Phase I trial of sulofenur (LY186641) given orally on a daily x 21 schedule.
Sulofenur (LY186641), a diarylsulfonylurea, was evaluated clinically utilizing 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. Toxicities included anemia, methemoglobinemia and hemolysis. One patient experienced a fatal subendocardial infarction on the daily x 21 schedule. One partial response was observed in a patient with a sertoli cell tumor on the daily x 5 for 3 weeks schedule. Daily x 5 for 3 weeks is the schedule recommended for phase II trials.
Brown
T D
TD
Duke University Medical Center, Durham, NC 27710.
O'Rourke
T J
TJ
Kuhn
J G
JG
Craig
J B
JB
Havlin
K
K
Burris
H A
HA
Cagnola
J
J
Hamilton
J M
JM
Grindey
G B
GB
Satterlee
W G
WG
D000284:Administration, Oral; D000740:Anemia / Q000139:chemically induced; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002851:Chromatography, High Pressure Liquid; D004334:Drug Administration Schedule; D005260:Female; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D008297:Male; D008708:Methemoglobinemia / Q000139:chemically induced; D008875:Middle Aged; D009369:Neoplasms / Q000188:drug therapy*; D013453:Sulfonylurea Compounds / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D013453:Sulfonylurea Compounds; C058179:sulofenur