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Abstract
BackgroundPalonosetron is a potent second generation 5- hydroxytryptamine-3 selective antagonist which can be administered by either intravenous (IV) or oral routes, but subcutaneous (SC) administration of palonosetron has never been studied, even though it could have useful clinical applications. In this study, we evaluate the bioavailability of SC palonosetron.Patients and MethodsPatients treated with platinum-based chemotherapy were randomized to receive SC or IV palonosetron, followed by the alternative route in a crossover manner, during the first two cycles of chemotherapy. Blood samples were collected at baseline and 10, 15, 30, 45, 60, 90 minutes and 2, 3, 4, 6, 8, 12 and 24 h after palonosetron administration. Urine was collected during 12 hours following palonosetron. We compared pharmacokinetic parameters including AUC0–24h, t1/2, and Cmax observed with each route of administration by analysis of variance (ANOVA).ResultsFrom October 2009 to July 2010, 25 evaluable patients were included. AUC0–24h for IV and SC palonosetron were respectively 14.1 and 12.7 ng × h/ml (p = 0.160). Bioavalability of SC palonosetron was 118% (95% IC: 69–168). Cmax was lower with SC than with IV route and was reached 15 minutes following SC administration.ConclusionsPalonosetron bioavailability was similar when administered by either SC or IV route. This new route of administration might be specially useful for outpatient management of emesis and for administration of oral chemotherapy. Trial Registration ClinicalTrials.gov NCT01046240
Highlights
Emesis remains one of the most relevant side effects of chemotherapy
Palonosetron bioavailability was similar when administered by either SC or IV route. This new route of administration might be specially useful for outpatient management of emesis and for administration of oral chemotherapy
It induces a decrease in health-related quality of life and it is often underestimated by physicians [1,2]. 5hydroxytryptamine-3 (5-HT3) inhibitors are universally recommended as part of standard anti-emetic premedication for moderate and highly emetogenic chemotherapy agents [3,4]
Summary
Emesis remains one of the most relevant side effects of chemotherapy. It induces a decrease in health-related quality of life and it is often underestimated by physicians [1,2]. 5hydroxytryptamine-3 (5-HT3) inhibitors are universally recommended as part of standard anti-emetic premedication for moderate and highly emetogenic chemotherapy agents [3,4]. Palonosetron (Aloxi; Italfarmaco Laboratories,) is a potent and highly selective 5-HT3 inhibitor with a prolonged half-life (40 hours), which has up to 30 times higher affinity for the receptor than first-generation 5-HT3 antagonists. It has weak antagonistic action against other 5-HT receptors [5]. Palonosetron, as the other 5-HT3 antagonists, can be administered by oral or intravenous (IV) route. Palonosetron is a potent second generation 5- hydroxytryptamine-3 selective antagonist which can be administered by either intravenous (IV) or oral routes, but subcutaneous (SC) administration of palonosetron has never been studied, even though it could have useful clinical applications. We evaluate the bioavailability of SC palonosetron
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