GR 38032F (GR-C507/75): A novel compound effective in the prevention of acute cisplatin-induced emesis

P. J. Hesketh, W. K. Murphy, E. P. Lester, David R Gandara, A. Khojasteh, E. Tapazoglou, G. P. Sartiano, Ralph W deVere White, K. Werner, J. M. Chubb

Research output: Contribution to journalArticlepeer-review

95 Scopus citations


We evaluated, in a multi-center trial, the safety and efficacy of GR 38032F (GR-C507/75), a novel and selective serotonin antagonist, in preventing acute emesis in chemotherapy-naive patients receiving treatment with regimens containing high-dose cisplatin (≥ 100 mg/m2). Eighty-five patients were randomized to receive GR 38032F, 0.18 mg/kg, either every six or every eight hours for three doses, beginning 30 minutes before cisplatin. Patients wre evaluated for emetic episodes (vomiting or retching) over a 24-hour period following cisplatin. All patients were evaluable for toxicity and 83 were evaluable for efficacy. The overall antimetic response rate was 75% (55% complete response [CR], 20% major response). No difference in antiemetic control between the two administration schedules was noted. Patients with histories of heavy ethanol use had significantly better antimetic control (74% CR) than modest or non-drinkers (33% CR). Toxicity of GR 38032F was modest and independent of administration schedule. The most common adverse events included mild hepatic transaminase elevations, self-limited diarrhea dry mouth, headache, and mild sedation. Our data indicate that GR 38032F is a safe and effective agent in the control of acute cisplatin-induced nausea and vomiting. Additional trials exploring dosing, schedule, and comparison to standard antiemetic agents are indicated.

Original languageEnglish (US)
Pages (from-to)700-705
Number of pages6
JournalJournal of Clinical Oncology
Issue number6
StatePublished - 1989
Externally publishedYes

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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