Edotreotide is a radioactive-labeled diagnostic and therapeutic drug, belonging to the class of somatostatin analogues. Its core mechanism is to highly selectively target cells with overexpressed somatostatin receptors, especially the common SSTR2 subtype found on the surface of neuroendocrine tumor cells. When it combines with positron radionuclides such as gallium-68 (⁶⁸Ga), it becomes an outstanding diagnostic tool (such as ⁶⁸Ga-Edotreotide), which can precisely locate, stage and evaluate the efficacy of tumors through positron emission tomography/computed tomography, with high image clarity. When it is combined with therapeutic beta-ray radionuclides such as lutetium-177 (¹⁷⁷Lu) or yttrium-90 (⁹⁰Y), it transforms into a targeted radioligand therapy drug, which can precisely deliver the radioactive nuclides to the interior of the tumor lesion, using radiation to destroy cancer cells from the inside, achieving systemic treatment for inoperable or metastatic neuroendocrine tumors. Therefore, Edotreotide embodies the advanced concept of "diagnosis and treatment integration", providing a key means for the entire course of management of neuroendocrine tumors.
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Edotreotide COA
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| Certificate of Analysis | ||
| Compound name | Edotreotide | |
| CAS No. | 204318-14-9 | |
| Quantity | 85g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co.,Ltd | |
| Lot No. | 20251205035 | |
| MFG | Dec.05th2025 | |
| EXP | Dec.05th2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White to off-white solid powder | Conformed |
| Water content | ≤5.0% | 0.23% |
| Loss on drying | ≤1.0% | 0.22% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.30% |
| Single impurity | <0.8% | 0.13% |
| Total microbial count | ≤750cfu/g | 102 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 540pm |
| Storage | Store in a sealed, dark, and dry place below 2-8°C | |
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| Chemical Formula | C65H92N14O18S2 |
| Exact Mass | 1420.62 |
| Molecular Weight | 1421.65 |
| m/z |
1420.62(100.0%),1421.62(70.3%),1422.62(24.3%),1422.61(9.0%), 1423.61(6.4%),1421.61(5.2%),1423.63(4.7%),1422.62(3.7%),1422.62(3.4%), 1423.62(2.6%),1424.62(2.2%),1421.61(1.6%),1423.62(1.3%),1422.62(1.1%),1421.62(1.1%) |
| Elemental Analysis | C,54.92;H,6.52,N,13.79;O,20.26'S,4.51 |
Edotreotide is an artificially synthesized cyclic octapeptide compound, belonging to the family of somatostatin analogues. It possesses unique chemical properties and plays a significant role in medical diagnosis and treatment.
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Basic Chemical Structure
The molecular formula of Edotreotide is C₆₅H₉₂N₁₄O₁₈S₂, with a molecular weight of approximately 1421.64 (variations may exist due to purity or preparation conditions in different sources). Its structure is formed by the combination of DOTA (a peptide cross-linking agent) and Tyr³-Octreotide (a somatostatin analogue), resulting in a stable cyclic conformation. This cyclic structure is maintained by the disulfide bond formed between two cysteines, which is crucial for its specific binding to the target receptor. The N-terminal of the Edotreotide peptide chain contains a large number of carboxyl functional groups, and the N-terminal itself is an alcohol hydroxyl functional group. The presence of these functional groups gives it certain chemical activity and reactivity.
Physical Properties
Edotreotide typically exists as a white to off-white solid powder at room temperature. It has good solubility and can dissolve in most organic solvents, such as dimethyl sulfoxide (DMSO), as well as water. This property enables Edotreotide to be conveniently formulated into the desired concentration solutions for laboratory research and clinical applications.
Chemical Stability
The chemical stability of Edotreotide is influenced by various factors, such as temperature, light exposure, humidity, and the choice of solvent. During storage, to maintain its chemical stability and biological activity, Edotreotide powder should be sealed and stored at a low temperature of -20°C, avoiding light and moisture. If it is prepared as a solution, it should be aliquoted to prevent repeated freezing and thawing, which could damage its structure and activity. At -80°C, the Edotreotide solution can be stored for several months; while at -20°C, the storage time is relatively shorter.
Binding Capacity with Radioisotopes
One of the most remarkable chemical properties of Edotreotide is its ability to bind with various radioisotopes, forming highly affinity tracers or therapeutic drugs. For instance, Edotreotide can bind with gallium-68 (⁶⁸Ga), forming ⁶⁸Ga-Edotreotide, which is an efficient PET diagnostic agent. After intravenous injection, ⁶⁸Ga-Edotreotide can specifically bind to the somatostatin receptors (SSTR) on the surface of neuroendocrine tumor cells, particularly the SSTR2 subtype, thereby clearly showing the location, size and metastasis of the tumor in PET scans.
Furthermore, Edotreotide can also be combined with therapeutic radioactive nuclides (such as yttrium-90 (⁹⁰Y), lutetium-177 (¹⁷⁷Lu)) to form radiopharmaceutical conjugates (RDCs). These drugs can target and deliver the radioactive nuclides to SSTR-positive tumor cells, releasing beta rays to induce apoptosis of the tumor cells, thereby achieving precise treatment.
Biological Activity and Pharmacological Effects
The biological activity of Edotreotide is mainly based on its high affinity binding to somatostatin receptors. Somatostatin receptors are highly expressed on the surface of various neuroendocrine tumor cells. After reaching the tumor site through the bloodstream, Edotreotide specifically binds to SSTR through its unique cyclic structure. After binding, it can trigger changes in a series of intracellular signaling pathways, such as inhibiting adenylate cyclase activity and reducing the production of cyclic adenosine monophosphate (cAMP), thereby inhibiting the metabolism, proliferation, and differentiation of tumor cells and achieving the purpose of inhibiting tumor growth.
Edotreotide is a selective ligand that targets the somatostatin receptor 2 (SSTR2). Its production process involves complex chemical synthesis and radioactive labeling techniques. The following details the manufacturing information from five aspects: raw material selection, synthesis steps, quality control, radioactive labeling, and formulation production.
Raw Material Selection
The synthesis of Edotreotide begins with precise ratios of various amino acids, among which glycine and phenylalanine are the key components. These amino acids must meet high purity standards to ensure the biological activity of the final product. Additionally, during the synthesis process, a metal chelating agent, DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), is used. It can form stable complexes with radioactive isotopes, providing the basis for the radioactive labeling of Edotreotide.
Synthesis Steps
Amino acid condensation
Under strict reaction conditions, the selected amino acids are subjected to a condensation reaction in a specific molar ratio. This step requires precise control of temperature, pH value, and reaction time to ensure that the amino acids are correctly linked to form a peptide chain.
The condensation reaction is typically carried out using the solid-phase synthesis method, which builds the peptide chain step by step by gradually adding amino acids and removing protecting groups. The solid-phase synthesis method has the advantages of simple operation and high product purity.
Deprotection and cyclization
After the peptide chain synthesis is completed, the protecting groups need to be removed to expose the reactive sites. This step is usually carried out using specific chemical reagents under mild conditions to avoid damaging the peptide chain.
Subsequently, a cyclization reaction is carried out to form the stable cyclic structure of Edotreotide. The cyclization reaction is typically carried out using oxidants or cross-linking agents to form disulfide bonds or other covalent bonds at specific positions in the peptide chain, thereby stabilizing the peptide chain structure.
Purification and desalting
The crude Edotreotide product after synthesis needs to undergo purification steps to remove impurities and unreacted raw materials. The purification methods typically include high-performance liquid chromatography (HPLC), ion exchange chromatography, etc.
The purified product also needs to undergo desalting treatment to remove residual salts and other small molecule impurities. Desalting treatment is typically carried out using methods such as dialysis, ultrafiltration, or gel filtration.
Quality Control
During the synthesis process, strict quality control measures need to be taken at each step to ensure the purity and biological activity of the final product. Quality control measures include:
Raw material inspection
Conduct purity tests and impurity analyses on the used amino acids, DOTA, etc.
Intermediate monitoring
Take samples regularly during the synthesis process to test the purity and structural correctness of the intermediates.
Finished product inspection
Conduct a comprehensive quality analysis of the final product, including tests for purity, molecular weight, specific rotation, solubility, etc.
Radioisotope Labeling
The radioisotope labeling of Edotreotide is one of the key steps in its manufacturing process. By combining with radioactive isotopes (such as ⁶⁸Ga, ¹⁷⁷Lu, ⁹⁰Y, etc.), Edotreotide can form radiopharmaceuticals with diagnostic and therapeutic functions. The radioisotope labeling process typically includes the following steps:
Radioisotope preparation: Radioactive isotopes required are prepared using generators or accelerators.
Labeling reaction: Under appropriate reaction conditions, the radioactive isotopes are subjected to a labeling reaction with Edotreotide. This step requires precise control of reaction conditions to ensure labeling efficiency and product purity.
Purification and quality control: The labeled product needs to undergo purification steps to remove unreacted radioactive isotopes and other impurities. Subsequently, strict quality control tests are conducted to ensure the safety and efficacy of the product.
Preparation of Formulations
The radioactively labeled Edotreotide needs to be further formulated into formulations suitable for clinical use. The formulation production process includes:
Solution preparation: Dissolve the labeled Edotreotide in an appropriate solvent and adjust the pH value and osmotic pressure parameters to meet the clinical usage requirements.
Sterility treatment: Perform sterility treatment on the prepared solution to ensure the sterility of the product.
Packaging and storage: Package the sterile solution into appropriate containers and store it under specified conditions to maintain the stability and activity of the product.
FAQ
What is edotreotide?
Edotreotide is defined as a radiolabelled somatostatin analogue that has a high binding affinity for somatostatin receptors and is used in peptide receptor radionuclide therapy for patients with neuroendocrine tumors, showing promise in symptom improvement and tumor stabilization.
How is it used for diagnosis and treatment respectively?
Diagnosis: Combined with the positron nuclide gallium-68 (⁶⁸Ga), it serves as a PET/CT imaging agent, precisely locating the tumor.
Treatment: Combined with therapeutic nuclides (such as lutetium-177), it becomes a targeted radioligand therapy drug, using radiation to kill tumor cells.
What are its core advantages?
It achieves "integrated diagnosis and treatment": By using the same targeted molecule for high-sensitivity imaging diagnosis and precise targeted radiotherapy, it provides a complete solution covering diagnosis, staging, efficacy evaluation and treatment for neuroendocrine tumors.
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