Fosaprepitant dimeglumine
- Product Name
- Fosaprepitant dimeglumine
- CAS No.
- 265121-04-8
- Chemical Name
- Fosaprepitant dimeglumine
- Synonyms
- CS-275;Mk-0517;L785298;Unii-D35fm8T64x;MK0517 dimeglumine;MK 0517 dimeglumine;MK-0517 dimeglumine;Foxapyrtam dimeglumine;osaprepitant Dimeglumine;Fosaprepitant dimeglumine
- CBNumber
- CB61105364
- Molecular Formula
- C30H39F7N5O11P
- Formula Weight
- 809.63
- MOL File
- 265121-04-8.mol
Fosaprepitant dimeglumine Property
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- SML2228
- Product name
- Fosaprepitant dimeglumine
- Purity
- ≥98% (HPLC)
- Packaging
- 10MG
- Price
- $102
- Updated
- 2024/03/01
- Product number
- SML2228
- Product name
- Fosaprepitant dimeglumine
- Purity
- ≥98% (HPLC)
- Packaging
- 50MG
- Price
- $411
- Updated
- 2024/03/01
- Product number
- 24034
- Product name
- Fosaprepitant dimeglumine
- Packaging
- 5mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 24034
- Product name
- Fosaprepitant dimeglumine
- Packaging
- 10mg
- Price
- $96
- Updated
- 2024/03/01
- Product number
- 24034
- Product name
- Fosaprepitant dimeglumine
- Packaging
- 25mg
- Price
- $225
- Updated
- 2024/03/01
Fosaprepitant dimeglumine Chemical Properties,Usage,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.
Originator
Merck (United States)
Uses
Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist
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.
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-).
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.
brand name
IvEmend
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.
Mode of action
Fosaprepitant is a prodrug of aprepitant and accordingly, its antiemetic effects are attributable to aprepitant. 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 (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies have shown that aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.
Clinical claims and research
One of the most debilitating side effects of cancer treatment is CINV. Although concomitant anti-emetic agents have been prevalent for the past two decades, 50 60% of patients are still plagued by CINV. To meet this need, fosaprepitant dimeglumine has been launched as a water-soluble, phosphoryl pro-drug of aprepitant for intravenous applications. This pro-drug is rapidly converted to aprepitant in vivo, which has a high affinity for the NK-1 receptor (IC50= 90 50 pM for the displacement of [125I]-substance P from hNK-1 expressed in CHO cells); antagonism 606 Shridhar Hegde and Michelle Schmidt of NK-1 prevents binding of the endogenous substance P that is known to induce vomiting. Fosaprepitant is prepared by the regioselective phosphorylation of aprepitant with dibenzylphosphoryl chloride followed by catalytic hydrogenolysis in the presence of N-methyl-Dglucamine. It is approved for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly and moderately emetogenic cancer chemotherapy.
References
[1] van belle sj1, 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.
Fosaprepitant dimeglumine Preparation Products And Raw materials
Raw materials
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View Lastest Price from Fosaprepitant dimeglumine manufacturers
- Product
- Fosaprepitant dimeglumine 265121-04-8
- Price
- US $1.00-1.00/KG
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 50tons
- Release date
- 2020-05-06
- Product
- Fosaprepitant dimeglumine 265121-04-8
- Price
- US $30.00-10.00/kg
- Min. Order
- 1kg
- Purity
- 0.99
- Supply Ability
- 10 tons
- Release date
- 2023-11-24
- Product
- Fosaprepitant dimeglumine 265121-04-8
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98.0%
- Supply Ability
- 10kg/month
- Release date
- 2021-12-17