pharmacopeia
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/api/v1/drug/palonosetron

Mechanism of action

Sourced from openFDA

Palonosetron is a 5-HT 3 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.

Serotonin 3 ReceptorSerotonin 5HT-3

Indications

Sourced from openFDA
  • Palonosetron hydrochloride injection is indicated in adults for prevention of: acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). acute nausea and vomiting associated with initial and repeat courses highly emetogenic cancer chemotherapy (HEC).ICD-10: R11.2

Contraindications

Sourced from openFDA
  • Palonosetron hydrochloride injection is contraindicated in patients known to have hypersensitivity to palonosetron [see Warnings and Precautions ( 5.1 )] .contraindicated

Dosage & administration

Sourced from openFDA

Chemotherapy-Induced Nausea and Vomiting ( 2.1 ) *Note different dosing units in pediatrics Age Dose* Infusion Time Adults 0.25 mg as a single dose Infuse over 30 seconds beginning approximately 30 minutes before the start of chemotherapy Pediatrics (1 month to less than 17 years) 20 micrograms per kilogram (maximum 1.5 mg) as a single dose Infuse over 15 minutes beginning approximately 30 minutes before the start of chemotherapy Postoperative Nausea and Vomiting ( 2.1 ) The recommended adult dosage is 0.075 mg as a single intravenous dose administered over 10 seconds immediately before the induction of anesthesia. 2.1 Recommended Dosage Prevention of Chemotherapy-Induced Nausea and Vomiting The recommended dosage of palonosetron hydrochloride injection for prevention of nausea and vomiting associated with HEC and MEC in adults and associated with emetogenic chemotherapy, including HEC in pediatric patients 1 month to less than 17 years of age is shown in Table 1 .

Warnings & precautions

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Hypersensitivity reactions, including anaphylaxis and anaphylactic shock: reported in patients with or without known hypersensitivity to other selective 5-HT 3 receptor antagonists. If symptoms occur, discontinue palonosetron hydrochloride injection and initiate appropriate medical treatment. ( 5.1 ) Serotonin syndrome: reported with 5-HT 3 receptor antagonists alone, but particularly with concomitant use of serotonergic drugs. ( 5.2 , 7.1 ) 5.1 Hypersensitivity Reactions Hypersensitivity reactions, including anaphylaxis and anaphylactic shock, have been reported with administration of palonosetron hydrochloride injection [see Adverse Reactions ( 6.2 )] . These reactions occurred in patients with or without known hypersensitivity to other 5-HT 3 receptor antagonists. If hypersensitivity reactions occur, discontinue palonosetron hydrochloride injection and initiate appropriate medical treatment. Do not reinitiate palonosetron hydrochloride injection in patients who have previously experienced symptoms of hypersensitivity [see Contraindications ( 4 )] . 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.

Adverse reactions

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Serious or otherwise clinically significant adverse reactions reported in other sections of labeling: Hypersensitivity Reactions [see Warnings and Precautions ( 5.1 )] Serotonin Syndrome [see Warnings and Precautions ( 5.2 )] Most common adverse reactions in chemotherapy-induced nausea and vomiting in adults (greater than or equal to 5%) are: headache and constipation ( 6.1 ) postoperative nausea and vomiting (greater than or equal to 2%) are: QT prolongation, bradycardia, headache, and constipation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Avenacy Inc. at 1-855-283-6229 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. Chemotherapy-Induced Nausea and Vomiting Adults In double-blind randomized clinical trials for the prevention of nausea and vomiting induced by MEC or HEC, 1374 adult patients received a single dose of palonosetron hydrochloride injection, ondansetron (Studies 1 and 3) or dolasetron (Study 2) administered 30 minutes prior to chemotherapy [see Clinical Studies ( 14.1 )] . Adverse reactions were similar in frequency and severity in all 3 treatment groups. Common adverse reactions reported in at least 2% of patients in these trials are shown in Table 2 .

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary There are no available data on palonosetron HCl use in pregnant women to inform a drug-associated risk. In animal reproduction studies, no effects on embryo-fetal development were observed with the administration of oral palonosetron HCl during the period of organogenesis at doses up to 1,894 and 3,789 times the recommended human intravenous dose in rats and rabbits, respectively (see Data ). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In animal reproduction studies, no effects on embryo-fetal development were observed in pregnant rats given oral palonosetron HCl at doses up to 60 mg/kg/day (1,894 times the recommended human intravenous dose based on body surface area) or pregnant rabbits given oral doses up to 60 mg/kg/day (3,789 times the recommended human intravenous dose based on body surface area) during the period of organogenesis.

Pharmacokinetics

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Metabolism
After intravenous dosing of palonosetron HCl in healthy subjects and cancer patients, an initial decline in palonosetron plasma concentrations is followed by a slow elimination from the body. Mean maximum plasma concentration (C max ) and area under the concentration-time curve (AUC 0-∞ ) are generally dose-proportional over the dose range of 0.3 to 90 mcg/kg in healthy subjects and in cancer patients.

Overdosage

Sourced from openFDA

There is no known antidote to palonosetron. Overdose should be managed with supportive care. Dialysis studies have not been performed, however, due to the large volume of distribution, dialysis is unlikely to be an effective treatment for palonosetron overdose. A single intravenous dose of palonosetron HCl at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.

Approval history

Sourced from openFDA
  • Jul 25, 2003NDANDA021372Helsinn Hlthcare
  • Oct 10, 2014NDANDA205718Helsinn Hlthcare
  • Oct 13, 2015ANDAANDA202521Sandoz
  • Mar 1, 2016NDANDA203050Avyxa Holdings
  • Apr 21, 2016ANDAANDA201533Dr Reddys
  • Mar 23, 2018ANDAANDA090713Teva Pharms Usa
  • Apr 19, 2018NDANDA210493Helsinn Hlthcare
  • Sep 19, 2018ANDAANDA204289Sagent Pharms Inc

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
6,197 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Nausea69611%
  2. 2Diarrhoea4357.0%
  3. 3Vomiting4206.8%
  4. 4Fatigue4136.7%
  5. 5Neutropenia3996.4%
  6. 6Febrile Neutropenia3796.1%
  7. 7Off Label Use3766.1%
  8. 8Anaemia3455.6%
  9. 9Death3325.4%
  10. 10Pyrexia3285.3%
  11. 11Dyspnoea3125.0%
  12. 12Decreased Appetite3085.0%
  13. 13Alopecia3014.9%
  14. 14Constipation2504.0%
  15. 15Asthenia2413.9%

Literature

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Recent PubMed references pinned to Palonosetron as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 153 ClinicalTrials.gov registrations naming Palonosetron as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Palonosetron. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • CYP2D6CPIC C (provisional)FDA label: No Clinical PGx

Frequently asked questions

How does Palonosetron work?
Palonosetron is a 5-HT 3 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.
What is Palonosetron used for?
According to FDA labeling, Palonosetron carries indications including: Palonosetron hydrochloride injection is indicated in adults for prevention of: acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). acute nausea and vomiting associated with initial and repeat courses highly emetogenic cancer chemotherapy (HEC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Palonosetron?
Palonosetron is classified as Serotonin (5HT3) antagonists, Serotonin-3 Receptor Antagonist, Serotonin 3 Receptor Antagonists, Serotonin 5HT-3 Antagonists, Decreased Central Nervous System Serotonin Activity, Decreased Peripheral Nervous System Serotonin Activity, Emesis Suppression.
What are the brand names for Palonosetron?
Palonosetron is marketed under brand names including Akynzeo, Posfrea.
What are the contraindications for Palonosetron?
Palonosetron labeling lists contraindications including: Palonosetron hydrochloride injection is contraindicated in patients known to have hypersensitivity to palonosetron [see Warnings and Precautions ( 5.1 )] .. Always consult the full prescribing information and a clinician.
Note. Data for palonosetron is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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