Lanreotide powder is a peptide drug with the chemical name N - [(1S) -1- [(2S, 3R) -3- (1-Carboxy-2-phenylethyl) -2-methyloxiran-2-yl] methyl] -3- (phenylmethod) propyl] - D tryptophanamide. The molecular formula is C38H48N4O7S, CAS 108736-35-2, and the molecular weight is 680.86. It is a white to grayish white powder, odorless. The solubility in water is low, but it has good solubility in organic solvents such as methanol and ethanol. It requires multiple chemical reactions, including protection, deprotection, condensation, and other reaction steps. During the synthesis process, it is necessary to strictly control the reaction conditions, such as temperature, pH value, reaction time, etc., to ensure the purity and yield of the final product. It is a growth hormone analogue with multiple uses, playing an important role in the treatment of diseases such as acromegaly, carcinoid syndrome, pancreatic endocrine tumors, gastroesophageal reflux disease, and pancreatic cystic fibrosis. When using lalotudine, it is important to follow the doctor's advice and undergo regular monitoring to ensure the effectiveness and safety of the medication. Please note that the products produced by Shaanxi BLOOM Tech Co., Ltd. are primary chemicals and cannot be used for clinical medical purposes.
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Customized Bottle Caps And Corks:
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Chemical Formula |
C54H69N11O10S2 |
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Exact Mass |
1095 |
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Molecular Weight |
1096 |
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m/z |
1095 (100.0%), 1096 (58.4%), 1097 (16.7%), 1097 (9.0%), 1098 (5.3%), 1096 (4.1%), 1098 (3.1%), 1097 (2.4%), 1097 (2.1%), 1096 (1.6%), 1099 (1.5%), 1098 (1.2%) |
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Elemental Analysis |
C, 59.16; H, 6.34; N, 14.05; O, 14.59; S, 5.85 |
Lanrelin is an artificially synthesized growth hormone inhibitor analogue, which exerts inhibitory effects on various hormones, including growth hormone, thyroid stimulating hormone (TSH), insulin, and glucagon. Lanrelin is similar to growth hormone inhibin and acts through receptors. It has a higher affinity for peripheral somatostatin receptors, similar activity, and weaker affinity for the central nervous system. Although growth hormone inhibin decomposes in the body within a few minutes, the attenuation period of Lanrelin is longer, resulting in a longer lasting effect.
Lanreotide powder is an artificially synthesized somatostatin analog with wide applications in the medical field, mainly used for the treatment of various endocrine diseases and tumors.
1. Treatment of acromegaly
Acromegaly is a rare chronic disease mainly caused by excessive secretion of growth hormone (GH) from the anterior pituitary gland. Patients often experience structural changes and endocrine metabolic disorders due to excessive secretion of GH and insulin-like growth factor-1 (IGF-1), which seriously affects their quality of life and lifespan. Lanrui peptide, as a somatostatin analogue, can effectively inhibit GH secretion, thereby improving patients' symptoms and quality of life.
Lanrui peptide is widely used in the treatment of acromegaly. For patients with active acromegaly, including those who have not reached normal serum GH levels after pituitary GH tumor surgery, and those who have not yet achieved sufficient therapeutic effect after external pituitary radiation therapy but still have elevated serum GH levels, lanrelitide is an effective therapeutic drug. It can alleviate symptoms such as headache, excessive sweating, fatigue, joint pain, etc. in patients by inhibiting GH secretion and reducing IGF-1 levels.
Cushing's syndrome is a clinical syndrome caused by long-term excessive secretion of glucocorticoids from the adrenal cortex due to various reasons, also known as endogenous Cushing's syndrome. Patients often experience symptoms such as central obesity, full moon face, appearance with multiple blood masses, purple lines, and hypertension. Lanrui peptide also has certain application value in the treatment of Cushing's syndrome.
Lanrui peptide can control the condition of Cushing's syndrome patients by inhibiting the secretion of adrenocorticotropic hormone (ACTH). For patients with Cushing's syndrome, the use of lanreotide can alleviate discomfort symptoms such as hypertension, obesity, and improve their quality of life.
Neuroendocrine tumors are a type of tumor that originates from neuroendocrine cells, including carcinoid tumors, pancreatic neuroendocrine tumors, etc. These tumors often secrete various hormones and bioactive substances, leading to a series of symptoms in patients. Lanrui peptide also has significant effects in the treatment of neuroendocrine tumors.
For patients with gastrointestinal neuroendocrine tumors and carcinoid syndrome, lanrelitide can alleviate symptoms such as severe diarrhea, flushing, electrolyte imbalance, and exudative polymorphic rash. Meanwhile, Lanrui peptide can also be used for the treatment of advanced, well differentiated or moderately differentiated, non functional, and growth hormone receptor positive neuroendocrine tumors, such as gastrointestinal and pancreatic neuroendocrine tumors.
Breast cancer is one of the most common malignant tumors in women, which poses a serious threat to women's life and health. Lanruitide also has certain application value in the adjuvant treatment of breast cancer. Although Lanruitide is not the main treatment drug for breast cancer, it can be used as an auxiliary treatment in some cases to help patients reduce symptoms and improve their quality of life.
For example, for postmenopausal patients with breast cancer, Lanruitide can selectively bind to gonadotropin releasing hormone receptor, block its signal transduction pathway with G-protein coupled receptor, reduce intracellular calcium concentration, inhibit cell division, induce tumor cell apoptosis, and thus play an anti-tumor role.
5. Other applications
(1) The treatment of rectal cancer: Lanrui peptide also has certain application value in the treatment of rectal cancer. Although the main treatment methods for rectal cancer are surgery and chemotherapy, lanrelitide can be used as an adjuvant therapy to help patients alleviate symptoms and improve their quality of life.
(2) Treatment of prostate cancer: Lanrui peptide can effectively inhibit prostate cell proliferation, thereby achieving the goal of reducing prostate volume. Therefore, it can be used as an adjuvant therapy for prostate cancer to help patients control the progression of the disease.
(3) Pain management: Lanrui peptide can reduce neuronal activity and alleviate pain by blocking the activity of nerve growth factors. This may be an effective treatment for some patients whose pain is difficult to control.
(4) Improvement of gastrointestinal symptoms: Lanrui peptide has the effect of promoting gastrointestinal motility, enhancing digestive and absorption functions, and helping to improve discomfort symptoms such as loss of appetite and bloating. This may be an effective adjuvant therapy for some patients with digestive diseases.
Amino acid protection: Properly protect the required amino acids to avoid unnecessary reactions during solid-phase synthesis. Common amino acid protecting groups include 9-fluoromethyl chloride (Fmoc), p-methoxybenzyl ester (Pbf), etc. These protective groups can effectively block certain reaction sites of amino acids during the reaction process, thereby controlling the specificity of the reaction.
Solid phase synthesis: Based on the amino acid sequence of Lanrelin, the protected amino acids are sequentially connected to the resin through solid-phase synthesis. In this process, it is necessary to select appropriate linking agents and coupling conditions to ensure that each amino acid can efficiently connect to the previous amino acid. Common linking agents include dichloromethane, dichloroquinoline, etc.
Solid phase synthesis by pyrolysis: After completion, the synthesized peptde needs to be cleaved from the resin. This process usually uses strong acid or strong base solutions to break the connection between amino acids and resin. After pyrolysis, the peptde needs to be purified to remove impurities and unreacted amino acids.
Linear peptide cyclization: After obtaining linear peptdes, they need to be cyclized with specific oxidants to obtain the cyclic structure of Lanrelin. Common oxidants include iodine oxidants, hydrogen peroxide oxidants, etc. This process needs to be carried out under specific pH and temperature conditions to ensure the efficiency of cyclization and the stability of the product.
Purification and crystallization: After cyclization, the peptde needs to be further purified to obtain high-purity blue ray peptde. The purification methods include gel filtration, ion exchange, etc. Crystallization is an important step in improving product purity and stability. By controlling crystallization conditions such as temperature, pH, concentration, etc., high-quality blue peptde crystals can be obtained.
Pharmacokinetics
The absorption kinetics of Lanrui peptide in healthy volunteers through intramuscular injection of the drug are characterized by rapid release in the first stage, which is the release of peptides bound to the surface of particles, followed by a slow decrease in the second stage of release. The first plasma peak (Cmax 1: 6.8 ± 3.8 μ g/L) was at 1.4 ± 0.8 hours, and the second peak (Cmax 2: 2.5 ± 0.9 μ g/L) was at 1.9 ± 1.8 days, with an absolute bioavailability of 46.1 ± 16.7%. The average retention time is 8.0 ± 1.0 days, and the surface half-life is 5.2 ± 2.5 days, which proves the sustained-release characteristics of the drug. For patients with acromegaly, there is a significant decrease in growth hormone and IGF-1 levels for at least 14 days after a single injection. Repeated medication for several months without any drug accumulation.
Frequently Asked Questions
What does the drug lanreotide do?
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Lanreotide injection is used to treat people with acromegaly (condition in which the body produces too much growth hormone, causing enlargement of the hands, feet, and facial features; joint pain; and other symptoms) who have not successfully, or cannot be treated with surgery or radiation.
Are lanreotide and octreotide the same?
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There are slight differences in FDA approval: octreotide (Sandostatin) is approved for symptoms of carcinoid/VIPoma syndrome and Lanreotide (Somatuline) is approved for tumor control.
What foods should you avoid while taking lanreotide?
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In addition, dietary changes may help. Avoid things that may worsen the symptoms, such as heavy or greasy/fatty, spicy, or acidic foods (lemons, tomatoes, oranges). Try antacids (such as milk of magnesia, calcium tablets such as Tums), saltines, or ginger ale to lessen symptoms.
How long can you stay on lanreotide?
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If you are having lanreotide to control the growth of your NET, you continue this for as long as it is working, and the side effects aren't too bad.
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