Netupitant/Palonosetron: A Review in Chemotherapy-Induced Nausea and Vomiting

Shirley, Matt

doi:10.1007/s40265-021-01558-2

Cited by 27 publications

(16 citation statements)

References 38 publications

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“…Consistent with previous research resultss, the acute phase is mainly mediated by 5-HT 3 receptors and is therefore particularly sensitive to 5-HT 3 receptor antagonists [16].In our study, acute CINV can be effectively controlled by the use of panolosetron, which has a high a nity for binding to 5-HT3 receptors. Panolosetron also inhibits cross-talk between the NK-1 and 5-HT3 receptor pathways [17], which is assumed to be the cause of the observed effect in preventing delayed nausea and vomiting. As a result, our ndings revealed that panolosetron and fosaprepitant act synergistically to keep the overall incidence of nausea (≤12%) and vomiting (≤4%) at a low level.…”

Section: Discussionmentioning

confidence: 99%

Prolonged usage of fosaprepitant for prevention of delayed CINV in patients receiving highly emetogenic chemotherapy

Gao#

Guan

Sun

et al. 2023

Preprint

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Background: Even though chemotherapy-induced nausea and vomiting (CINV) can be well controlled in the acute phase, the incidence of delayedCINV remains high. In this study, we intend to investigate whether prolonged use of NK-1 receptor antagonist (RA) in addition to 5-HT3 RA and dexamethasone (DEX) was more effective in preventing delayed CINV. Methods: This study was designed to compare the efficacy and safetyof fosaprepitant 150 mg given on days 1,3 (prolonged group) versus on day 1 (regular group) in patients receiving highly emetogenic chemotherapy (HEC). All patients also treated withpalonosetron on day 1 and DEX on days 1-3. The primary endpoint was the incidence of delayed nausea and vomiting. The second endpoint was related AEs. All the above endpoints were defined according to CTCAE 5.0. Results: Seventy-seven patients were randomly assigned to prolonged group and seventy-nine to regular group. Prolonged group demonstrated superiority in controlling delayed CINV to regular group, with statistically significant lower incidence of nausea (6.17% vs 12.66%, P=0.0056), and slightly lower incidence of grade 1 vomiting (1.62% vs 3.80%, P=0.0953) in the delayed phase. In addition, prolonged use of fosaprepitant was safe. No significant difference was found between the two groups regarding constipation, diarrhea, hiccough, fatigue, palpitation and headache in delayed phase. Conclusions: Prolonged use of fosaprepitant can effectively and safely prevent delayed CINV in patients receiving HEC.

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Section: Discussionmentioning

confidence: 99%

Prolonged usage of fosaprepitant for prevention of delayed CINV in patients receiving highly emetogenic chemotherapy

Gao#

Guan

Sun

et al. 2023

Preprint

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“…Fosnetupitant is a novel NK 1 receptor antagonist for intravenous administration, which has high selectivity and affinity for NK 1 receptors [ 20 , 21 ].…”

Section: Mechanism Of Action Of Fosnetupitantmentioning

confidence: 99%

Fosnetupitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting: A Short Review and Clinical Perspective

2023

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Chemotherapy-induced nausea and vomiting (CINV) is often ranked by patients as one of the most distressing and feared consequences of chemotherapy. The novel neurokinin-1 (NK 1 ) receptor antagonist fosnetupitant, a phosphorylated prodrug formulation of netupitant, was approved in Japan in 2022. Fosnetupitant is one of the standard treatments for the prevention of CINV in patients who are receiving highly (any treatment where CINV occurs in more than 90% of patients) or moderately (where CINV occurs in 30–90% of patients) emetogenic chemotherapies. The aim of this commentary is to describe the mechanism of action, tolerability, and antiemetic efficacy of single-agent fosnetupitant in the prevention of CINV, and to discuss its clinical application, in order to aid optimal use.

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“…[ 1 ] To date, more than ten oligonucleotide therapeutics have been approved by the US Food and Drug Administration (FDA); most are antisense oligonucleotide and short interfering RNA (siRNA) drugs. [ 1b,2 ] The considerable therapeutic effects and broad room for improvement continue to inspire further exploration. The research challenge remains the delivery efficiency of targeted oligonucleotides and includes impermeability to cells, nuclease degradation, and failed lysosome escape.…”

Section: Introductionmentioning

confidence: 99%

A Lysosome‐Activated Tetrahedral Nanobox for Encapsulated siRNA Delivery

et al. 2022

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Tetrahedral framework nucleic acids (tFNAs) have attracted extensive attention as drug nanocarriers because of their excellent cellular uptake. However, for oligonucleotide cargos, tFNA mainly acts as a static delivery platform generated via sticky‐ended ligation. Here, inspired by the original stable space inside the tetrahedral scaffold, a dynamic lysosome‐activated tFNA nanobox is fabricated for completely encapsulating a short interfering RNA (siRNA) of interest. The closed tetrahedral structure endows cargo siRNA with greater resistance against RNase and serum and enables solid integration with the vehicle during delivery. Moreover, the pH‐responsive switch of nanobox allows the controlled release of siRNA upon entry into lysosomes at cell culture temperature. Based on protective loading and active unloading, an excellent silencing effect on the target tumor necrosis factor alpha (TNFα) gene is achieved in in vitro and in vivo experiments. Conclusively, the nanobox offers a dynamic pH‐sensitive confinement delivery system for siRNA and can be an extendable strategy for other small RNA.

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Netupitant/Palonosetron: A Review in Chemotherapy-Induced Nausea and Vomiting

Cited by 27 publications

References 38 publications

Prolonged usage of fosaprepitant for prevention of delayed CINV in patients receiving highly emetogenic chemotherapy

Prolonged usage of fosaprepitant for prevention of delayed CINV in patients receiving highly emetogenic chemotherapy

Fosnetupitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting: A Short Review and Clinical Perspective

A Lysosome‐Activated Tetrahedral Nanobox for Encapsulated siRNA Delivery

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