Abstract
Twenty patients receiving a variety of emetogenic cytotoxics (including cisplatin in 5) were given a single i.v. infusion of 40 micrograms kg-1 of BRL43694 (as the hydrochloride salt) in successive groups of 3-4 patients between 0-6 hours after chemotherapy. Eleven patients were completely protected from vomiting; 9 had mild to moderate nausea and vomiting, but none severe enough to require alternative anti-emetic 'rescue'. In 4 of the patients in whom BRL43694 was delayed until 4-6 h after chemotherapy, vomiting had already begun; in each case immediate termination of vomiting occurred when BRL43694 was infused. No adverse effects attributable to the anti-emetic were observed. Mean pharmacokinetic parameters in 14 patients in whom plasma assay data are available were: Maximum observed concentration = 30.7 ng ml-1; terminal phase half-life = 8.96 h; total body clearance = 0.376 (1 h-1) kg-1; apparent volume of distribution = 2.85 l kg-1. This study shows BRL43694 to be an effective and well tolerated anti-emetic. Further studies aimed at defining an optimal dose and schedule for use against the most emetogenic cytotoxics are in progress.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 24 print issues and online access
$259.00 per year
only $10.79 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
Similar content being viewed by others
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Cassidy, J., Raina, V., Lewis, C. et al. Pharmacokinetics and anti-emetic efficacy of BRL43694, a new selective 5HT-3 antagonist. Br J Cancer 58, 651–653 (1988). https://doi.org/10.1038/bjc.1988.278
Issue Date:
DOI: https://doi.org/10.1038/bjc.1988.278
This article is cited by
-
Randomized, double-blind, crossover study of palonosetron compared with granisetron for the prevention of chemotherapy-induced nausea and vomiting in a Chinese population
Medical Oncology (2011)
-
Análisis de coste-efectividad de granisetron en el tratamiento antiemético en oncología
PharmacoEconomics Spanish Research Articles (2008)
-
An open study to assess the safety, tolerance and pharmacokinetics of an intravenous infusion of granisetron given at 3 mg over 30 s in patients receiving chemotherapy for malignant disease
Cancer Chemotherapy and Pharmacology (1995)
-
A dose-finding study of granisetron, a novel antiemetic, in patients receiving high-dose cisplatin
Supportive Care in Cancer (1994)
-
Ondansetron ? a new safe and effective antiemetic in patients receiving high-dose melphalan
Cancer Chemotherapy and Pharmacology (1990)