Fosaprepitant (BioDeep_00000033374)

   

human metabolite blood metabolite Chemicals and Drugs


代谢物信息卡片


(3-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid

化学式: C23H22F7N4O6P (614.1165)
中文名称: 福沙吡坦
谱图信息: 最多检出来源 not specific(not specific) 0%

分子结构信息

SMILES: CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NN(C(=O)N3)P(=O)(O)O)C4=CC=C(C=C4)F
InChI: InChI=1S/C23H22F7N4O6P/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)40-20-19(13-2-4-17(24)5-3-13)33(6-7-39-20)11-18-31-21(35)34(32-18)41(36,37)38/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38)/t12-,19+,20-/m1/s1

描述信息

Fosaprepitant is only found in individuals that have used or taken this drug. It is an intravenously administered antiemetic drug. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment.Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.In summary, the active form of fosaprepitant is as an NK1 antagonist which is because it blocks signals given off by NK1 receptors. This therefore decreases the likelihood of vomiting in patients experiencing.
D018377 - Neurotransmitter Agents > D064729 - Neurokinin-1 Receptor Antagonists
D018373 - Peripheral Nervous System Agents > D001337 - Autonomic Agents
C78272 - Agent Affecting Nervous System > C267 - Antiemetic Agent
D005765 - Gastrointestinal Agents > D000932 - Antiemetics
D002491 - Central Nervous System Agents

同义名列表

7 个代谢物同义名

(3-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid; Fosaprepitant dimeglumine; Emend for injection; Fosaprepitantum; Fosaprepitant; L-758,298; L-758298



数据库引用编号

9 个数据库交叉引用编号

分类词条

相关代谢途径

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代谢反应

0 个相关的代谢反应过程信息。

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1 个相关的物种来源信息

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

  • PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

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亚细胞结构定位 关联基因列表


文献列表

  • Fei Xue, Xin Liu, Xiao Qi, Jiajing Zhou, Yongjun Liu. The clinical research study for fosaprepitant to prevent chemotherapy-induced nausea and vomiting: A review. Advances in clinical and experimental medicine : official organ Wroclaw Medical University. 2023 Jun; 32(6):701-706. doi: 10.17219/acem/157061. [PMID: 37026971]
  • Jill N Modi, Sarah K Cimino. Incidence of ifosfamide induced encephalopathy in patients receiving concomitant fosaprepitant. Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners. 2021 Dec; 27(8):1891-1895. doi: 10.1177/1078155220971794. [PMID: 33166244]
  • Kang Lu, Sisi Lin, Yannan Wang, Rui Hao, Lu Fang, Jingjing Zhu, Di Zhao, Jin Yu, Shengjia Tong, Yi Wu, Yongkai Si, Tiantian Ye, Qigang Yang, Ying Wang. Pharmacokinetics and Safety of Fosaprepitant Dimeglumine in Healthy Chinese Volunteers: Bioequivalence Study. Clinical pharmacology in drug development. 2021 07; 10(7):748-755. doi: 10.1002/cpdd.892. [PMID: 33277980]
  • Tom Ottoboni, Mary Rose Keller, Matt Cravets, Neil Clendeninn, Barry Quart. Bioequivalence of HTX-019 (aprepitant IV) and fosaprepitant in healthy subjects: a Phase I, open-label, randomized, two-way crossover evaluation. Drug design, development and therapy. 2018; 12(?):429-435. doi: 10.2147/dddt.s155875. [PMID: 29535504]
  • K Van Laere, J De Hoon, G Bormans, M Koole, I Derdelinckx, I De Lepeleire, R Declercq, S M Sanabria Bohorquez, T Hamill, P D Mozley, D Tatosian, W Xie, Y Liu, F Liu, P Zappacosta, C Mahon, K L Butterfield, L B Rosen, M G Murphy, R J Hargreaves, J A Wagner, C R Shadle. Equivalent dynamic human brain NK1-receptor occupancy following single-dose i.v. fosaprepitant vs. oral aprepitant as assessed by PET imaging. Clinical pharmacology and therapeutics. 2012 Aug; 92(2):243-50. doi: 10.1038/clpt.2012.62. [PMID: 22739139]
  • Thomas C Marbury, Phung L Ngo, Craig R Shadle, Bo Jin, Deborah Panebianco, Luzelena Caro, Jack Valentine, Gail Murphy. Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects. Journal of clinical pharmacology. 2011 Dec; 51(12):1712-20. doi: 10.1177/0091270010387792. [PMID: 21209230]
  • Thomas C Marbury, Bo Jin, Deborah Panebianco, M Gail Murphy, Hong Sun, Judith K Evans, Tae H Han, Marvin L Constanzer, James Dru, Craig R Shadle. Lack of effect of aprepitant or its prodrug fosaprepitant on QTc intervals in healthy subjects. Anesthesia and analgesia. 2009 Aug; 109(2):418-25. doi: 10.1213/ane.0b013e3181ac1066. [PMID: 19608812]
  • Ian N Olver. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Therapeutics and clinical risk management. 2008 Apr; 4(2):501-6. doi: 10.2147/tcrm.s2345. [PMID: 18728837]
  • Kenneth C Lasseter, Jay Gambale, Bo Jin, Art Bergman, Marvin Constanzer, James Dru, Tae H Han, Anup Majumdar, Judith K Evans, M Gail Murphy. Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects. Journal of clinical pharmacology. 2007 Jul; 47(7):834-40. doi: 10.1177/0091270007301800. [PMID: 17525168]
  • J J Hale, S G Mills, M MacCoss, C P Dorn, P E Finke, R J Budhu, R A Reamer, S E Huskey, D Luffer-Atlas, B J Dean, E M McGowan, W P Feeney, S H Chiu, M A Cascieri, G G Chicchi, M M Kurtz, S Sadowski, E Ber, F D Tattersall, N M Rupniak, A R Williams, W Rycroft, R Hargreaves, J M Metzger, D E MacIntyre. Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs. Journal of medicinal chemistry. 2000 Mar; 43(6):1234-41. doi: 10.1021/jm990617v. [PMID: 10737756]