Fosnetupitant

**Semantic type:** Pharmacologic Substance

**Definition:** A prodrug of netupitant, a selective neurokinin 1 receptor (NK1R; TACR1) antagonist, with potential antiemetic activity. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form netupitant. Netupitant competitively binds to and blocks the activity of NK1Rs in the central nervous system (CNS), by inhibiting binding of the endogenous tachykinin-derived neuropeptide substance P (SP) to NK1R. This prevents delayed emesis, which is associated with SP secretion. This may prevent chemotherapy-induced nausea and vomiting (CINV).

**Synonyms:** - FOSNETUPITANT