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Drug intelligence / Profile preview
90 mg MK-0517 (PS80)
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
90 mg MK-0517 (PS80) is a specific dose and polysorbate 80 (PS80)-based intravenous formulation of fosaprepitant dimeglumine, a water-soluble phosphoryl prodrug of aprepitant developed by Merck. Fosaprepitant is a neurokinin-1 (NK-1) receptor antagonist that, upon intravenous administration, is rapidly converted by endogenous phosphatases to its active moiety, aprepitant, within approximately 30 minutes. Aprepitant acts as a selective, high-affinity antagonist of human substance P/neurokinin-1 (NK1) receptors in the central and peripheral nervous systems. This formulation was evaluated in a Phase 1 clinical trial (MK-0517-012) to assess the safety, tolerability, pharmacokinetics, and bioequivalence of various fosaprepitant formulations compared to oral aprepitant. Fosaprepitant is indicated for the prevention of chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
- Other names
- 90 mg MK-0517 (PS80)
02
Targets
TACR1 (Neurokinin‑1 Receptor)
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