Fosaprepitant has been initially approved in 2008 in the USA. In August, 2023, an improved composition also containing SBECD has been launched under tradename FOCINVEZ (fosaprepitant injection for intravenous use) by Spes Pharmaceuticals Inc. This is the 19th approved API composition with SBECD.
The API is a prodrug of aprepitant which is a neurokinin-1 (NK 1) receptor antagonist, indicated in adults and pediatric patients 6 months of age and older, in combination with other antiemetic agents, for the prevention of:
- acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin.
- delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC).
Each vial contains 150 mg Fosaprepitant (equivalent to 245.3 mg of fosaprepitant dimeglumine) as active substance besides inactive ingredients: Betadex sulfobutylether sodium (8 g), edetate disodium (5.4mg), sodium hydroxide (for pH adjustment) in water for injection.
According to the patent of the product (US11065265), SBECD plays role as a dual functional agent for hydrolysis inhibition and solubility enhancement. The hydrolysis inhibitory effect of SBECD has been shown. Increase in amount of cyclodextrin derivative used in the fosaprepitant composition resulted in significantly less amount hydrolytic degradation product of fosaprepitant, i.e. aprepitant. On the other hand, it has been demonstrated that SBECD dramatically enhanced the solubility of aprepitant in aqueous medium. The inventors found appropriate ratio of fosaprepitant to SBECD wherein, the composition showed to prevent the drastic hydrolytic degradation of fosaprepitant to aprepitant, and in the meantime, prevent the crystallization and precipitation of aprepitant.
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