Dose-ranging evaluation of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic in patients receiving anticancer chemotherapy Journal Article
| Authors: | Kris, M. G.; Gralla, R. J.; Clark, R. A.; Tyson, L. B. |
| Article Title: | Dose-ranging evaluation of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic in patients receiving anticancer chemotherapy |
| 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. |
| Keywords: | cancer chemotherapy; clinical article; cisplatin; doxorubicin; side effect; sedation; cyclophosphamide; xerostomia; ondansetron; antiemetic agent; headache; intravenous drug administration; vertigo; human; priority journal |
| Journal Title: | Journal of Clinical Oncology |
| Volume: | 6 |
| Issue: | 4 |
| ISSN: | 0732-183X |
| Publisher: | American Society of Clinical Oncology |
| Date Published: | 1988-04-01 |
| Start Page: | 659 |
| End Page: | 662 |
| Language: | English |
| DOI: | 10.1200/jco.1988.6.4.659 |
| PUBMED: | 2965755 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Source: Scopus |
Altmetric
Citation Impact
BMJ Impact Analytics
Related MSK Work