Dose-ranging evaluation of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic in patients receiving anticancer chemotherapy

M. G. Kris, Richard J. Gralla, R. A. Clark, L. B. Tyson

Research output: Contribution to journalArticle

89 Citations (Scopus)

Abstract

GR-C507/75 (GR38032F) antagonizes the 5-HT3 (serotonin) receptor and prevents cisplatin-induced emesis in animals. In this dose-ranging trial, 44 patients with cancer receiving chemotherapy known to produce nausea and vomiting (including cisplatin, cyclophosphamide, and doxorubicin) received three intravenous (IV) infusions of GR-C507/75 every two hours beginning 30 minutes before chemotherapy. Ten dosage levels were explored, ranging from 0.04 mg/kg to 0.35 mg/kg in each of the three infusions. Toxicities were mild and included sedation, dizziness, headache, transient elevations of SGOT or alanine aminotransferase (ALT), and dry mouth. No akathisia or acute dystonic reactions were observed. Antiemetic effects were seen in patients receiving cisplatin at 120 mg/m2. GR-C507/75 can be safely administered on this schedule at IV dosages up to 0.35 mg/kg in patients receiving chemotherapy. Further studies of this agent at higher dosages and by different schedules are appropriate.

Original languageEnglish (US)
Pages (from-to)659-662
Number of pages4
JournalJournal of Clinical Oncology
Volume6
Issue number4
StatePublished - 1988
Externally publishedYes

Fingerprint

Ondansetron
Serotonin Antagonists
Antiemetics
Cisplatin
Drug Therapy
Vomiting
Appointments and Schedules
Receptors, Serotonin, 5-HT3
Psychomotor Agitation
Dizziness
Aspartate Aminotransferases
Alanine Transaminase
Intravenous Infusions
Doxorubicin
Cyclophosphamide
Nausea
Headache
Mouth
Neoplasms

ASJC Scopus subject areas

  • Cancer Research
  • Oncology

Cite this

Dose-ranging evaluation of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic in patients receiving anticancer chemotherapy. / Kris, M. G.; Gralla, Richard J.; Clark, R. A.; Tyson, L. B.

In: Journal of Clinical Oncology, Vol. 6, No. 4, 1988, p. 659-662.

Research output: Contribution to journalArticle

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