PHASE-I TRIAL OF SULOFENUR (LY186641) GIVEN ORALLY ON A DAILY X 21 SCHEDULE

Sulofenur (LY186641), a diarylsulfonylurea, was evaluated clinically u tilizing either a daily x 21 schedule or a daily x 5 (with 2 days off) for 3 weeks schedule. Eighteen patients with refractory solid tumors received 47 evaluable courses of sulofenur given p.o. daily x 21 every 28 days at five dose levels while 14 received 29 courses of sulofenur given daily x 5 for 3 weeks every 28 days at three dose levels. Toxic ities included anemia, methemoglobinemia and hemolysis. One patient ex perienced a fatal subendocardial infarction on the daily x 21 schedule . One partial response was observed in a patient with a sertoli cell t umor on the daily x 5 for 3 weeks schedule. Daily x 5 for 3 weeks is t he schedule recommended for phase II trials.