Fosaprepitant Chemical Properties

Melting point:

>74°C (dec.)

Density 

1.65

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO, Methanol

pka

2.45±0.20(Predicted)

form 

Solid

color 

White

Fosaprepitant Usage And Synthesis

Chemical Properties

White Solid

Uses

Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

Uses

Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

Uses

An antiemetic drug, a Aprepitant prodrug.

Definition

ChEBI: A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triaz l-1-yl)phosphonic acid.

Biological Activity

fosaprepitant (l-758,298 mk-0517) is an antagonist of neurokinin-1[1].fosaprepitant has shown the pharmacodynamic function by its active metabolite aprepitant. fosaprepitanot has been found to be a highly selective antagonist of the nk-1 receptor and inhibit the cation of substance p. in addition, fosaprepitant has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. besides, because of the brain penetrating of aprepitant, fosaprepitant has been revealed to have a very high affinity for the nk-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. fosaprepitant has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (cinv) by combination with a 5-ht3 antagonist and a steroid [1].

Drug interactions

Potentially hazardous interactions with other drugs
Antidepressants: avoid with St John’s wort.
Antipsychotics: avoid with pimozide.
Cytotoxics: possibly increases bosutinib concentration - avoid or reduce bosutinib dose.
Oestrogens and progestogens: may cause contraceptive failure.

Metabolism

Fosaprepitant is a prodrug and is rapidly metabolised to aprepitant. Aprepitant undergoes extensive hepatic metabolism, mainly via oxidation by the cytochrome P450 isoenzyme CYP3A4; the isoenzymes CYP1A2 and CYP2C19 mediate minor metabolic pathways. The resultant metabolites have weak activity and are excreted in the urine and in the faeces.

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(172673-20-0)Related Product Information

• Moroxydine hydrochloride
• Piracetam
• PHENYL VALERATE
• Diphenyl ether
• Moroxydine
• Dimethomorph
• Zolpidem tartrate
• Voriconazole
• PHENYL RESIN
• Fosaprepitant Impurity 9
• Fosaprepitant Impurity 11
• Fosaprepitant Impurity 17
• Fosaprepitant Impurity 14
• Aprepitant
• fosaprepitant dibenzyl ester
• Fosaprepitant Benzyl Ester
• Fosaprepitant dimeglumine
• Diphosphoric acid, tris(phenylmethyl) ester (9CI)