Summary
In a phase I study of BRL43694A, a 5HT3-receptor antagonist, a single dose of 40 μg/kg was given to 24 patients. All patients received cytostatic treatment expected to cause nausea and vomiting. During the first 24 h, 12 patients were completely protected from nausea and vomiting, 4 experienced nausea and 8 had moderate vomiting; mild headache occurred in 10 patients. No cardiovascular (including ECG) changes took place. Apart from headache, no neurological side effects occurred.
Similar content being viewed by others
References
Addleman M, Erlichman O, Warr D, Fine S, Murray C (1988) Phase I trial of BRL43694, a 5-HT3 antagonist in the prevention of chemotherapy induced nausea and vomiting (Abstract 297). Proc Am Soc Clin Oncol 7: 77
Beecham Pharmaceuticals (March 1988) Clinical Brochure BRL43694A. A novel antiemetic agent
Carmichael J, Cantwell B, Edwards C, Harris AL, Coates P, Thompson S, Rapeport G (1988) Phase I and pharmacokinetic study of BRL43694A selective 5HT3 receptor antagonist: effective control of cisplatin induced emesis (Abstract 1082). Proc Am Soc Clin Oncol 7: 279
Cassidy J, Lewis C, Adams L, Rapeport WG, Zussman BD, Raina V, Soukop M, Kaye SB (1988) Anti-emetic activity and pharmacokinetics of BRL43694A, a selective 5-HT3 antagonist in cancer chemotherapy (Abstract 1418). Proc Am Assoc Clin Res 29: 356
Gumbrell LA, Qualmann C, Perren TJ, Forgeson G, Calvert AH, Thompson S, Rapeport WG (1988) An open pilot study of the 5-HT3 antagonist, BRL43694, an effective antiemetic in refractory highly emetogenic cytotoxic drug induced emesis (Abstract 1149). Proc Am Soc Clin Oncol 7: 296
Joss R, Rohrbach D, Pirovino M, Brunner K, Terrey JP (1988) BRL43694: a novel antiemetic to prevent chemotherapy-induced nausea and vomiting (Abstract 1128). Proc Am Soc Clin Oncol 7: 291
Khojasteh A, Ruble K, Chambers J, Coleman J, Ahmed K (1988) The antiemetic response to GR-C507/75 (GR-38032F) (GR) in patients (Pts) receiving multiple-dose cisplatin (DDP) regimens (Abstract 1159). Proc Am Soc Clin Oncol 7: 298
Kris MG, Gralla RJ, Tyson LB, Clark RA (1988) Phase I and pharmacologic study of the serotonin antagonist GR-C507/75 (GR38032F) when used as an antiemetic (Abstract 1099). Proc Am Soc Clin Oncol 7: 283
Leibundgut U, Rabineau A, Obrecht JP (1988) ICS 205-930: a 5HT3 receptor antagonist to prevent cisplatin-induced emesis (Abstract 1100). Proc Ams Soc Clin Oncol 7: 284
Miner WD, Sanger GJ (1986) Inhibition of cisplatin-induced vomiting by selective 5-hydroxy-tryptamine M-receptor antagonism. Br J Pharmacol 88: 497
Oken MM, Creech RH, Tormey DC, Horton J, Davis TE, McFadden ET, Carbone PP (1982) Toxicity and response criteria of the Eastern Cooperative Oncology Group. Am J Clin Oncol 5: 649
Plezia PM, Davis LE, Alberts DS, Davis A, Garewal HS, Greenberg BR, Smaldone L, Fairchild C (1988) BMY-25801: an effective single agent antiemetic (A) for cisplatin (C)-induced nausea (N) and vomiting (V) (Abstract 1143). Proc Am Soc Clin Oncol 7: 294
Smaldone L, Fairchild C, Rozencweig M, Aapro M, Sartiano G, Plezia P, Alberts D (1988) Dose-range evaluation of BMY-25801, a non dopaminergic antiemetic (Abstract 1086). Proc Am Soc Clin Oncol 7: 280
Stables R, Andrews PLR, Bailey HE, Costall B, Gunning SJ, Hawthorn J, Naylov RJ, Tyes MB (1987) Antiemetic properties of the 5HT3-receptor antagonist, GR38032F. Cancer Treat Rev 14: 333
Zulian G, Selby P, Viner C, Grove M, Patel P, Butcher M, McElwain T (1988) GR38032F (GR) — A safe and effective antiemetic in patients receiving high-dose melphalan (M) (Abstract 1123). Proc Am Soc Clin Oncol 7: 289
Plezia PM, Davis LE, Alberts DS, Davis A, Garewal HS, Greenberg BR, Smaldone L, Fairchild C (1988) BMY-25801: an effective single agent antiemetic (A) for cisplatin (C)-induced nausea (N) and vomiting (V) (Abstract 1143). Proc Am Soc Clin Oncol 7: 294
Smaldone L, Fairchild C, Rozencweig M, Aapro M, Sartiano G, Plezia P, Alberts D (1988) Dose-range evaluation of BMY-25801, a non dopaminergic antiemetic (Abstract 1086). Proc Am Soc Clin Oncol 7: 280
Stables R, Andrews PLR, Bailey HE, Costall B, Gunning SJ, Hawthorn J, Naylov RJ, Tyes MB (1987) Antiemetic properties of the 5HT3-receptor antagonist, GR38032F. Cancer Treat Rev 14: 333
Zulian G, Selby P, Viner C, Grove M, Patel P, Butcher M, McElwain T (1988) GR38032F (GR) — A safe and effective antiemetic in patients receiving high-dose melphalan (M) (Abstract 1123). Proc Am Soc Clin Oncol 7: 289
Author information
Authors and Affiliations
Additional information
Supported by a grant from the National Cancer Association of South Africa
Rights and permissions
About this article
Cite this article
Falkson, G., van Zyl, A.J. A phase I study of a new 5HT3-receptor antagonist, BRL43694A, an agent for the prevention of chemotherapy-induced nausea and vomiting. Cancer Chemother. Pharmacol. 24, 193–196 (1989). https://doi.org/10.1007/BF00300242
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00300242