Fosaprepitant dimeglumine

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MedKoo CAT#: 205461

CAS#: 265121-04-8 (dimeglumine)

Description: Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4.

Chemical Structure

Fosaprepitant dimeglumine
CAS# 265121-04-8 (dimeglumine)

Theoretical Analysis

MedKoo Cat#: 205461
Name: Fosaprepitant dimeglumine
CAS#: 265121-04-8 (dimeglumine)
Chemical Formula: C37H56F7N6O16P
Exact Mass:
Molecular Weight: 1004.84
Elemental Analysis: C, 44.23; H, 5.62; F, 13.23; N, 8.36; O, 25.48; P, 3.08

Price and Availability

Size Price Availability Quantity
200.0mg USD 165.0 Same day
500.0mg USD 350.0 Same day
1.0g USD 585.0 Same day
2.0g USD 1050.0 Same day
5.0g USD 2250.0 Same day
10.0g USD 3850.0 Same day
20.0g USD 6850.0 2 weeks
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Related CAS #: 265121-04-8 (dimeglumine)   172673-20-0 (free acid)  

Synonym: MK0517; MK 0517; MK-0517; Fosaprepitant; Fosaprepitant dimeglumine; Emend; Inemend.

IUPAC/Chemical Name: (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol hemi((3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonate)


InChi Code: InChI=1S/C23H22F7N4O6P.2C7H17NO5/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;2*1-8-2-4(10)6(12)7(13)5(11)3-9/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38);2*4-13H,2-3H2,1H3/t12-,19+,20-;2*4-,5+,6+,7+/m100/s1

SMILES Code: O=C(N1)N(P(O)(O)=O)N=C1CN2CCO[C@H](O[C@H](C)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)[C@@H]2C4=CC=C(F)C=C4.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO or water

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 1004.84 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Grunberg S, Chua D, Maru A, Dinis J, DeVandry S, Boice JA, Hardwick JS, Beckford E, Taylor A, Carides A, Roila F, Herrstedt J. Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with cisplatin therapy: randomized, double-blind study protocol--EASE. J Clin Oncol. 2011 Apr 10;29(11):1495-501. Epub 2011 Mar 7. PubMed PMID: 21383291.

2: Marbury TC, Ngo PL, Shadle CR, Jin B, Panebianco D, Caro L, Valentine J, Murphy G. Pharmacokinetics of Oral Dexamethasone and Midazolam When Administered With Single-Dose Intravenous 150 mg Fosaprepitant in Healthy Adult Subjects. J Clin Pharmacol. 2011 Jan 5. [Epub ahead of print] PubMed PMID: 21209230.

3: Langford P, Chrisp P. Fosaprepitant and aprepitant: an update of the evidence for their place in the prevention of chemotherapy-induced nausea and vomiting. Core Evid. 2010 Oct 21;5:77-90. PubMed PMID: 21042544; PubMed Central PMCID: PMC2963924.

4: Colon-Gonzalez F, Kraft WK. Pharmacokinetic evaluation of fosaprepitant dimeglumine. Expert Opin Drug Metab Toxicol. 2010 Oct;6(10):1277-86. Review. PubMed PMID: 20795794; PubMed Central PMCID: PMC3155701.

5: Marbury TC, Jin B, Panebianco D, Murphy MG, Sun H, Evans JK, Han TH, Constanzer ML, Dru J, Shadle CR. Lack of effect of aprepitant or its prodrug fosaprepitant on QTc intervals in healthy subjects. Anesth Analg. 2009 Aug;109(2):418-25. PubMed PMID: 19608812.

6: Van Belle SJ, Cocquyt V. Fosaprepitant dimeglumine (MK-0517 or L-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting. Expert Opin Pharmacother. 2008 Dec;9(18):3261-70. Review. PubMed PMID: 19040346.

7: Navari RM. Fosaprepitant: a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Expert Rev Anticancer Ther. 2008 Nov;8(11):1733-42. Review. PubMed PMID: 18983233.

8: Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6. PubMed PMID: 18728837; PubMed Central PMCID: PMC2504061.

9: Navari RM. Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Expert Opin Investig Drugs. 2007 Dec;16(12):1977-85. Review. PubMed PMID: 18042005.

10: Lasseter KC, Gambale J, Jin B, Bergman A, Constanzer M, Dru J, Han TH, Majumdar A, Evans JK, Murphy MG. Tolerability of fosaprepitant and bioequivalency to aprepitant in healthy subjects. J Clin Pharmacol. 2007 Jul;47(7):834-40. Epub 2007 May 24. PubMed PMID: 17525168.

Additional Information

Related CAS#
CAS# 265121-04-8 (Fosaprepitant dimeglumine salt);
CAS#172673-20-0 (Fosaprepitant)