Palonosetron

Catalog No.S5740 Synonyms: RS25259, RS 25259 197

For research use only.

Palonosetron (RS25259, RS 25259 197) 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).

Palonosetron Chemical Structure

CAS No. 135729-61-2

Purity & Quality Control

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Biological Activity

Description Palonosetron (RS25259, RS 25259 197) 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).
Targets
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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 59 mg/mL
(199.04 mM)
Ethanol ''-1 mg/mL

Chemical Information

Molecular Weight 296.41
Formula

C19H24N2O

CAS No. 135729-61-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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 Completed Drug: IN-A012|Drug: Akynzeo 300Mg-0.5Mg Capsule Healthy HK inno.N Corporation March 18 2021 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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