title: Phase II trial of the novel sulphonylurea sulofenur in advanced breast cancer.
abstract: A total of 18 women with advanced breast cancer were treated with sulofenur [LY186641; N-(5-indanylsulfonyl)-N'-(4-chlorophenyl)-urea], a diarylsulfonylurea that has broad-spectrum activity against a number of murine mammary tumour xenografts. The dosage chosen on the basis of pre-clinical and phase I studies was 700 mg/m2 given orally once daily for 14 days, with treatments being repeated every 3 weeks. There was no response. All patients experienced at least grade 1 anaemia, and two patients developed symptomatic methaemoglobinaemia. Two patients developed grade 4 rises in serum liver-function values along with histological changes consistent with drug-induced toxicity. The mean plasma concentrations of 176 micrograms/ml were lower than the levels required to exert anti-tumour effect in the mouse model.
authors.affiliation: Breast Unit, Royal Marsden Hospital, London, UK.
authors.forename: D C
authors.initials: DC
authors.lastname: Talbot
authors.forename: I E
authors.initials: IE
authors.lastname: Smith
authors.forename: M C
authors.initials: MC
authors.lastname: Nicolson
authors.forename: T J
authors.initials: TJ
authors.lastname: Powles
authors.forename: D
authors.initials: D
authors.lastname: Button
authors.forename: J
authors.initials: J
authors.lastname: Walling
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000097:blood / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008875:Middle Aged; D013453:Sulfonylurea Compounds / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*
chemical_list: D000970:Antineoplastic Agents; D013453:Sulfonylurea Compounds; C058179:sulofenur