Netupitant

Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Palonosetron is a 5-HT 3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors.

• AKYNZEO capsules is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. AKYNZEO capsules is a combination of palonosetron and netupitant: palonosetron prevents nausea and vomiting during the acute phase and netupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.ICD-10: R11.2

• None.contraindicated

Recommended Dosage AKYNZEO capsules: The recommended dosage is one AKYNZEO capsule administered 1 hour prior to the start of chemotherapy, with or without food. ( 2.1 ) Preparation and Administration AKYNZEO injection is supplied either as a Ready-to-Use (with hanger) vial or a To-be-Diluted vial. (2.2) AKYNZEO for injection requires dilution prior to administration. ( 2.3 ) See full prescribing information for information on preparation, administration, and incompatibilities for each product. (2.2, 2.3, 2.4 ) 2.1 Recommended Dosage The recommended dosages of AKYNZEO and dexamethasone in adults for the prevention of nausea and vomiting associated with administration of emetogenic chemotherapy are shown in Table 1. AKYNZEO capsules can be taken with or without food. Table 1: Antiemetic Treatment Regimen Treatment Regimen Day 1 Days 2 to 4 Highly Emetogenic Chemotherapy, including Cisplatin-Based Chemotherapy AKYNZEO capsules 1 capsule of AKYNZEO 1 hour before chemotherapy Dexamethasone 8 mg once a day Dexamethasone 12 mg 30 minutes before chemotherapy AKYNZEO for injection and AKYNZEO injection 1 vial of AKYNZEO Infuse over 30 minutes starting 30 minutes before chemotherapy [see Dosage and Administration (2.2)] Dexamethasone 8 mg once a day Dexamethasone 12 mg 30 minutes before chemotherapy Anthracyclines and Cyclophosphamide-Based Chemotherapy and Chemotherapy Not Considered Highly Emetogenic AKYNZEO capsules 1 capsule of AKYNZEO 1 hour before chemotherapy None Dexamethasone 12 mg 30 minutes before chemotherapy 2.2 Preparation and Administration of AKYNZEO Injection (Ready-…

Hypersensitivity reactions, including anaphylaxis, have been reported in patients receiving palonosetron, one of the components of AKYNZEO, with or without known hypersensitivity to other 5-HT 3 receptor antagonists. ( 5.1 ) Serotonin syndrome has been reported with 5-HT 3 receptor antagonists alone but particularly with concomitant use of serotonergic drugs. If such symptoms occur, discontinue AKYNZEO and initiate supportive treatment. If concomitant use of AKYNZEO with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome. ( 5.2, 7.3 ) 5.1 Hypersensitivity Hypersensitivity reactions, including anaphylaxis, have been reported in patients treated with palonosetron, one of the components of AKYNZEO, with or without known hypersensitivity to other 5-HT 3 receptor antagonists. 5.2 Serotonin Syndrome The development of serotonin syndrome has been reported with 5-HT 3 receptor antagonists. Most reports have been associated with concomitant use of serotonergic drugs (e.g., selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, mirtazapine, fentanyl, lithium, tramadol, and intravenous methylene blue). Some of the reported cases were fatal. Serotonin syndrome occurring with overdose of another 5-HT 3 receptor antagonist alone has also been reported. The majority of reports of serotonin syndrome related to 5-HT 3 receptor antagonist use occurred in a post-anesthesia care unit or an infusion center.

The following clinically significant adverse reactions are found elsewhere in the labeling: Hypersensitivity Reactions [see Warnings and Precautions ( 5.1 )] Serotonin Syndrome [see Warnings and Precautions ( 5.2 )] Most common adverse reactions (≥3%) for AKYNZEO capsules are headache, asthenia, dyspepsia, fatigue, constipation and erythema ( 6.1 ) The safety profile of AKYNZEO for injection was generally similar to that seen with AKYNZEO capsules. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact HELSINN at 1-844-357-4668 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. AKYNZEO Capsules The overall safety of AKYNZEO capsules was evaluated in 1538 cancer patients and healthy subjects in clinical trials. The data described below reflect exposure to AKYNZEO in 1169 cancer patients, receiving at least one cycle of cancer chemotherapy in 3 active-controlled trials [see Clinical Studies ( 14 .1 )] , including 782 exposed to AKYNZEO for at least 4 cycles and 321 exposed for at least 6 cycles, up to a maximum of 12 cycles of chemotherapy. The median age was 55, 79% were female, 83% were White, 13% were Asian, and 4% were Hispanic. All patients received a single oral dose of AKYNZEO 1 hour prior to the start of each chemotherapy cycle.

Pregnancy: May cause fetal harm ( 8.1 ). Hepatic Impairment: Avoid use in patients with severe hepatic impairment ( 8.6 ) Renal Impairment: Avoid use in patients with severe renal impairment or end-stage renal disease ( 8.7 ) 8.1 Pregnancy Risk Summary Limited available data with AKYNZEO use in pregnant women are insufficient to inform a drug- associated risk of adverse developmental outcomes. In animal reproduction studies with netupitant, no effects on embryo-fetal development were observed following daily oral administration in pregnant rats during the period of organogenesis at doses up to 3.7 times the human AUC (area under the plasma concentration-time curve) at the recommended single dose to be given with each cycle of chemotherapy. However, a dose-dependent increase in adverse effects on embryo-fetal development was observed following daily oral administration of netupitant in pregnant rabbits during the period of organogenesis with doses at least 0.2 times the human AUC at the recommended single dose to be given with each cycle of chemotherapy. Daily oral administration of netupitant in rats up to 3.7 times the human AUC at the recommended dose during organogenesis through lactation produced no adverse effects in the offspring (see Data).

Metabolism

Netupitant and Palonosetron Absorption Upon single oral administration of AKYNZEO capsules to healthy subjects and patients, netupitant and palonosetron were measurable within 1 hour after administration and reached the maximum concentration (Cmax) in approximately 4 to 5 hours (Table 8).

In the event of overdose, AKYNZEO should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of AKYNZEO, drug- induced emesis may not be effective. Dialysis studies have not been performed; due to the large volume of distribution, dialysis is unlikely to be an effective treatment for AKYNZEO overdose. A total of 33 adult cancer patients were administered oral palonosetron at a dose of 90 mcg/kg (approximately 12 times the recommended dose in AKYNZEO capsules), as part of a dose ranging study and had a similar incidence of adverse reactions compared to lower doses. A single dose of 600 mg (2 times the recommended dose in AKYNZEO capsules) of oral netupitant was administered to 49 healthy subjects and a similar incidence of adverse reactions was observed when compared to lower doses of netupitant in cancer patients and healthy subjects.

• Oct 10, 2014NDANDA205718Helsinn Hlthcare

1. 1Nausea12011%
2. 2Diarrhoea857.8%
3. 3Fatigue857.8%
4. 4Neutropenia827.5%
5. 5Vomiting716.5%
6. 6Dyspnoea706.4%
7. 7Death676.1%
8. 8Off Label Use534.8%
9. 9Pyrexia514.7%
10. 10Febrile Neutropenia474.3%
11. 11Decreased Appetite464.2%
12. 12Asthenia433.9%
13. 13Anaemia423.8%
14. 14Constipation423.8%
15. 15Hypotension423.8%

The 10 most recently updated of 28 ClinicalTrials.gov registrations naming Netupitant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• NEPA Combined With Olanzapine, Dexamethasone-sparing for the Effect of CINV in Patients Receiving HEC Regimens
  Completed · Phase 3 · Interventional · 644 enrolled · Fudan University
  NCT06331520updated 2026-04-09
• AKY15-HK-301_NEPA Study
  Active not recruiting · Phase 2 · Interventional · 55 enrolled · Chinese University of Hong Kong
  NCT03386617updated 2026-03-04
• NEPA in Patients With HER2-positive or HER2-low Advanced Breast Cancer Treated With T-DXd
  Enrolling by invitation · Observational · 100 enrolled · Yeon Hee Park
  NCT07132749updated 2026-01-08
• Electroacupuncture for Chemotherapy-Induced GI Symptom Clusters in Breast Cancer
  Recruiting · Phase 3 · Interventional · 388 enrolled · Jiuda Zhao
  NCT06952920updated 2025-12-15
• Oral Akynzeo® vs Standard of Care in Preventing CINV in High-risk MEC Patients (MyRisk)
  Completed · Phase 4 · Interventional · 414 enrolled · Helsinn Healthcare SA
  NCT04817189updated 2025-12-02
• A Study on Nausea and Vomiting Caused by T-DXd in Breast Cancer Patients
  Not yet recruiting · Phase 4 · Interventional · 120 enrolled · Tianjin Medical University Cancer Institute and Hospital
  NCT07254416updated 2025-11-28
• Treatment of Refractory Nausea and Vomiting in Patients With Breast Cancer
  Completed · Phase 3 · Interventional · 1,363 enrolled · University of Rochester NCORP Research Base
  NCT03367572updated 2025-09-25
• A Clinical Trial to Assess Safety and Pharmacokinetics of Fosnetupitant 235 mg and Metabolites in Healthy Volunteers
  Terminated · Phase 1 · Interventional · 50 enrolled · Helsinn Healthcare SA
  NCT06840769updated 2025-05-04
• Electroacupuncture for the Prevention of Chemotherapy-induced Nausea and Vomiting in Patients With Breast Cancer
  Recruiting · Phase 3 · Interventional · 370 enrolled · Jiuda Zhao
  NCT06200168updated 2025-04-02
• Akynzeo as Antiemetic Treatment in Patients With Endometrial Cancer
  Recruiting · Phase 4 · Interventional · 84 enrolled · Fondazione IRCCS Istituto Nazionale dei Tumori, Milano
  NCT06726291updated 2024-12-10

Frequently asked questions

How does Netupitant work?

Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Palonosetron is a 5-HT 3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors.

What is Netupitant used for?

According to FDA labeling, Netupitant carries indications including: AKYNZEO capsules is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy. AKYNZEO capsules is a combination of palonosetron and netupitant: palonosetron prevents nausea and vomiting during the acute phase and netupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Netupitant?

Netupitant is classified as Substance P/Neurokinin-1 Receptor Antagonist, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A4 Inhibitors, Neurokinin 1 Antagonists, P-Glycoprotein Inhibitors, Emesis Suppression.

What are the brand names for Netupitant?

Netupitant is marketed under brand names including Akynzeo.

What are the contraindications for Netupitant?

Netupitant labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.