Combination of | |
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Netupitant | NK1 receptor antagonist |
Palonosetron | 5-HT3 receptor antagonist |
Clinical data | |
Trade names | Akynzeo |
AHFS/Drugs.com | Monograph |
MedlinePlus | a614053 |
License data | |
Pregnancy category |
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Routes of administration | By mouth, intravenous |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
CAS Number | |
KEGG |
Netupitant/palonosetron, sold under the brand name Akynzeo, is a fixed-dose combination medication used for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. [5] [7] It is marketed and distributed by Helsinn Therapeutics. Netupitant is an NK1 receptor antagonist and palonosetron is a 5-HT3 receptor antagonist. [8]
The capsules contain netupitant and palonosetron hydrochloride. The intravenous version is a combination of fosnetupitant chloride hydrochloride and palonosetron hydrochloride. [9] [5] [6]
Netupitant/palonosetron may be contraindicated during pregnancy. [10] [1] [11]
The most common side effects include headache, weakness, fatigue, upset stomach, constipation, and skin redness. [5] The overall profile of adverse effects is comparable to that of palonosetron (see Palonosetron#Adverse effects); no common adverse effects can be attributed to netupitant. [10]
Netupitant/palonosetron was approved for use in the United States in October 2014. [12] It was approved for use in the European Union in May 2015. [6] The intravenous version, which contains the prodrug fosnetupitant in place of netupitant, was approved in the United States in April 2018. [13] [9]
Metoclopramide is a medication used for stomach and esophageal problems. It is commonly used to treat and prevent nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying, and to help with gastroesophageal reflux disease. It is also used to treat migraine headaches.
Esomeprazole, sold under the brand name Nexium among others, is a medication which reduces stomach acid. It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome. Effectiveness is similar to other proton pump inhibitors (PPIs). It is taken by mouth or injection into a vein.
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Cefixime, sold under the brand name Suprax among others, is an antibiotic medication used to treat a number of bacterial infections. These infections include otitis media, strep throat, pneumonia, urinary tract infections, gonorrhea, and Lyme disease. For gonorrhea typically only one dose is required. In the United States it is a second-line treatment to ceftriaxone for gonorrhea. It is taken by mouth.
Meloxicam, sold under the brand name Mobic among others, is a nonsteroidal anti-inflammatory medication (NSAID) used to treat pain and inflammation in rheumatic diseases and osteoarthritis. It is used by mouth or by injection into a vein. It is recommended that it be used for as short a period as possible and at a low dose.
Dolasetron (trade name Anzemet) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.
Irinotecan, sold under the brand name Camptosar among others, is a medication used to treat colon cancer, and small cell lung cancer. For colon cancer it is used either alone or with fluorouracil. For small cell lung cancer it is used with cisplatin. It is given intravenously.
Cysteamine is a chemical compound that can be biosynthesized in mammals, including humans, by the degradation of coenzyme A. The intermediate pantetheine is broken down into cysteamine and pantothenic acid. It is the biosynthetic precursor to the neurotransmitter hypotaurine.
Defibrotide, sold under the brand name Defitelio, is a mixture of single-stranded oligonucleotides that is purified from the intestinal mucosa of pigs. It is used to treat veno-occlusive disease of the liver of people having had a bone marrow transplant, with different limitations in the US and the European Union. It works by protecting the cells lining blood vessels in the liver and preventing blood clotting; the way it does this is not well understood.
Palonosetron, sold under the brand name Aloxi, is used for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is a 5-HT3 antagonist.
Isavuconazonium sulfate, sold under the brand name Cresemba, is a systemic antifungal medication of the triazole class which is used to treat invasive aspergillosis and mucormycosis.
Azasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27 It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg". Pharmacokinetics data from S. Tsukagoshi.
Tedizolid, is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics, and is marketed for the treatment of acute bacterial skin and skin structure infections.
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Netupitant is an antiemetic medication. In the United States, the combinations of netupitant/palonosetron and fosnetupitant/palonosetron are approved by the Food and Drug Administration for the prevention of acute and delayed chemotherapy-induced nausea and vomiting, including highly emetogenic chemotherapy such as with cisplatin. In the European Union, the combinations are approved by the European Medicines Agency (EMA) for the same indication.
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Fosnetupitant is a medication used for the treatment of chemotherapy-induced nausea and vomiting. It is a prodrug of netupitant. It is used in combination with palonosetron hydrochloride and formulated as the salt fosnetupitant chloride hydrochloride for intravenous use.
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