This article reviews therapeutic efficacy and tolerability data relating to the use of (fos)netupitant/palonosetron in the prevention of CINV, and also summarises pharmacological data relating to the drug combination. Netupitant/palonosetron is approved in the USA and the EU for use (in combination with dexamethasone) in the prevention of CINV in adults, and is available in oral and, more recently, intravenous (IV) formulations (with fosnetupitant, a water-soluble prodrug of netupitant, used in the IV formulation). Netupitant/palonosetron (NEPA Akynzeo ®) is a fixed-dose combination of the NK1 receptor antagonist netupitant and the second-generation 5-HT 3 receptor antagonist palonosetron, with the rationale that the convenience of administering the two drugs in a fixed combination (as a single dose) has the potential to improve adherence to CINV prevention guidelines. dolasetron, granisetron, ondansetron, palonosetron) and corticosteroids (typically dexamethasone). Different options for use in CINV prophylaxis include the dopamine and serotonin 2 (5-HT 2) receptor antagonist olanzapine, neurokinin 1 (NK1) receptor antagonists, serotonin 3 (5-HT 3) receptor antagonists (e.g. Guidelines for the prevention of CINV recommend that patients scheduled to receive highly emetogenic chemotherapy (HEC) or moderately emetogenic chemotherapy (MEC) should be given combination prophylaxis with drugs targeting different pathways. In conclusion, netupitant/palonosetron is a simple, convenient and effective drug combination for the prevention of acute and delayed CINV in patients receiving chemotherapy that has a moderate to high potential to cause nausea and vomiting.Ĭhemotherapy-induced nausea and vomiting (CINV) is mediated by an interaction of neurotransmitter pathways, including serotonin and substance P pathways. Both the oral and intravenous formulations of the drug combination are well tolerated. In clinical trials, high proportions of patients who received netupitant/palonosetron (used in combination with the corticosteroid dexamethasone) prior to chemotherapy reported no vomiting, no requirement for rescue medication, and no significant nausea in the 5 days post chemotherapy. Approved for use in the prevention of acute and delayed CINV in adults, netupitant/palonosetron is given orally or via intravenous infusion as a single dose prior to chemotherapy. Netupitant/palonosetron (NEPA Akynzeo ®) is a fixed-dose combination of two drugs (netupitant, a neurokinin 1 receptor antagonist and palonosetron, a serotonin 3 receptor antagonist) which target two different signalling pathways involved in the induction of vomiting. The fixed-dose combination is concordant with guideline recommendations and provides a simple and convenient option for prophylaxis against acute and delayed CINV in patients receiving highly or moderately emetogenic chemotherapy.Ĭhemotherapy-induced nausea and vomiting (CINV) is a common problem during cancer treatment. Both the oral and IV formulations of the drug combination are well tolerated. Further, oral netupitant/palonosetron was found to be superior to palonosetron and non-inferior to aprepitant plus granisetron in preventing CINV in individual trials. In clinical trials, (fos)netupitant/palonosetron plus dexamethasone was associated with high complete response rates (no emesis and no rescue medication) in the acute, delayed and overall phases in patients receiving highly or moderately emetogenic chemotherapy, with efficacy maintained over multiple cycles. Administered as a single dose, (fos)netupitant/palonosetron (in combination with dexamethasone) is indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Netupitant/palonosetron (NEPA Akynzeo ®), available in oral and intravenous (IV) formulations, is a fixed-dose combination of the neurokinin 1 (NK1) receptor antagonist netupitant (or the prodrug, fosnetupitant, in the IV formulation) and the second-generation serotonin 3 (5-HT 3) receptor antagonist palonosetron.
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