Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant.

Therapeutics and Clinical Risk Management
I N Olver

Abstract

Fosaprepitant is a prodrug of aprepitant, a neurokinin(1) (NK(1)) receptor antagonist used in prophylactic antiemetic regimens used prior to cytotoxic chemotherapy. Fosaprepitant is being developed to provide a parenterally administered alternative to the orally administered aprepitant. Fosaprepitant is rapidly converted to aprepitant and an intravenous dose of 115 mg is bioequivalent to 125 mg orally, with similar plasma concentrations at 24 hours. In phase I and II trials fosaprepitant shows efficacy, but the large randomized efficacy studies have utilized aprepitant. When it is added to dexamethasone and a 5HT(3) receptor antagonist on day 1 prior to chemotherapy aprepitant improves the control of acute post chemotherapy emesis and when continued on days 2 and 3 with dexamethasone it demonstrated even greater improvement in the control of delayed emesis. This has been shown with both cisplatin-containing regimens and those based upon cyclophosphamide and an anthracycline. Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate. Headaches are the other toxicity most commonly r...Continue Reading

Citations

Nov 27, 2009·Expert Opinion on Investigational Drugs·Laura QuartaraCarlo A Maggi
Mar 17, 2010·Indian Pediatrics·Pooja DewanDeepika Harit
Jan 1, 2013·Supportive Care in Cancer : Official Journal of the Multinational Association of Supportive Care in Cancer·I N OlverUNKNOWN Australian and New Zealand Urogenital and Prostate Cancer Trials Group
Dec 1, 2010·Journal of Applied Toxicology : JAT·Anna Giulia CattaneoGiovanni Bernardini
Aug 2, 2021·Supportive Care in Cancer : Official Journal of the Multinational Association of Supportive Care in Cancer·Jai N PatelFred Ashbury

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