GR-205171 (Glaxo Wellcome plc).

Abstract

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.

• Authors: N M Griffiths
• Journal: IDrugs : the investigational drugs journal (IDrugs) Vol. 1 Issue 4 Pg. 480-5 (Aug 1998) ISSN: 1369-7056 [Print] England
• PMID: 18465582 (Publication Type: Journal Article)