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GPCR/G ProteinNeuronal Signaling-
Fosaprepitant(L-758298)???????????????-1?????????????????????????????????????????????????????????????????????
相关产品
Aprepitant-Maropitant-Fosaprepitant dimeglumine-Netupitant-Talnetant-NKP608-SB-222200-Rolapitant-Substance P-Befetupitant-Fezolinetant-Hemokinin 1 mouse-Kassinin-MEN11467-Neurokinin A-
生物活性
Description
Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.IC50 Value:Target: NK1 receptorin vitro: Fosaprepitant (also known as MK-0517 and L-758,298) is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min of intravenous administration via the action of ubiquitous phosphatases. Owing to the rapid conversion offosaprepitant to the active form (aprepitant), fosaprepitant 115 mg provided the same aprepitant exposure in terms of AUC as aprepitant 12 mg orally, and fosaprepitant is expected to provide a correspondingly similar antiemetic effect as aprepitant [1]. in vivo: Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate [2]. Patients receiving cisplatin ??? 70 mg/m(2) for the first time received ondansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80 mg on day 3) or a single-dose fosaprepitant regimen (150 mg on day 1) [3]. Single-dose fosaprepitant used in combination with granisetron and dexamethasone was well-tolerated and effective in preventing chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic cancer chemotherapy, including high-dose cisplatin [4].
Clinical Trial
St. Louis University-Merck Sharp & Dohme Corp.
Chemotherapy-induced Nausea and Vomiting
September 2013
Phase 2
Ajeet Gajra-Merck Sharp & Dohme Corp.-State University of New York - Upstate Medical University
Non-small Cell Lung Cancer-Vomiting-Nausea-Emesis
April 2015
Phase 2
Stanford University
Postoperative Nausea
August 1, 2017
Phase 4
Lawrence Einhorn-Hoosier Cancer Research Network-Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting
January 2013
Phase 2
Merck Sharp & Dohme Corp.
Nausea-Vomiting
October 2011
Phase 2
Merck Sharp & Dohme Corp.
Chemotherapy-induced Nausea and Vomiting
September 2015
Phase 3
Gynecologic Oncology Associates-Merck Sharp & Dohme Corp.
Ovarian Cancer-Uterine Cancer
September 2011
Phase 4
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting
February 2009
Phase 1
Multicenter Clinical Study Group of Osaka, Colorectal Cancer Treatment Group
Colorectal Cancer
April 2011
Philip Philip-National Cancer Institute (NCI)-Barbara Ann Karmanos Cancer Institute
Gastrointestinal Cancer-Nausea Post Chemotherapy
June 2012
OHSU Knight Cancer Institute-National Cancer Institute (NCI)
Breakthrough Nausea and Vomiting-Unspecified Adult Solid Tumor, Protocol Specific
August 2008
Phase 1-Phase 2
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting (CINV)
September 2012
Phase 3
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting
February 5, 2009
Phase 1
Odense University Hospital-Helsinn Healthcare SA
Nausea-Vomiting-Genital Neoplasms, Female
April 2010
Phase 3
M.D. Anderson Cancer Center-Merck Sharp & Dohme Corp.
Sarcoma-Chemotherapy-induced Nausea and Vomiting-Effects of Chemotherapy-Adverse Effects of Medical Drugs
May 2012
Merck Sharp & Dohme Corp.
Chemotherapy-induced Nausea and Vomiting
December 13, 2012
Phase 2
University of Southern California-National Cancer Institute (NCI)
Breast Cancer-Nausea-Vomiting
September 4, 2012
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting (CINV)
April 2010
Phase 1
University of Washington-National Cancer Institute (NCI)
Nausea and Vomiting-Stage III Squamous Cell Carcinoma of the Hypopharynx-Stage III Squamous Cell Carcinoma of the Larynx-Stage III Squamous Cell Carcinoma of the Lip and Oral Cavity-Stage III Squamous Cell Carcinoma of the Nasopharynx-Stage III Squamous Cell Carcinoma of the Oropharynx-Stage IV Squamous Cell Carcinoma of the Hypopharynx-Stage IV Squamous Cell Carcinoma of the Larynx-Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity-Stage IV Squamous Cell Carcinoma of the Nasopharynx-St
February 2009
Phase 2
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting (CINV)
February 2008
Phase 3
Arun Gupta-Cambridge University Hospitals NHS Foundation Trust-University of Cambridge
Traumatic Brain Injury
September 2017
Early Phase 1
Heron Therapeutics
Chemotherapy-induced Nausea and Vomiting
March 2014
Phase 3
M.D. Anderson Cancer Center-Tesaro, Inc.
Sarcoma
October 2016
Phase 2
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting
January 1, 2007
Phase 3
Acacia Pharma Ltd
CINV
October 2013
Phase 2
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Hematopoietic/Lymphoid Cancer-Nausea and Vomiting-Unspecified Adult Solid Tumor, Protocol Specific
August 2014
Phase 3
Merck Sharp & Dohme Corp.
Chemotherapy-Induced Nausea and Vomiting-Postoperative Nausea and Vomiting
January 2005
Phase 1
Merck Sharp & Dohme Corp.
Post-Operative Nausea and Vomiting
July 2005
Phase 3
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