Fosnetupitant and palonosetron

What is Fosnetupitant and palonosetron?

• Fosnetupitant is a prodrug of Netupitant is a substance P/neurokinin-1 (NK-1) receptor antagonists; Palonosetron is a serotonin-3 (5-HT3) receptor antagonist.

Palonosetron metabolites

Netupitant

What are the uses of this medicine?

• Fosnetupitant and palonosetron combination along with dexamethasone is indicated 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.

How does this medicine work?

Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors.

• Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used.
• 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema.
• Chemotherapeutic agents produce nausea and vomiting by stimulating the release of serotonin from the enterochromaffin cells of the small intestine.
• Serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex.
• The development of acute emesis is known to depend on serotonin and its 5-HT3 receptors have been demonstrated to selectively stimulate the emetic response.

Who Should Not Use this medicine?

• This medicine have no usage limitations.

Is this medicine FDA approved?

• Akynzeo (netupitant and palonosetron) capsules, for oral use Initial U.S. Approval: 2014
• Akynzeo (fosnetupitant and palonosetron) for injection, for intravenous use Initial U.S. Approval: 2018

What are the brand names and dosage forms of this medicine?

Brand name:

• Akynzeo

Dosage form:

1. Capsules: 300 mg netupitant/0.5 mg palonosetron in a hard gelatin capsule with white body and caramel cap with “HE1” printed on the body.
2. For Injection: 235 mg fosnetupitant/0.25 mg palonosetron white to off-white lyophilized powder in single-dose vial for reconstitution.
3. Injection: 235 mg fosnetupitant/0.25 mg palonosetron per 20 mL as a clear solution in single-dose vial.

How should this medicine be used?

• Take Akynzeo exactly as your doctor tells you to take it.
• Take 1 Akynzeo capsule by mouth, about 1 hour before you get your anti-cancer medicine (chemotherapy).
• Akynzeo for injection will be given to you in your vein by I.V. (intravenous) infusion about 30 minutes before you start your chemotherapy treatment.
• Take Akynzeo capsule with or without food.
• If you take too much Akynzeo, call your doctor or go to the nearest hospital emergency room right away.

What side effects can this medication cause?

• Allergic reactions, such as anaphylaxis. Get emergency medical help right away if you get any of the following symptoms of a serious allergic reaction with Akynzeo: hives, swollen face, trouble breathing, or chest pain.
• Serotonin syndrome which can happen with Akynzeo particularly with certain other medicines such as anti-depressants and anti-migraine medicines and can lead to death.
• The most common side effects of Akynzeo capsules and injection include: headache, weakness, fatigue, upset stomach, constipation, and skin redness.

What special precautions should I follow?

• Medicines are sometimes prescribed for purposes other than those listed in a Patient Information leaflet.
• Do not use Akynzeo for a condition for which it was not prescribed.
• Do not give Akynzeo to other people, even if they have the same symptoms you have. It may harm them.
• You can ask your doctor or pharmacist for information about Akynzeo that is written for health professionals.

What to do in case of emergency/overdose?

• 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.

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Limited available data with Akynzeo use in pregnant women are insufficient to inform a drug- associated risk of adverse developmental outcomes.

Can this medicine be used in children?

• The safety and effectiveness of Akynzeo in patients below the age of 18 years have not been established.

What should I know about storage and disposal of this medication?

• Akynzeo capsules should be stored at 20 °C to 25 °C (68 °F to 77 °F); excursions permitted from 15 °C to 30 °C (59 °F to 86 °F).
• Akynzeo for injection should be stored in carton, protected from light at 2° to 8°C (35.6 F to 46.4°F).
• Store Akynzeo injection in carton, protected from light at 20°C-25°C (68°F-77°F).

• Dailymed label info on Fosnetupitant and palonosetron
• FDA Fosnetupitant and palonosetron

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