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药品详细

Pasireotide(帕瑞肽)

化学结构式图
中文名
帕瑞肽
英文名
Pasireotide
分子式
Not Available
化学名
分子量
Not Available
CAS号
396091-73-9
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

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor®, which is used in the treatment of Cushing’s disease.

生产厂家
    封装厂家
    参考
    Synthesis Reference

    Bruns C, Lewis I, Briner U, Meno-Tetang G, Weckbecker G: SOM230: a novel somatostatin peptidomimetic with broad somatotropin release inhibiting factor (SRIF) receptor binding and a unique antisecretory profile. Eur J Endocrinol. 2002 May;146(5):707-16.
    General Reference
    1. Weckbecker G, Briner U, Lewis I, Bruns C: SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology. 2002 Oct;143(10):4123-30. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of Cushing’s disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.
    Pharmacodynamics Signifor® is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.
    Mechanism of action Pasireotide activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.
    Absorption The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.
    Volume of distribution

    Pasireotide is widely distributed and has a volume of distribution of >100L.
    Protein binding Plasma protein binding is 88%.
    Metabolism
    Metabolism is minimal.
    Route of elimination Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).
    Half life The half-life is 12 hours.
    Clearance

    The clearance in healthy patient is ~7.6 L/h and in Cushing’s disease patients is ~3.8 L/h.
    Toxicity The most common toxic effects observed are hyperglycemia, cholelithiasis, diarrhea, nausea, headache, abdominal pain, fatigue, and diabetes mellitus.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    water solubility Soluble in water. From The Merck Index.
    Predicted Properties Not Available
    药物相互作用
    Drug Interaction
    Mifepristone Avoid combination with mifepristone and other moderate to high risk QTc prolonging agents. The combinaton may enhance the QTc-prolonging effect of these drugs.
    食物相互作用
    • Since Signifor® is administered subcutaneously, food has no effect.

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