CAS 265121-04-8|Fosaprepitant dimeglumine salt

Introduction：Basic information about CAS 265121-04-8|Fosaprepitant dimeglumine salt, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Fosaprepitant dimeglumine salt BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Fosaprepitant dimeglumine salt
CAS Number	265121-04-8	Molecular Weight	1004.83000
Density	/	Boiling Point	/
Molecular Formula	C₃₇H₅₆F₇N₆O₁₆P	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	fosaprepitant dimeglumine
Synonym	More Synonyms

Fosaprepitant dimeglumine salt BiologicalActivity

Description	Fosaprepitant dimeglumine(MK-0517) 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].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Neurokinin ReceptorSignaling Pathways >>Neuronal Signaling >>Neurokinin ReceptorResearch Areas >>Neurological Disease
References	[1]. 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. [2]. Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6. [3]. Grunberg S, et al. 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. [4]. Saito H, et al. Efficacy and safety of single-dose fosaprepitant in the prevention of chemotherapy-induced nausea and vomiting in patients receiving high-dose cisplatin: a multicentre, randomised, double-blind, placebo-controlled phase 3 trial. Ann Oncol. 2013 Apr;24(4):1067-73.

Description

Fosaprepitant dimeglumine(MK-0517) 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].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Neurokinin ReceptorSignaling Pathways >>Neuronal Signaling >>Neurokinin ReceptorResearch Areas >>Neurological Disease

References

[1]. 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.

[2]. Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6.

[3]. Grunberg S, et al. 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.

[4]. Saito H, et al. Efficacy and safety of single-dose fosaprepitant in the prevention of chemotherapy-induced nausea and vomiting in patients receiving high-dose cisplatin: a multicentre, randomised, double-blind, placebo-controlled phase 3 trial. Ann Oncol. 2013 Apr;24(4):1067-73.

Chemical & Physical Properties

Molecular Formula	C₃₇H₅₆F₇N₆O₁₆P
Molecular Weight	1004.83000
Exact Mass	1004.34000
PSA	366.08000
InChIKey	VRQHBYGYXDWZDL-OOZCZQCLSA-N
SMILES	CC(OC1OCCN(Cc2nn(P(=O)(O)O)c(=O)[nH]2)C1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1.CNCC(O)C(O)C(O)C(O)CO.CNCC(O)C(O)C(O)C(O)CO
Storage condition	-20°C

Safety Information

Hazard Codes	Xi

Synonyms

Ivemend

phosphonic acid, [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]-, compd. with D-glucitol, 1-deoxy-1-(m

acide (3-{[(2R,3S)-2-{(1R)-1-[3,5-bis(trifluorométhyl)phényl]éthoxy}-3-(4-fluorophényl)morpholin-4-yl]méthyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonique - (2R,3R,4R,5S)-6-(méthylamino)hexane

[5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-3-oxo-1H-1,2,4-triazol-2-yl]phosphonic acid,(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol

(3-{[(2R,3S)-2-{(1R)-1-[3,5-Bis(trifluormethyl)phenyl]ethoxy}-3-(4-fluorphenyl)morpholin-4-yl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonsäure--(2R,3R,4R,5S)-6-(methylamino)hexan-1,2,3,4,5-pentol(1:2)

(3-{[(2R,3S)-2-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)morpholin-4-yl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid - (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol (1:2)

fosaprepitant dimeglumine

Fosaprepitant dimeglumine (USAN)

Proemend (TN)

(3-{[(2R,3S)-2-{(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)-4-morpholinyl]methyl}-5-oxo-2,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid - 1-deoxy-1-(methylamino)-D-glucitol (1:2)

Phosphonic acid, [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-4,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]-, compd. with D-glucitol, 1-deoxy-1-(methylamino)- (1:2)

MK-0517

UNII-D35FM8T64X

Fosaprepitant dimeglumine salt

Fosaprepitant meglumine

Fosaprepitant (dimeglumine)

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