Chemical Information

• English Name: Fosaprepitant Dimeglumine

• Molecular Formula: C23H22F7N4O6P·(C7H17NO5)2

• This represents the combination of Fosaprepitant       with the dimeglumine counter-ion.

• Molecular Weight: 1004.83 g/mol

• CAS Number: 265121-04-8

Pharmacological Action

Fosaprepitant Dimeglumine is a prodrug of aprepitant, meaning it is converted into the active form (aprepitant) in the body. Its primary pharmacological actions include:

1.     Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV):

o    Fosaprepitant works by blocking the neurokinin-1 (NK1) receptors in the brain, which are involved in the vomiting reflex. This inhibition prevents nausea and vomiting associated with chemotherapy treatments.

2.     Interaction with Substance P:

o    Substance P is a neuropeptide that binds to NK1 receptors and is involved in the emetic (vomiting) pathway. By blocking these receptors, Fosaprepitant reduces the effects of substance P.