptide fragments generated by proteolytic cleavage, not dependent on CYP450 enzymes.

Biological Half-Life：

Approximately 3.5 days.

Mechanism of Action：

Retatrutide is a triple agonist of GLP-1, GIP, and GLP-2 receptors, promoting insulin secretion, suppressing glucagon release, delaying gastric emptying, enhancing satiety, and protecting renal function by reducing albuminuria in diabetic kidney disease models.

Impurities：

No significant impurities reported in clinical-grade formulations; minor peptide degradation products may occur during storage but are within acceptable limits per ICH guidelines.

Health Hazards：

Common side effects include nausea, diarrhea, vomiting, constipation, and headache; rare but serious risks include pancreatitis, gallbladder disease, hypoglycemia, and acute kidney injury.

First Aid：

In case of overdose or severe adverse reaction, discontinue drug immediately; provide supportive care including hydration, antiemetics, and monitoring of vital signs; no specific antidote available.

Antidote：

No known antidote; management is symptomatic and supportive; monitor for dehydration, electrolyte imbalance, and hypoglycemia; hospitalization may be required in severe cases.

Human Toxicity Excerpts：

Retatrutide has favorable safety profile in clinical trials with dose-dependent GI tolerability; no major organ toxicities observed; long-term human toxicity data still under evaluation.

MeSH Entry Terms：

Retatrutide; Glucagon-Like Peptide-1 Receptor Agonists; Obesity; Diabetes Mellitus, Type 2; Weight Loss Agents; Peptide Hormones

DEA Controlled Substances：

Not listed as a controlled substance under the U.S. Controlled Substances Act (DEA); not scheduled by FDA or international regulatory bodies.

Exposure Routes：

Subcutaneous injection only; systemic absorption via SC route; not intended for oral, intravenous, or other routes of administration.

Symptoms：

Nausea, vomiting, diarrhea, constipation, headache, fatigue, dizziness, abdominal pain, and hypoglycemia-related symptoms such as sweating, tremor, and confusion.

Target Organs：

Pancreas, liver, gastrointestinal tract, kidneys, adipose tissue, central nervous system (via appetite regulation), and cardiovascular system.

Retatrutide Use and Manufacturing

Methods of Manufacturing

Retatrutide is synthesized using recombinant DNA technology and solid-phase peptide synthesis (SPPS). The peptide backbone is assembled chemically, followed by purification via high-performance liquid chromatography (HPLC) and sterile filtration. Final formulation includes stabilizing excipients such as sodium chloride, citric acid, and polysorbate 20 in a pH-controlled buffer system for subcutaneous injection.

Uses

Retatrutide is an investigational triple agonist of GLP-1, GIP, and GLP-2 receptors being developed for the treatment of type 2 diabetes mellitus, obesity, and overweight in adults. It is also under clinical evaluation for weight management in patients with metabolic dysfunction-associated steatotic liver disease (MASH) and cardiovascular risk reduction.

Retatrutide is a once-weekly triple hormone receptor agonist developed by Eli Lilly and Company. It is a single-molecule peptide consisting of 39 amino acids with a molecular weight of approximately 4,731.33 Da. Its amino acid sequence has been optimised to achieve balanced agonist activity at the glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide-1 receptor (GLP-1R), and glucagon receptor (GCGR). By simultaneously targeting all three receptors, retatrutide provides a multifaceted approach to metabolic regulation. Activation of the GLP-1 pathway suppresses appetite and delays gastric emptying, GIP signalling enhances insulin sensitivity and supports lipid metabolism, while GCGR activation increases energy expenditure and promotes hepatic fat oxidation. The complementary actions of these pathways enable comprehensive regulation of energy intake, metabolic efficiency, and energy expenditure, contributing to substantial weight loss and metabolic improvement.

Drug Function and Efficacy

Triple agonist of GCGR, GIPR, and GLP-1R, involved in weight management and blood sugar control

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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