PHASE-I TRIAL OF ERBULOZOLE (R55104)

Erbulozole (R55 104) is a water soluble congener of the microtubule in hibitor tubulozole, which has proven possess anti-invasive, antitumora l and radiosensitizing capacities. A dose-finding study was performed on respectively 9 patients (every three weeks; doses ranging from 20 m g/m(2) to 100 mg/m(2); maximum 2 cycles per patient) and 6 patients (w eekly; doses ranging from 20 mg/m(2) to 50 mg/m(2); maximum 60 cycles per patient). At all dosages, hematological and biochemical toxicity w as very limited. Seven patients complained of pain at the tumor site ( grade I to III). Dose limiting toxicity appeared at respectively 100 m g/m(2) (one administration every three weeks) and 50 mg/m(2) (weekly a dministration). At this level, 2 patients displayed a dose-limiting We rnicke's encephalopathy-like syndrome. Other secondary effects were he adache, fever, exacerbation of dyspnea and moderate nausea and vomitin g.