Fosaprepitant dimeglumine

Fosaprepitant dimeglumine Properties

storage temp.	Sealed in dry,Store in freezer, under -20°C
solubility	≥50.24 mg/mL in DMSO; insoluble in EtOH; ≥13.16 mg/mL in H2O with ultrasonic
form	Powder
pka	Fosaprepitant dimeglumine has four functional groups which have pKa values of 3.05 ± 0.03, 4.92 ± 0.02, 9.67 ± 0.01 and 10.59 ± 0.03. The pka value of 3.05 corresponds to the morpholinium group, the pka of 4.92 corresponds to the monophosphonate group, the pka of 9.67 corresponds to the meglumine counter ion, and the pka of 10.59 corresponds to the triazolinone NH group.
color	White to off-white

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H315-H319

Precautionary statements

P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

NFPA 704

	0
3		0

Fosaprepitant dimeglumine Chemical Properties,Uses,Production

Description

Fosaprepitant dimeglumine belongs to the group of antiemetics. The active substance inhibits part of the vomiting centre. It is used for the treatment of postoperative or chemotherapyinduced nausea and vomiting.

Chemical Properties

Fosaprepitant dimeglumine is a white to off-white amorphous powder. It is freely soluble in water. The pH of a 1.0 g sample of fosaprepitant dimeglumine, dissolved in 25 mL of water, is approximately 8.3. Fosaprepitant, a prodrug of aprepitant, when administered intravenously is rapidly converted to aprepitant.

Uses

Fosaprepitant-d4 Dimeglumine is a labeled analogue of Fosaprepitant Dimeglumine (F727305), a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

Indications

Fosaprepitant dimeglumine is a new drug indicated to prevent nausea and vomiting associated with highly emetogenic cisplatin-based and moderately emetogenic cancer chemotherapy in adults.

Definition

ChEBI: Fosaprepitant dimeglumine is an organoammonium salt obtained by reaction of fosaprepitant with two equivalents of 1-deoxy-1-(methylamino)-D-glucitol. A substance P/neurokinin 1 (NK1) receptor antagonist. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting and postoperative nausea and vomiting It has a role as a prodrug, an antiemetic and a neurokinin-1 receptor antagonist. It contains a fosaprepitant(2-).

Biological Activity

Fosaprepitant dimeglumine acts as a therapeutic agent to treat chemotherapy-induced nausea and vomiting. It also acts as a weak inhibitor of cytochrome P450 3A4 (CYP3A4).
Fosaprepitant dimeglumine is a Substance P/neurokinin-1 (NK1) receptor antagonist. It is a water soluble prodrug of the antiemetic drug aprepitant.
Fosaprepitant dimeglumine is a water-soluble prodrug form of the neurokinin-1 receptor antagonist aprepitant. Formulations containing fosaprepitant dimeglumine have been used to prevent chemotherapy-induced nausea and vomiting.

Side effects

Most common adverse reactions in adults (≥2%) are: fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, pain in extremity.
Adverse reactions in pediatrics are similar to adults.

Fosaprepitant dimeglumine Preparation Products And Raw materials

Raw materials

Preparation Products

Fosaprepitant dimeglumine Suppliers

Global( 311)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
Hetero Drugs Limited	+91-4023704923 +91-4023704923	Telangana, India	296	58	Inquiry
Apothecon Pharmaceuticals Pvt Ltd	+91-2662244212 +91-9099007601	Gujarat, India	28	58	Inquiry
Moleculochem	9811853366	New Delhi, India	25	58	Inquiry
Rivashaa Agrotech Biopharma Pvt. Ltd.	+91-26463395 +91-7926462688	Gujarat, India	1615	58	Inquiry
Aurobindo Pharma Limited	+914066725000	Telangana, India	112	58	Inquiry
Piramal Pharma Solutions	+919892735994	Maharashtra, India	48	58	Inquiry
SMS Lifesciences India Ltd (MAHI Drugs Pvt Ltd)	+91-40-66288888 +91-8374455507	Telangana, India	23	58	Inquiry
WISDOM PHARMACEUTICAL CO LTD	+91 22 6640 2222	New Delhi, India	17	58	Inquiry
WOCKHARDT BIO AG		New Delhi, India	8	58	Inquiry
PIRAMAL ENTERPRISES LTD	+91-22-3802 3000/4000	New Delhi, India	45	58	Inquiry

Supplier	Advantage
Hetero Drugs Limited	58
Apothecon Pharmaceuticals Pvt Ltd	58
Moleculochem	58
Rivashaa Agrotech Biopharma Pvt. Ltd.	58
Aurobindo Pharma Limited	58
Piramal Pharma Solutions	58
SMS Lifesciences India Ltd (MAHI Drugs Pvt Ltd)	58
WISDOM PHARMACEUTICAL CO LTD	58
WOCKHARDT BIO AG	58
PIRAMAL ENTERPRISES LTD	58

Fosaprepitant dimeglumine Spectrum

Fosaprepitant dimeglumine(265121-04-8)MS Fosaprepitant dimeglumine(265121-04-8)¹HNMR

265121-04-8(Fosaprepitant dimeglumine)Related Search:

Fosaprepitant Benzyl Ester Aprepitant Impurity 17 (2R)-2-[(1R)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-5,6-dihydro-2H-1,4-oxazine (2R,3R)-2-[(1S)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)Morpholine hydrochloride Aprepitant

(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(phenyl)Morpholine hydrochloride Aprepitant Impurity 6 Aprepitant Aprepitant Eszopiclone

fosaprepitant dibenzyl ester Aprepitant 5-[[(2S,3R)-2-[(1S)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one (2S,3R)-2-((S)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)Morpholine Benzyl dihydrogen phosphate

(2R,3R)-2-[(1R)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)Morpholine Meglumine Fosaprepitant

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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 1-deoxy-1-(methylamino)-D-glucitol (1:2) Unii-D35fm8T64x [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]phosphonate 1-Deoxy-1-(MethylaMino)-D-glucitol 1-Deoxy-1-(MethylaMino)-D-glucitol [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]phosphonate 1-DEOXY-1-(METHYLAMINO)-D-GLUCITOL [[(2R,3S]-2-[(1R)-1-[3,5-BIS (TRIFLUOROMETHYL)PHENYL] PHENYL]ETHOXY]-(4-FLUOROPHENYL) 3-[2(R)-[1(R)-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)Morpholin-4-ylMethyl]-5-oxo-4,5-dihydro-1H-1,2,4-triazole-1-phosphinic acid bis(N-Methyl-D-glucaMine) salt Fosaprepitant diMegluMine salt Fosaprepitant dimeglumine, >=99% Fosaprepitant dimegluminer Fosaprepitant dimeglumine D-Glucitol, 1-deoxy-1-(methylamino)-, (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)phosphonate (2:1) (salt) Mk-0517 Forxatriptan Meglumine Reference Fosaprepitant dimeglumine(MK-0517) Fosaprepitant dimeglumine(MK0517,Emend, Inemend) [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 Fosaprepitant-d4 Dimeglumine CS-275 L785298 FOSAPREPITANT DIMEGLUMINE 265121-04-8 Fosaprepitant dimeglumine USP/EP/BP Fosaprepitant dimeglumine dimeglumine osaprepitant Dimeglumine Fosaprepitant D4 DimeglumineQ: What is Fosaprepitant D4 Dimeglumine Q: What is the CAS Number of Fosaprepitant D4 Dimeglumine Q: What is the storage condition of Fosaprepitant D4 Dimeglumine Q: What are the applications of Fosaprepitant D4 Dimeglumine Fosaprepitant dimeglumineQ: What is Fosaprepitant dimeglumine Q: What is the CAS Number of Fosaprepitant dimeglumine Q: What is the storage condition of Fosaprepitant dimeglumine Q: What are the applications of Fosaprepitant dimeglumine 265121-04-8 Fosaprepitant dimeglumine (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)phosphonic acid bis (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol (2R,3R,4R,5S)-6-(Methylamino)hexane-1,2,3,4,5-pentaol ((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)(2:1) 1- deoxy -1- (methylamino) -D- glucitol [3-[(2r, 3s)-2-[(1r) -1- [3,5-bis (trifluoromethyl) phenyl] ethoxy ]-3-(4- fluorophenyl) -4- morpholinyl] Fosaprepitant Dimeglumine Impurity Foxapyrtam dimeglumine Fosapitam Dimethylglucosamine MK 0517 dimeglumine MK0517 dimeglumine MK-0517 dimeglumine 265121-04-8 C23H22F7N4O6P2C7H17NO5 Inhibitors Other APIs 265121-04-8