Fosaprepitant dimeglumine salt

Catalog No.S3038 Synonyms: MK-0517

Fosaprepitant dimeglumine salt Chemical Structure

Molecular Weight(MW): 1004.83

Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.

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Biological Activity

Description Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
Targets
NK-1 receptor [1]
In vitro

Fosaprepitant (MK-0517, L-758,298) is a phosphoryl prodrug for aprepitant. Aprepitant is a selective substance P (NK-1 receptor) antagonist approved as part of combination therapy with a corticosteroid and a 5-HT 3 receptor antagonist for the prevention of acute and delayed Chemotherapy-induced nausea and vomiting. [1]

In vivo Fosaprepitant is converted to aprepitant within 30 min after intravenous administration via the action of ubiquitous phosphatases when administered intravenously. Fosaprepitant is well tolerated up to 150 mg (1 mg/ml), and Fosaprepitant 115 mg is bioequivalent in its AUC to aprepitant 125 mg. Fosaprepitant 115 mg has been submitted for FDA approval as an alternative on day 1 of a 3-day oral aprepitant regimen, with oral aprepitant administered on days 2 and 3. [1]

Protocol

Solubility (25°C)

In vitro DMSO 201 mg/mL (200.03 mM)
Water 135 mg/mL (134.35 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1004.83
Formula

C23H22F7N4O6P.2C7H17NO5

CAS No. 265121-04-8
Storage powder
in solvent
Synonyms MK-0517

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03035838 Not yet recruiting Traumatic Brain Injury Arun Gupta|Cambridge University Hospitals NHS Foundation Trust|University of Cambridge October 2019 Early Phase 1
NCT03035838 Not yet recruiting Traumatic Brain Injury Arun Gupta|Cambridge University Hospitals NHS Foundation Trust|University of Cambridge October 2019 Early Phase 1
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03578081 Recruiting Malignant Neoplasm Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) October 15 2018 Phase 3
NCT03578081 Recruiting Malignant Neoplasm Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) October 15 2018 Phase 3

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