Trial reportJournal of clinical pharmacology2014
Netupitant PET imaging and ADME studies in humans.
Trial report in Journal of clinical pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
29 citing papers in PubMed, 1 synthesis or guideline pooled it, 57 citations in OpenAlex.
- MASCC antiemetics in advanced cancer updated guideline.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2021Guideline
- Challenges in the Development of Intravenous Neurokinin-1 Receptor Antagonists: Results of a Safety and Pharmacokinetics Dose-Finding, Phase 1 Study of Intravenous Fosnetupitant.Clinical pharmacology in drug development · 2022Trial
- Efficacy and safety of netupitant/palonosetron combination (NEPA) in preventing nausea and vomiting in non-Hodgkin's lymphoma patients undergoing to chemomobilization before autologous stem cell transplantation.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2022Trial
- Efficacy and safety of NEPA, an oral combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy: a randomized dose-ranging pivotal study.Annals of oncology : official journal of the European Society for Medical Oncology · 2014Trial
- Netupitant versus aprepitant: model-predicted neurokinin-1 receptor occupancy and implications for long-delayed nausea and vomiting prevention.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2026Article
- Sustained antiemetic efficacy of fosnetupitant versus aprepitant in carboplatin-based chemotherapy: a retrospective observational study.International journal of clinical oncology · 2026Observational
- Comparative Efficacy of Fosnetupitant and Fosaprepitant for Delayed Vomiting in Patients Receiving Irinotecan-Oxaliplatin Combination Chemotherapy: A Retrospective Propensity Score-Matched Study.Cancer management and research · 2026Article
- Expert Consensus Guidance on the Management of Chemotherapy-Induced Nausea and Vomiting: An Indian Perspective.Cureus · 2025Review
- Demonstration of the Early Cardiac Bioavailability of a Non-Specific Cell-Targeted Peptide Using Radionuclide-Based Imaging In Vivo.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Fosnetupitant for the Prevention of Chemotherapy-Induced Nausea and Vomiting: A Short Review and Clinical Perspective.Advances in therapy · 2023Review
- PET Tracing of Biodistribution for Orally AdministeredJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Simulation of the oxidative metabolization pattern of netupitant, an NKJournal of pharmaceutical analysis · 2021Article
- The effectiveness of NEPA in the prevention of chemotherapy-induced nausea vomiting among chemo naive patients in an Indian setting.BMC cancer · 2021Article
- ΔEuropean journal of pharmacology · 2019Article
- The Significance of NK1 Receptor Ligands and Their Application in Targeted Radionuclide Tumour Therapy.Pharmaceutics · 2019Review
- Complementary Pharmacokinetic Profiles of Netupitant and Palonosetron Support the Rationale for Their Oral Fixed Combination for the Prevention of Chemotherapy-Induced Nausea and Vomiting.Journal of clinical pharmacology · 2019Article
- Timing flexibility of oral NEPA, netupitant-palonosetron combination, administration for the prevention of chemotherapy-induced nausea and vomiting (CINV).Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2019Article
- Anti-stress neuropharmacological mechanisms and targets for addiction treatment: A translational framework.Neurobiology of stress · 2018Review
- Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting.OncoTargets and therapy · 2018Review
- Recent developments in the clinical pharmacology of rolapitant: subanalyses in specific populations.Drug design, development and therapy · 2017Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Netupitant is a new, selective NK1 receptor antagonist under development for the prevention of chemotherapy-induced nausea and vomiting. Two studies were conducted to evaluate the brain receptor occupancy (RO) and disposition (ADME) of netupitant in humans. Positron emission tomography (PET) imaging with the NK1 receptor-binding-selective tracer [(11) C]-GR205171 was used to evaluate the brain penetration of different doses of netupitant (100, 300, and 450 mg) and to determine the NK1 -RO duration. A NK1 -RO of 90% or higher was achieved with all doses in the majority of the tested brain regions at Cmax, with a long duration of RO. The netupitant minimal plasma concentration predicted to achieve a NK1 -RO of 90%, C90% , in the striatum was 225 ng/mL; after administration of netupitant 300 mg, concentrations exceeded the C90% . In the ADME study, a single nominal dose of [(14) C]-netupitant 300 mg was used to assess its disposition. Absorption was rapid and netupitant was extensively metabolized via Phase I and II hepatic metabolism. Elimination of >90% was predicted at day 29 and was principally via hepatic/biliary route (>85%) with a minor contribution of the renal route (<5%). In conclusion, these studies demonstrate that netupitant is a potent agent targeting NK1 receptors with long lasting RO. In addition, netupitant is extensively metabolized and is mainly eliminated through the hepatic/biliary route and to a lesser extent via the kidneys.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.