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药品详细

Vapreotide(伐普肽)

化学结构式图
中文名
伐普肽
英文名
Vapreotide
分子式
C57H70N12O9S2
化学名
2-amino-N-[10-(4-aminobutyl)-4-{[1-carbamoyl-2-(1H-indol-2-yl)ethyl]carbamoyl}-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-(propan-2-yl)-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-19-yl]-3-phenylpropanamide
分子量
Average: 1131.371
Monoisotopic: 1130.483013278
CAS号
103222-11-3
ATC分类
H01C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Vapreotide is a synthetic octapeptide somatostatin analog. It was being studied for the treatment of cancer.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Sarr MG: The potent somatostatin analogue vapreotide does not decrease pancreas-specific complications after elective pancreatectomy: a prospective, multicenter, double-blinded, randomized, placebo-controlled trial. J Am Coll Surg. 2003 Apr;196(4):556-64; discussion 564-5; author reply 565. Pubmed
    2. Vapreotide: BMY 41606, RC 160, Sanvar. Drugs R D. 2003;4(5):326-30. Pubmed
    3. Norman P: Vapreotide (Debipharm). IDrugs. 2000 Nov;3(11):1358-72. Pubmed
    4. Betoin F, Ardid D, Herbet A, Aumaitre O, Kemeny JL, Duchene-Marullaz P, Lavarenne J, Eschalier A: Evidence for a central long-lasting antinociceptive effect of vapreotide, an analog of somatostatin, involving an opioidergic mechanism. J Pharmacol Exp Ther. 1994 Apr;269(1):7-14. Pubmed
    5. Girard PM, Goldschmidt E, Vittecoq D, Massip P, Gastiaburu J, Meyohas MC, Coulaud JP, Schally AV: Vapreotide, a somatostatin analogue, in cryptosporidiosis and other AIDS-related diarrhoeal diseases. AIDS. 1992 Jul;6(7):715-8. Pubmed
    6. Stiefel F, Morant R: Vapreotide, a new somatostatin analogue in the palliative management of obstructive ileus in advanced cancer. Support Care Cancer. 1993 Jan;1(1):57-8. Pubmed
    7. Betoin F, Eschalier A, Duchene-Marullaz P, Lavarenne J: Seven-day antinociceptive effect of a sustained release vapreotide formulation. Neuroreport. 1994 Jan 31;5(5):642-4. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Polypeptides
    • Tryptamines and Derivatives
    • Lactams
    Substructures
    • Polypeptides
    • Hydroxy Compounds
    • Indoles and Indole Derivatives
    • Phenols and Derivatives
    • Amino Ketones
    • Pyrroles
    • Aliphatic and Aryl Amines
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Organic Disulfides
    • Tryptamines and Derivatives
    • Carbamates and Derivatives
    • Phenethylamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Phenylpropylamines
    • Lactams
    • Phenyl Esters
    • Amphetamines
    适应症
    药理
    Indication For the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and has also shown efficacy in the treatment of patients with AIDS-related diarrhea.
    Pharmacodynamics Vapreotide is a somatostatin analog with a higher metabolic stability than the parent hormone. Vapreotide reduces splanchnic blood flow; inhibits growth hormone release, and inhibits the release of peptides and vasoactive compounds from neuroendocrine tumors.
    Mechanism of action The exact mechanism of action is unknown, although one study has provided in vitro and in vivo evidence for a tachykinin NK1 receptor antagonist effect in the analgesic effects of vapreotide (PMID: 7556407).
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Vapreotide is 76% eliminated in bile. The remainder is renally eliminated.
    Half life 30 minutes
    Clearance Not Available
    Toxicity Safety data are limited, however, headache, fatigue, diarrhea, nausea, vomiting, and abdominal pain have been reported commonly with the use of vapreotide.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 3.99e-03 g/l ALOGPS
    logP 2.7 ALOGPS
    logP 0.76 ChemAxon
    logS -5.5 ALOGPS
    pKa (strongest acidic) 9.43 ChemAxon
    pKa (strongest basic) 10.26 ChemAxon
    physiological charge 2 ChemAxon
    hydrogen acceptor count 11 ChemAxon
    hydrogen donor count 13 ChemAxon
    polar surface area 350.64 ChemAxon
    rotatable bond count 18 ChemAxon
    refractivity 306.2 ChemAxon
    polarizability 118.82 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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