Comparative Pharmacology
Head-to-head clinical analysis: EMRELIS versus FOSAPREPITANT DIMEGLUMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMRELIS versus FOSAPREPITANT DIMEGLUMINE.
EMRELIS vs FOSAPREPITANT DIMEGLUMINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Emrelis is a monoclonal antibody that inhibits the interaction between programmed cell death protein 1 (PD-1) and its ligands PD-L1 and PD-L2, thereby activating T-cell-mediated antitumor immune response.
Fosaprepitant dimeglumine is a prodrug of aprepitant, a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It inhibits emesis by blocking NK1 receptors in the central nervous system, particularly in the area postrema and the nucleus tractus solitarius.
100 mg subcutaneously once weekly.
150 mg intravenous over 30 minutes on day 1, combined with dexamethasone and a 5-HT3 antagonist; alternatively, 115 mg IV on day 1 followed by 80 mg IV on day 2 and 80 mg IV on day 3, or 150 mg oral (as fosaprepitant dimeglumine or aprepitant) on day 1 and 80 mg oral on days 2 and 3.
None Documented
None Documented
12 hours (terminal); dosing interval adjusted in renal impairment (CrCl <30 mL/min)
Terminal elimination half-life of aprepitant is approximately 9 to 13 hours; clinical significance includes once-daily dosing for prevention of chemotherapy-induced nausea and vomiting.
Renal: 70% unchanged; fecal: 15%; biliary: 10%
Fosaprepitant is rapidly converted to aprepitant. Aprepitant is eliminated primarily by metabolism; <5% of the dose is excreted unchanged in urine. Fecal excretion accounts for approximately 58% of the dose, and urinary excretion accounts for 43% (mostly as metabolites).
Category C
Category C
Antiemetic
Antiemetic