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Griffiths NM: GR-205171 (Glaxo Wellcome plc). IDrugs. 1998 Aug;1(4):480-5. 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 ED (90) 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. |
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