Octreotide Acetate Injection is an artificially synthesized octapeptide derivative of natural somatostatin. Its chemical essence is a cyclic octapeptide with a molecular formula of C51H70N10O12S2 and a molecular weight of approximately 1079.29. Its amino acid sequence is D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OH, connected by disulfide bonds to form a cyclic structure. Compared with natural somatostatin, the chemical structure of octreotide acetate has been optimized, retaining key active fragments while enhancing its stability and biological activity through artificial synthesis. The chemical properties of octreotide acetate are stable and it is in a solid state at room temperature. It is easily soluble in solvents such as dimethyl sulfoxide (DMSO), ethanol, and water. Its half-life is about 100 minutes, significantly longer than natural somatostatin (only 1-3 minutes), therefore it has more long-lasting pharmacological effects. This substance inhibits the secretion of various hormones by binding to ST receptors widely distributed in the central nervous system, pituitary gland, pancreatic beta cells, and other parts. Octreotide acetate has a threefold inhibitory effect on GH compared to natural somatostatin, and can significantly reduce GH and insulin-like growth factor-1 (IGF-1) levels in patients with acromegaly.
Our product Form
Octreotide Acetate COA
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| Certificate of Analysis | ||
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| Grade | Pharmaceutical grade | |
| CAS No. | 83150-76-9 | |
| Quantity | 15g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090054 | |
| MFG | Jan 9th 2025 | |
| EXP | Jan 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.46% |
| Loss on drying | ≤1.0% | 0.54% |
| 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% | 99.90% |
| Single impurity | <0.8% | 0.26% |
| Total microbial count | ≤750cfu/g | 70 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula: | C49H66N10O10S2 |
| Exact Mass: | 1018.44 |
| Molecular Weight: | 1019.25 |
| m/z: | 1018.44 (100.0%), 1019.44 (53.0%), 1020.45 (13.8%), 1020.44 (9.0%), 1021.44 (4.8%), 1019.44 (3.7%), 1020.44 (2.1%), 1020.44 (2.0%), 1019.44 (1.6%), 1021.45 (1.5%), 1022.44 (1.2%), 1021.45 (1.1%) |
| Elemental Analysis: | C, 57.74; H, 6.53; N, 13.74; O, 15.70; S, 6.29 |
Octreotide Acetate Injection is an artificially synthesized octapeptide derivative with a chemical structure similar to natural somatostatin, but enhanced stability and biological activity through optimization. As a somatostatin analogue, it plays a crucial role in multiple therapeutic fields by specifically binding to the somatostatin receptor (ST receptor), inhibiting the secretion of various hormones.
Pharmacological Action
Octreotide Acetate is an artificially synthesized octapeptide derivative with a chemical structure similar to natural somatostatin, but with stronger and more persistent effects. It exerts various pharmacological effects by binding to somatostatin receptors in the pituitary gland and gastrointestinal tract:
Inhibition of growth hormone secretion:
Directly inhibits the secretion of GH by pituitary GH tumor cells and reduces blood GH levels.
Inhibit the secretion of gastrointestinal and pancreatic endocrine hormones:
Reduce the secretion of hormones such as gastrin, vasoactive intestinal peptide (VIP), and glucagon, thereby alleviating related symptoms.
Inhibiting visceral blood flow:
Reducing visceral vascular resistance and decreasing visceral blood flow can help control esophageal and gastric variceal bleeding.
Inhibition of cell proliferation:
It has anti proliferative effects on certain tumor cells.
Acromegaly
Main treatment objectives
The main objectives of Octreotide Acetate in the treatment of acromegaly include:
Control symptoms: Relieve symptoms such as headache, joint pain, excessive sweating, and skin thickening caused by excessive secretion of GH.
Reduce GH and IGF-1 levels: Lower blood GH levels to the normal range (usually<2.5 ng/mL) and restore insulin-like growth factor-1 (IGF-1) levels to normal to reduce the risk of complications.
Reducing tumor volume: Some patients' tumor volume can be reduced, which is beneficial for subsequent surgical treatment or radiation therapy.
Improving quality of life: By controlling symptoms and reducing the risk of complications, we aim to enhance the quality of life for patients.
As a first-line drug treatment: Octreotide Acetate can be used as a first-line drug treatment for patients with mild to moderate acromegaly or those at high surgical risk. Long term subcutaneous injection or monthly administration of long-acting formulations such as Sandostatin LAR can effectively control GH and IGF-1 levels.
Preoperative pre-treatment: For patients with large tumor volume or severe complications such as sleep apnea syndrome and heart failure, preoperative use of Octreotide Acetate can reduce tumor volume, improve symptoms, and lower surgical risks. Preoperative pre-treatment usually lasts for several weeks to months, and surgery is performed only after GH and IGF-1 levels have decreased to a safe range.
Postoperative adjuvant therapy: For patients whose postoperative GH levels do not meet the standard, Octreotide Acetate Injection can be used as an adjuvant therapy to further reduce GH and IGF-1 levels. Postoperative adjuvant therapy is usually continued until GH and IGF-1 levels stabilize and reach the standard or the patient receives other treatments (such as radiation therapy).
Combined application with radiation therapy: Radiation therapy takes effect slowly, and Octreotide Acetate can be used to control symptoms during this period. The combination of the two can improve treatment efficacy and reduce the risk of complications.
Long term maintenance therapy: Octreotide acetate can be used as a long-term maintenance therapy to control symptoms and reduce the risk of complications for patients who are unable to undergo surgery or radiation therapy is ineffective. Long term maintenance therapy requires regular monitoring of GH and IGF-1 levels, as well as evaluation of adverse drug reactions.
Therapeutic effect and evidence support
Reduce GH and IGF-1 levels
Multiple clinical studies have confirmed that Octreotide Acetate can significantly reduce GH and IGF-1 levels in patients with acromegaly. For example, a clinical study involving over 100 patients showed that after treatment with Octreotide Acetate, approximately 60% to 70% of patients had their GH levels reduced to the normal range and IGF-1 levels significantly decreased.
Reduce tumor volume
Some patients may experience a reduction in tumor volume after using Octreotide Acetate. A study shows that after long-term treatment, about 30% to 40% of patients' tumor volume shrinks by more than 20%. The reduction of tumor volume is beneficial for subsequent surgical or radiation therapy.
Improve symptoms and quality of life
Octreotide acetate can significantly alleviate symptoms such as headache, joint pain, and excessive sweating in patients with acromegaly, and improve their quality of life. A quality of life assessment study showed that patients' quality of life scores significantly improved after treatment.
Long term efficacy and safety
Long term follow-up studies have shown that Octreotide Acetate has sustained efficacy in controlling GH and IGF-1 levels, with relatively mild adverse reactions. Common adverse reactions include injection site pain, diarrhea, bloating, etc., which most patients can tolerate. Long term use requires monitoring of potential adverse reactions such as blood glucose, thyroid function, and gallstones formation.
Frequently Asked Questions
What are the key defects of natural somatostatin solved by the design of "D-amino acid" and "cyclization" in its structure?
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Introducing D-type amino acids (such as D-phenylalanine) can resist degradation by various proteases in the body; By intramolecular cyclization (via disulfide bonds), its spatial conformation is fixed, significantly improving its affinity and selectivity for somatostatin receptors. Both together extend its half-life from 2-3 minutes to approximately 100 minutes.
Why does its injection require the use of an "acetic acid" buffer system, and what is the special significance of this for the stability of peptide drugs?
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Acetic acid provides a weakly acidic buffer environment, which can inhibit the hydrolysis and oxidation of peptides, as well as prevent unnecessary aggregation or precipitation of octreotide acetate molecules. In addition, the acetate octreotide salt formed between acetate and drugs helps to enhance its long-term stability in freeze-drying or solution state.
What is the difference between the mechanism of controlling symptoms (such as necrotic erythema) and inhibiting tumor growth in the treatment of "glucagonoma"?
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The control of symptoms such as rash mainly relies on its strong inhibition of glucagon secretion, thereby reducing blood amino acid levels and skin damage. The inhibition of tumor growth relies on its direct activation of somatostatin receptors on tumor cells, inducing apoptosis through the mitochondrial pathway, which is a relatively independent effect.
What are the core technical challenges of its "long-acting sustained-release microsphere" formulation (Shanlong)?
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The core lies in controllable microsphere degradation and drug release. Microspheres are made of biodegradable polylactic acid hydroxyacetic acid copolymers, and their molecular weight, crystallinity, etc. need to be precisely controlled to ensure that the drug is released at a nearly constant rate within one month, and to avoid "burst release effects" or insufficient release in the later stage.
Why is it necessary to check the clarity of the medication before use, and what may be the possible reasons for the formation of "mist" or "particles"?
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The polypeptide chain of octreotide may undergo conformational changes or aggregation due to shaking, temperature changes, or contact with certain surfaces, forming sub visible or visible particles. This not only affects the accuracy of dosage, but also increases the risk of thrombosis or immune response after injection into the blood vessel, so it must be visually examined to ensure complete clarity and transparency.
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