Palonosetron

Catalog No.S5740 Synonyms: RS25259, RS 25259 197

Palonosetron Chemical Structure

Molecular Weight(MW): 296.41

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).
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

Solubility (25°C)

In vitro DMSO 59 mg/mL (199.04 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 296.41
Formula

C19H24N2O

CAS No. 135729-61-2
Storage powder
in solvent
Synonyms RS25259, RS 25259 197

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT03817970 Not yet recruiting Nephrotoxicity University of Colorado Denver|Memorial Sloan Kettering Cancer Center|Rutgers University|National Institute of General Medical Sciences (NIGMS) April 25 2019 Not Applicable
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03586817 Recruiting Nausea and Vomiting Postoperative Hospital Federal de Bonsucesso March 2 2019 Phase 4
NCT03578081 Recruiting Malignant Neoplasm Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) October 15 2018 Phase 3
NCT03578081 Recruiting Malignant Neoplasm Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) October 15 2018 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID