 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 265121-04-8 |
| Molecular formula(MF) | C23H22F7N4O6P.2C7H17NO5 |
| Molecular Weight(MW): | 1004.83 |
| Alias |
| In vitro | DMSO | 201 mg/mL (200.03 mM) |
|---|---|---|
| Water | 135 mg/mL (134.35 mM) | |
| Ethanol | <1 mg/mL | |
| In vivo |
| Description | Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. | |
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| Targets |
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| 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] |
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| 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] |