口服舒洛菲尼（LY186641），每日一次，连续21天的I期试验。

Phase I trial of sulofenur (LY186641) given orally on a daily x 21 schedule.

作者信息

Brown T D, O'Rourke T J, Kuhn J G, Craig J B, Havlin K, Burris H A, Cagnola J, Hamilton J M, Grindey G B, Satterlee W G

机构信息

Duke University Medical Center, Durham, NC 27710.

出版信息

Anticancer Drugs. 1994 Apr;5(2):151-9. doi: 10.1097/00001813-199404000-00005.

DOI:10.1097/00001813-199404000-00005

PMID:8049498

Abstract

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.

摘要

舒洛芬脲（LY186641），一种二芳基磺酰脲，采用每日一次共21天的给药方案或每日一次共5天（休息2天）持续3周的给药方案进行了临床评估。18例难治性实体瘤患者接受了47个可评估疗程的舒洛芬脲治疗，口服给药，每28天每日一次共21天，分五个剂量水平；14例患者接受了29个疗程的舒洛芬脲治疗，每28天每日一次共5天持续3周，分三个剂量水平。毒性包括贫血、高铁血红蛋白血症和溶血。1例患者在每日一次共21天的给药方案中发生致命性心内膜下梗死。1例患有支持细胞瘤的患者在每日一次共5天持续3周的给药方案中出现部分缓解。每日一次共5天持续3周是推荐用于II期试验的给药方案。