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Palonosetron as an anti-emetic and anti-nausea agent in oncology.

Aapro MS - Ther Clin Risk Manag (2007)

Bottom Line: Palonosetron (Aloxi(®), Onicit(®), Paloxi(®)) is a second-generation 5-HT(3) receptor antagonist (RA) with an extended half-life of ~40 hours and high binding affinity for the 5-HT₃ receptor that is markedly different from other 5-HT(3) RAs.Recent research has focused on optimization of palonosetron-based antiemetic regimens, particularly in combination with steroids and neurokinin-1 RAs.The available clinical data indicate high control rates for palonosetron, suggesting a synergistic potential for protection in patients scheduled to receive emetogenic drug regimens.

View Article: PubMed Central - PubMed

Affiliation: Clinique de Genolier Genolier, Switzerland. maapro@genolier.net

ABSTRACT
Palonosetron (Aloxi(®), Onicit(®), Paloxi(®)) is a second-generation 5-HT(3) receptor antagonist (RA) with an extended half-life of ~40 hours and high binding affinity for the 5-HT₃ receptor that is markedly different from other 5-HT(3) RAs. Phase III trials demonstrate that a single dose of palonosetron compared with traditional 5-HT₃ RAs is more effective in preventing chemotherapy-induced nausea and vomiting (CINV) during the first 24 hours following chemotherapy (acute CINV), and also exhibits prolonged efficacy to provide significantly better protection from CINV in the delayed and overall phases. This superior and extended protection from CINV conferred by palonosetron following a single intravenous dose before chemotherapy simplifies dosing schedules. Recent research has focused on optimization of palonosetron-based antiemetic regimens, particularly in combination with steroids and neurokinin-1 RAs. The available clinical data indicate high control rates for palonosetron, suggesting a synergistic potential for protection in patients scheduled to receive emetogenic drug regimens.

No MeSH data available.


Related in: MedlinePlus

Molecular structure of palonosetron hydrochloride.
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fig3: Molecular structure of palonosetron hydrochloride.

Mentions: Palonosetron (Figure 3) is the first 5-HT3 RA to show an efficacy that is superior to other 5-HT3 RAs against CINV due to MEC in FDA registration trials (Eisenberg et al 2003; Gralla et al 2003; Rubenstein et al 2003). It was first approved by the FDA in 2003 and is currently licensed in the USA for the prevention of acute nausea and vomiting associated with MEC and HEC, and the prevention of delayed nausea and vomiting associated with MEC. More recently, palonosetron has gained approval in Europe for the prevention of acute nausea and vomiting associated with HEC, and the prevention of nausea and vomiting associated with MEC. It is postulated that the superior clinical efficacy of palonosetron, including the control of delayed CINV following a single dose prior to chemotherapy, can be related to the >30-fold higher binding affinity for the 5-HT3 receptor subtype and a 4–10-fold longer half-life compared to first-generation 5-HT3 RAs (Eisenberg, Figueroa-Vadillo et al 2003; Grunberg et al 2003). Despite having a longer half-life and higher binding affinity, however, palonosetron has a similar tolerability profile to the first-generation 5-HT3 RAs, demonstrating minimal side effects. Headache and constipation are the most commonly reported adverse events for both generations of 5-HT3 RAs (Hesketh et al 1996; Eisenberg, Figueroa-Vadillo et al 2003; Eisenberg, Rubenstein et al 2003; Gralla et al 2003; Grunberg et al 2003; Rubenstein et al 2003).


Palonosetron as an anti-emetic and anti-nausea agent in oncology.

Aapro MS - Ther Clin Risk Manag (2007)

Molecular structure of palonosetron hydrochloride.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2387285&req=5

fig3: Molecular structure of palonosetron hydrochloride.
Mentions: Palonosetron (Figure 3) is the first 5-HT3 RA to show an efficacy that is superior to other 5-HT3 RAs against CINV due to MEC in FDA registration trials (Eisenberg et al 2003; Gralla et al 2003; Rubenstein et al 2003). It was first approved by the FDA in 2003 and is currently licensed in the USA for the prevention of acute nausea and vomiting associated with MEC and HEC, and the prevention of delayed nausea and vomiting associated with MEC. More recently, palonosetron has gained approval in Europe for the prevention of acute nausea and vomiting associated with HEC, and the prevention of nausea and vomiting associated with MEC. It is postulated that the superior clinical efficacy of palonosetron, including the control of delayed CINV following a single dose prior to chemotherapy, can be related to the >30-fold higher binding affinity for the 5-HT3 receptor subtype and a 4–10-fold longer half-life compared to first-generation 5-HT3 RAs (Eisenberg, Figueroa-Vadillo et al 2003; Grunberg et al 2003). Despite having a longer half-life and higher binding affinity, however, palonosetron has a similar tolerability profile to the first-generation 5-HT3 RAs, demonstrating minimal side effects. Headache and constipation are the most commonly reported adverse events for both generations of 5-HT3 RAs (Hesketh et al 1996; Eisenberg, Figueroa-Vadillo et al 2003; Eisenberg, Rubenstein et al 2003; Gralla et al 2003; Grunberg et al 2003; Rubenstein et al 2003).

Bottom Line: Palonosetron (Aloxi(®), Onicit(®), Paloxi(®)) is a second-generation 5-HT(3) receptor antagonist (RA) with an extended half-life of ~40 hours and high binding affinity for the 5-HT₃ receptor that is markedly different from other 5-HT(3) RAs.Recent research has focused on optimization of palonosetron-based antiemetic regimens, particularly in combination with steroids and neurokinin-1 RAs.The available clinical data indicate high control rates for palonosetron, suggesting a synergistic potential for protection in patients scheduled to receive emetogenic drug regimens.

View Article: PubMed Central - PubMed

Affiliation: Clinique de Genolier Genolier, Switzerland. maapro@genolier.net

ABSTRACT
Palonosetron (Aloxi(®), Onicit(®), Paloxi(®)) is a second-generation 5-HT(3) receptor antagonist (RA) with an extended half-life of ~40 hours and high binding affinity for the 5-HT₃ receptor that is markedly different from other 5-HT(3) RAs. Phase III trials demonstrate that a single dose of palonosetron compared with traditional 5-HT₃ RAs is more effective in preventing chemotherapy-induced nausea and vomiting (CINV) during the first 24 hours following chemotherapy (acute CINV), and also exhibits prolonged efficacy to provide significantly better protection from CINV in the delayed and overall phases. This superior and extended protection from CINV conferred by palonosetron following a single intravenous dose before chemotherapy simplifies dosing schedules. Recent research has focused on optimization of palonosetron-based antiemetic regimens, particularly in combination with steroids and neurokinin-1 RAs. The available clinical data indicate high control rates for palonosetron, suggesting a synergistic potential for protection in patients scheduled to receive emetogenic drug regimens.

No MeSH data available.


Related in: MedlinePlus