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Published online: 10 August 2016
© Springer International Publishing Switzerland 2016
Abstract Intravenous fosaprepitant dimeglumine (Emend® for injection, IVEmend®; henceforth referred to as fosaprepitant) is a prodrug of and is rapidly converted to the antiemetic aprepitant, and is approved in several countries worldwide (as part of an antiemetic regimen) for the prevention of nausea and vomiting associated with highly and moderately emetogenic chemotherapy (HEC and MEC). This narrative review discusses the pharmacological properties of intravenous fosaprepitant and its clinical efficacy and tolerability in the prevention of nausea and vomiting associated with HEC and MEC. In large, randomized phase III clinical trials, a single intravenous dose of fosaprepitant 150 mg was an effective and generally well tolerated addition to an antiemetic regimen that included dexamethasone and a serotonin 5-HT^sub 3^ receptor antagonist in adult cancer patients undergoing treatment with HEC or MEC. It was also noninferior to an oral aprepitant-based regimen in adult cancer patients undergoing HEC treatment. The tolerability profile of a fosaprepitant-based regimen was typical of that in patients receiving emetogenic chemotherapy, and adverse events were generally consistent with those observed with an aprepitant-based regimen. Fosaprepitant provides a useful addition to antiemetic therapy regimens.
1 Introduction
Untreated, [90 % of highly emetogenic chemotherapy (HEC) [e.g. cisplatin, high-dose cyclophosphamide] and 30-90 % of moderately emetogenic chemotherapy (MEC) [e.g. bendamustine, low-dose cyclophosphamide] recipients experience emesis as a result of cancer treatment [1, 2]. Chemotherapy-induced nausea and vomiting (CINV) is generally categorized as acute (occurring 0-24 h after chemotherapy initiation), delayed (starting after the first 24 h), anticipatory (a conditioned response triggered by e.g. arrival at the clinic), breakthrough (occurring despite prophylaxis) and refractory (occurring despite prophylaxis during multiple treatment cycles) [1]. While the prevention and treatment of acute CINV has, in the past few decades, become easier to control, control of delayed CINV has been more elusive [3].
In general, guidelines recommend a combination of antiemetic agents to provide full protection against the various phases and types of CINV [1, 2]. For example, in recipients of HEC, guidelines recommend treatment with a serotonin 5-HT3 receptor antagonist (e.g. ondansetron) plus dexamethasone (a corticosteroid) plus a substance P/neurokinin-1 (NK1) receptor antagonist (e.g. fosaprepitant dimeglumine [Emend^ for injection, IVEmend^;henceforth referred to as fosaprepitant]) [1, 2], among other options...