Netupitant/palonosetron (Akynzeo)
Pronunciation: a-KIN-zee-oh.
- Generic name
- netupitant and palonosetron
- Drug class
- Combination antiemetic: NK1-receptor antagonist (netupitant) + 5-HT3-receptor antagonist (palonosetron)
- Form
- Capsule, 300 mg netupitant / 0.5 mg palonosetron; IV concentrate for infusion (fosnetupitant/palonosetron)
- Route
- Oral (capsule); intravenous infusion (fosnetupitant/palonosetron formulation)
- Legal status
- Prescription-only
Availability and supply rules vary by country
Trade names by country: United States · United Kingdom · Canada · Australia · New Zealand
Australia: Akynzeo (5) · Full directory
What netupitant and palonosetron is and how it works
Akynzeo is a prescription-only combination medicine used to help prevent nausea and vomiting caused by cancer chemotherapy. It combines two medicines -- netupitant and palonosetron -- and is always given together with dexamethasone. (1) (3)
Akynzeo is taken once per chemotherapy cycle, timed around when chemotherapy starts, exactly as your cancer care team directs. It is used to prevent sickness before it starts, not to treat sickness that is unrelated to chemotherapy.
Mechanism of action: how netupitant and palonosetron works
Netupitant is a selective NK1-receptor antagonist that blocks substance P-mediated signalling involved in both the acute and delayed phases of chemotherapy-induced nausea and vomiting. Palonosetron is a long-acting 5-HT3-receptor antagonist that blocks serotonin-mediated signalling primarily in the acute phase. Netupitant is a moderate CYP3A4 inhibitor with effects lasting several days after a single dose. (1) (2)
What netupitant and palonosetron is used for
Preventing chemotherapy-induced nausea and vomiting
Used together with dexamethasone in adults to help prevent acute (early) and delayed nausea and vomiting associated with cancer chemotherapy, including highly emetogenic (strongly nausea-inducing) chemotherapy such as cisplatin-based regimens, and moderately emetogenic chemotherapy. (1) (2)
Before taking netupitant and palonosetron
Do not take / not appropriate for
- Do not take Akynzeo if you have had a serious allergic reaction to netupitant, palonosetron, or any of the ingredients. (all countries) (1) (4)
- In the United Kingdom, European Union, and Canada, Akynzeo is contraindicated during pregnancy. In the United States it is not formally listed as contraindicated in pregnancy, but it may cause fetal harm based on animal data, so pregnancy status should always be discussed with the cancer care team before use. (country-dependent -- see text) (2) (3) (4) (1)
Tell your clinician about
- Whether you are pregnant, could become pregnant, or are breastfeeding.
- Any heart rhythm problems, a history of QT-interval prolongation, or electrolyte imbalances (such as low potassium or magnesium).
- All other medicines you take, especially antidepressants (SSRIs/SNRIs), other serotonergic medicines, dexamethasone, and any chemotherapy medicines broken down by the liver enzyme CYP3A4.
- Any liver or kidney problems, particularly if severe.
How to take netupitant and palonosetron
- Taken as a single capsule by mouth, approximately 1 hour before the start of chemotherapy, with or without food.
- Given once per chemotherapy cycle, on day 1 only, together with dexamethasone as directed by the cancer care team.
- The IV form (fosnetupitant/palonosetron) is given by a healthcare professional as an infusion over about 30 minutes, starting about 30 minutes before chemotherapy.
Procedures and treatment changes
Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3) (4) (5) (6)
Missed dose
Akynzeo is given on a schedule tied to chemotherapy, always by or under the direction of the cancer care team, so contact them directly about any timing question rather than adjusting the schedule independently.
Overdose
Seek urgent medical attention if too much Akynzeo may have been taken, or if severe symptoms such as a very fast or irregular heartbeat, severe confusion, or fainting occur. (1)
Side effects
Side effects and their urgency vary; report severe, persistent, or concerning symptoms.
Headache.
What to notice: Headache.
What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)
Constipation.
What to notice: Constipation.
What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)
Fatigue and asthenia (weakness).
What to notice: Fatigue and asthenia (weakness).
What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)
Dyspepsia (indigestion).
What to notice: Dyspepsia (indigestion).
What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)
Redness of the skin (erythema).
What to notice: Redness of the skin (erythema).
What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1)
Serious warnings
Signs of serotonin syndrome — emergency
Symptoms: Agitation, hallucinations, confusion, a fast heartbeat, unstable blood pressure, muscle twitching or rigidity, loss of coordination, sweating, shivering, or diarrhoea -- especially if also taking an antidepressant (SSRI/SNRI) or another serotonergic medicine.
Action: Seek emergency medical help immediately if these symptoms develop. (1) (2)
Signs of a serious allergic reaction (hypersensitivity/anaphylaxis) — emergency
Symptoms: Swelling of the face, lips, tongue, or throat; difficulty breathing; widespread rash or hives; dizziness or fainting.
Action: Seek emergency medical help immediately. (1)
Signs of a heart rhythm problem (QT-interval effects) — high caution
Symptoms: A fast, irregular, or pounding heartbeat, dizziness, or fainting -- particularly if also taking other medicines that affect heart rhythm, or with an existing heart rhythm condition or electrolyte imbalance.
Action: Tell the cancer care team promptly and seek urgent medical attention for fainting or a very irregular heartbeat. A dedicated study found no clinically relevant QT change at the approved dose, but caution is still advised in higher-risk patients. (1) (2)
Interactions
- Netupitant moderately inhibits the liver enzyme CYP3A4 for several days after a single dose, which can raise levels of other medicines broken down by this enzyme, including some chemotherapy medicines, dexamethasone, and midazolam -- the cancer care team will usually adjust related medicine doses, particularly dexamethasone. (1) (2)
- Strong CYP3A4 inducers, such as rifampin, are best avoided with ongoing Akynzeo use, as they can reduce netupitant levels and its effect. (1)
- Other serotonergic medicines, including SSRIs, SNRIs, and MAOIs, increase the risk of serotonin syndrome when combined with Akynzeo. (1) (4)
- Other medicines that affect heart rhythm (QT-prolonging medicines) may add to the cardiac caution associated with Akynzeo. (2)
Pregnancy, breastfeeding, kidney/liver function, age
Pregnancy
In the European Union, United Kingdom, and Canada, Akynzeo is contraindicated in pregnancy, and effective contraception is required during treatment and for one month after the last dose. In the United States it is not formally listed as a contraindication, but animal data suggest it may cause fetal harm. Pregnancy plans or status should always be discussed with the cancer care team before starting treatment. (1) (2) (3) (4) (5) (6)
Breastfeeding
Akynzeo should not be used while breastfeeding, per European and UK labelling; no data exist on whether netupitant, fosnetupitant, or palonosetron pass into human milk. (1) (2) (3) (4) (5) (6)
Children
Not established for use in children in the sources reviewed for this dossier -- this content covers adult use only. (1) (2) (3) (4) (5) (6)
Elderly
No specific dose adjustment based on age alone is described in the sources reviewed, but overall health, other medicines, and organ function are considered by the cancer care team regardless of age. (1) (2) (3) (4) (5) (6)
Hepatic_impairment
No dose adjustment needed for mild-to-moderate liver impairment; use is best avoided in severe liver impairment because of increased netupitant exposure. (1) (2) (3) (4) (5) (6)
Renal_impairment
No dose adjustment needed for mild-to-moderate kidney impairment; use is best avoided in severe kidney impairment or end-stage kidney disease. (1) (2) (3) (4) (5) (6)
Source_ids
US-DAILYMED-AKYNZEO-2026,EU-EMA-AKYNZEO-SMPC-2026,CA-HC-AKYNZEO-PM-2026 (1) (2) (3) (4) (5) (6)
Monitoring
Before starting
- Review of other medicines for CYP3A4 and serotonergic interactions
- Cardiac history and electrolyte status where relevant
- Pregnancy status where relevant
- Liver and kidney function in patients with known impairment
During treatment
- Watching for signs of serotonin syndrome, especially if taking other serotonergic medicines.
- Watching for signs of an allergic reaction after dosing.
- Monitoring heart rhythm in patients with existing cardiac risk factors or on other QT-prolonging medicines.
Storage
Store capsules at room temperature, in the original packaging, protected from moisture, per standard storage practice for this product; the IV concentrate is prepared and stored by healthcare professionals according to product-specific handling instructions.
Professional information
Clinician-facing context only, sourced from the current US FDA prescribing information and EU SmPC; verify against the current full label before prescribing.
United States
Indication: Prevention of acute and delayed CINV with highly/moderately emetogenic chemotherapy, in combination with dexamethasone
Dose summary: One 300 mg netupitant/0.5 mg palonosetron capsule approximately 1 hour before chemotherapy, day 1 of cycle only, with or without food. IV formulation (fosnetupitant 235 mg/palonosetron 0.25 mg) infused over 30 minutes starting 30 minutes before chemotherapy. Avoid concomitant CYP3A4 substrates for one week where feasible or consider dose reduction; avoid strong CYP3A4 inducers.
Renal context: No adjustment for mild-to-moderate renal impairment; avoid in severe renal impairment or end-stage renal disease. (1)
European Union / United Kingdom
Indication: Prevention of acute and delayed CINV with highly emetogenic cisplatin-based and moderately emetogenic chemotherapy, in adults
Dose summary: One capsule approximately 1 hour before chemotherapy. Reduce dexamethasone dose by approximately 50% when co-administered. Contraindicated in pregnancy; effective contraception required during treatment and for one month afterward.
Renal context: Not separately detailed beyond general CYP3A4/hepatic cautions in the sources reviewed. (2) (3)
Hepatic guidance
No adjustment for mild-to-moderate hepatic impairment; avoid in severe hepatic impairment due to increased netupitant exposure.
Overdose note
No specific antidote; manage supportively, with attention to cardiac rhythm and serotonergic symptoms given the combination's mechanisms. (1) (2)
Frequently asked questions
Is Akynzeo (netupitant/palonosetron) available in the US, UK, Europe, Canada, Australia, and New Zealand?
Yes, it is approved and available in all of these regions. (1) (2) (3) (4) (5) (6)
Can Akynzeo be used during pregnancy?
This differs by country: in the European Union, United Kingdom, and Canada, Akynzeo is contraindicated in pregnancy. In the United States it is not formally listed as a contraindication, but animal data suggest possible fetal harm. Pregnancy plans or status should always be discussed with the cancer care team before use. (2) (3) (4) (1)
Why does Akynzeo carry a serotonin syndrome warning?
Palonosetron, one of the two medicines in Akynzeo, belongs to a drug class (5-HT3-receptor antagonists) that has been linked to serotonin syndrome, particularly when combined with other serotonergic medicines such as SSRIs or SNRIs. This is a recognised risk to discuss with the cancer care team. (1) (2)
What is the mechanism of action of netupitant and palonosetron?
Netupitant is a selective NK1-receptor antagonist that blocks substance P-mediated signalling involved in both the acute and delayed phases of chemotherapy-induced nausea and vomiting. Palonosetron is a long-acting 5-HT3-receptor antagonist that blocks serotonin-mediated signalling primarily in the acute phase. Netupitant is a moderate CYP3A4 inhibitor with effects lasting several days after a single dose. (1) (2)
What is the generic name of Netupitant/palonosetron (Akynzeo)?
The generic name is netupitant and palonosetron. (1)
What class of drug is netupitant and palonosetron?
Netupitant/palonosetron (Akynzeo) is classed as: Combination antiemetic: NK1-receptor antagonist (netupitant) + 5-HT3-receptor antagonist (palonosetron). (1)
References
- AKYNZEO (netupitant and palonosetron capsules; fosnetupitant and palonosetron injection) -- full prescribing informationU.S. Food and Drug Administration / DailyMed (NIH), full prescribing information, Helsinn Therapeutics (U.S.), Inc. · United States · accessed 2026-07-29 · source 1
- Akynzeo, INN-netupitant/palonosetron hydrochloride -- EPAR Product InformationEuropean Medicines Agency (EMA), Summary of Product Characteristics · European Union · accessed 2026-07-29 · source 2
- Akynzeo 300 mg/0.5 mg hard capsules -- Summary of Product Characteristicselectronic medicines compendium (emc), United Kingdom -- Chugai Pharma UK Limited · United Kingdom · accessed 2026-07-29 · source 3
- AKYNZEO (netupitant/palonosetron) capsules -- Product MonographHealth Canada product monograph · Canada · accessed 2026-07-29 · source 4
- AKYNZEO netupitant/palonosetron (as hydrochloride) 300 mg/500 mcg capsule blister pack -- ARTG registrationTherapeutic Goods Administration (TGA), Australia · Australia · accessed 2026-07-29 · source 5
- Recent Approvals of Medicines Containing a New Active Ingredient (September 2017) -- Akynzeo (netupitant/palonosetron)Medsafe (New Zealand regulator) -- Prescriber Update, Recent Approvals of Medicines Containing a New Active Ingredient · New Zealand · accessed 2026-07-29 · source 6
Brand names by country
Single-ingredient netupitant and palonosetron names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.
Priority countries
United States
- Akynzeo (1)FDA approved currently labeled · 300 mg/0.5 mg capsule, 235 mg/0.25 mg IV (fosnetupitant/palonosetron) · Helsinn Therapeutics (U.S.), Inc.
United Kingdom
- Akynzeo (3)MHRA licensed emc smpc confirmed · 300 mg/0.5 mg capsule · Chugai Pharma UK Limited
Canada
- Akynzeo (4)Health Canada approved confirmed · 300 mg/0.5 mg capsule · not specified in fetched source
Australia
- Akynzeo (5)TGA ARTG registered 2015-05-06 confirmed · 300 mg/500 mcg capsule · not specified in fetched source
New Zealand
- Akynzeo (6)Medsafe new active ingredient approval confirmed 2017 · 300 mg/0.5 mg capsule · not specified in fetched source
View brands in additional countries.
European Union
Akynzeo (2)