For research use only.

Catalog No.S5740 Synonyms: RS25259, RS 25259 197

Palonosetron Chemical Structure

CAS No. 135729-61-2

Palonosetron is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

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Biological Activity

Description Palonosetron is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
5-HT3 receptor [2]
0.17 nM(Ki)
In vitro

Palonosetron is a 5-HT3 receptor antagonist with a high binding affinity for this receptor and little or no affinity for other receptors[1].

In vivo

Palonosetron has a longer half-life and a higher binding affinity than the first-generation 5-HT3 receptor antagonists. After intravenous dosing of palonosetron in healthy subjects and cancer patients, an initial decline in plasma concentration is followed by a slow elimination from the body. Mean maximum plasma concentration and area under the concentration-time curves are generally dose-proportional over the dose range of 0.3 to 90 μg/kg in healthy subjects and in cancer patients. Palonosetron has a volume of distribution of approximately 8.3 ± 2.5 L/kg and is 62% bound to plasma proteins. It is eliminated from the body through renal excretion and metabolic pathways. The mean terminal elimination half-life is approximately 40 hours[1].


Solubility (25°C)

In vitro DMSO 59 mg/mL (199.04 mM)

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Chemical Information

Molecular Weight 296.41


CAS No. 135729-61-2
Storage powder
in solvent
Synonyms RS25259, RS 25259 197
Smiles C1CC2CN(C(=O)C3=CC=CC(=C23)C1)C4CN5CCC4CC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04486157 Not yet recruiting Drug: IN-A012|Drug: Akynzeo 300Mg-0.5Mg Capsule Healthy HK inno.N Corporation October 2020 Phase 1
NCT03148704 Unknown status Drug: palonosetron hydrochloride capsules Palonosetron Cttq March 8 2017 --
NCT00982995 Terminated Drug: Palonosetron Nausea|Vomiting|Terminally Ill University of Michigan Rogel Cancer Center November 2010 Phase 2
NCT01074697 Completed Drug: Fosaprepitant dimeglumine|Drug: Placebo Nausea|Vomiting|Genital Neoplasms Female Odense University Hospital|Helsinn Healthcare SA April 2010 Phase 3
NCT01046240 Completed Drug: Palonosetron Emesis Clinica Universidad de Navarra Universidad de Navarra October 2009 Phase 1|Phase 2

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5-HT Receptor Signaling Pathway Map

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