GR-205171 (Glaxo Wellcome plc).
Glaxo Wellcome is developing the NK1 antagonist GR-205171 for the potential treatment of chemotherapy- and radiotherapy-induced emesis, post-operative nausea and emesis, and migraine. Phase II trials have commenced for both these indications. GR-205171 has a similar affinity for the NK1 receptor as CP-99994 [176071,193105]. Glaxo anticipates NDA and MAA filings in 2000 [244813]. A trial of GR-205171 in combination with ondansetron demonstrated the combination to be highly effective in the prevention of acute cisplatin-induced emesis. Complete responses were seen in all patients receiving high-dose GR-205171 plus ondansetron. The combination provided complete control of nausea in 16 h in 10 out of 12 patients [289484]. The compound has an ED90 value of 0.03 mg/kg against radiation-induced emesis in the ferret [207316]. GR-205171 is also active against adjuvant-induced inflammatory pain in the rat and may be of potential use in the treatment of chronic inflammatory pain.
Griffiths
N M
NM
DPHD/SARAM, Institut de Protection et de Surete Nucleaire, BP 6 Fontenay aux Roses, F-92265, France. nina.griffths@ipsn.fr