Fosaprepitant dimeglumine - CAS 172673-20-0
Catalog number: 172673-20-0
Category: Inhibitor
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Molecular Formula:
C23H22F7N4O6P
Molecular Weight:
614.414
COA:
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Targets:
Neurokinin Receptor
Description:
Fosaprepitant (L-758298) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
Purity:
>98%
Appearance:
white solid powder
Synonyms:
Fosaprepitant; Fosaprepitant dimeglumine, Emend; Inemend. UNII-D35FM8T64X; MK-0517; MK 0517; MK0517.
MSDS:
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InChIKey:
BARDROPHSZEBKC-OITMNORJSA-N
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
Canonical SMILES:
CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)N(N3)P(=O)(O)O)C4=CC=C(C=C4)F
1.Infusion site adverse events in breast cancer patients receiving highly emetic chemotherapy with prophylactic anti-emetic treatment with aprepitant and fosaprepitant: A retrospective comparison.
Tsuda T1, Kyomori C2, Mizukami T1, Taniyama T1, Izawa N1, Horie Y1, Hirakawa M1, Ogura T1, Nakajima TE1, Tsugawa K3, Boku N1. Mol Clin Oncol. 2016 Apr;4(4):603-606. Epub 2016 Feb 5.
The incidences of infusion site adverse events in chemotherapy regimens, including anthracyclines with either fosaprepitant or aprepitant as the anti-emetic, were not highlighted in the randomized trial comparing aprepitant and fosaprepitant. The present retrospective analysis was performed in breast cancer patients receiving anthracycline-containing chemotherapy, a combination of epirubicin and cyclophosphamide with or without 5-fluorouracil as the adjuvant or neoadjuvant, at the outpatient infusion center of St. Marianna University Hospital (Kawasaki, Japan). Infusion site adverse events were retrospectively compared between the 3 months prior to and three months following switching from 3 day oral administration of aprepitant to intravenous infusion of fosaprepitant. A total of 62 patients were included in the aprepitant group and 38 in the fosaprepitant group. Of these patients, 26 (42%) in the aprepitant group and 36 patients (96%) in the fosaprepitant group experienced any grade of infusion site adverse events at least once (P<0.
2.Phase II study of fosaprepitant + 5HT3 receptor antagonist + dexamethasone in patients with germ cell tumors undergoing 5-day cisplatin-based chemotherapy: a Hoosier Cancer Research Network study.
Adra N1, Albany C2, Brames MJ2, Case-Eads S2, Johnson CS3, Liu Z3, Fausel CA2, Breen T4, Hanna NH2, Hauke RJ5, Picus J6, Einhorn LH2. Support Care Cancer. 2016 Feb 2. [Epub ahead of print]
PURPOSE: A phase III study adding aprepitant to a 5HT3 receptor antagonist (5HT3-RA) plus dexamethasone in germ cell tumor (GCT) patients treated with 5-day cisplatin combination chemotherapy demonstrated a significant improvement in complete response (CR) (J Clin Onc 30:3998-4003, 2012). Fosaprepitant has demonstrated non-inferiority compared to aprepitant in single-day cisplatin chemotherapy and is approved as a single-dose alternative. This single-arm phase II study is the first clinical trial evaluating fosaprepitant in patients receiving multi-day cisplatin regimen.
3.Drug interactions with aprepitant or fosaprepitant: Review of literature and implications for clinical practice.
Dushenkov A1, Kalabalik J2, Carbone A2, Jungsuwadee P2. J Oncol Pharm Pract. 2016 Feb 25. pii: 1078155216631408. [Epub ahead of print]
PURPOSE: Aprepitant and its parenteral formulation fosaprepitant are widely used for the prevention of chemotherapy-induced nausea and vomiting. Aprepitant exerts modest inhibitory effect on CYP3A4 and modest inductive effect on CYP2C9 substrates such as some antineoplastics and multiple other medications. This article is aimed to provide pharmacists and other healthcare professionals with an updated summary of drug-drug interactions of aprepitant/fosaprepitant and implications for clinical practice.
4.Drug interactions with aprepitant or fosaprepitant: Review of literature and implications for clinical practice.
Dushenkov A1, Kalabalik J2, Carbone A2, Jungsuwadee P2. J Oncol Pharm Pract. 2016 Feb 25. pii: 1078155216631408. [Epub ahead of print]
PURPOSE: Aprepitant and its parenteral formulation fosaprepitant are widely used for the prevention of chemotherapy-induced nausea and vomiting. Aprepitant exerts modest inhibitory effect on CYP3A4 and modest inductive effect on CYP2C9 substrates such as some antineoplastics and multiple other medications. This article is aimed to provide pharmacists and other healthcare professionals with an updated summary of drug-drug interactions of aprepitant/fosaprepitant and implications for clinical practice.
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CAS 172673-20-0 Fosaprepitant dimeglumine

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