Inoue K, Wang Y, Shibata H, Mukaiyama T, Hamada K, Ogawa M
Division of Clinical Chemotherapy, Cancer Chemotherapy Center.
Gan To Kagaku Ryoho. 1990 Jan;17(1):85-8.
An analog of diarylsulfonylurea, LY 186641 has a broad spectrum activity against murine solid tumors including Colon 26 and LX-1. Preclinical evaluation of the anticancer activity of LY 186641 using the subrenal capsule assay was performed in fresh human tumor samples derived from 87 patients with various cancers and 70 (80%) samples were evaluable. The overall chemosensitivity rate of LY 186641 was 37% and the average tumor growth inhibition rates (TGIRs) of malignant lymphoma, esophageal cancer and colorectal cancer were 51 +/- 19%, 51 +/- 20% and 48 +/- 12%, respectively. The antitumor effect obtained by LY 186641 was comparable to that of the standard anticancer drugs including adriamycin, 5-fluorouracil and cisplatin evaluated in this assay simultaneously. Based upon these results, LY 186641 is considered to have antitumor activity against some human cancers.
LY 186641是二芳基磺酰脲的类似物，对包括结肠26和LX - 1在内的小鼠实体瘤具有广谱活性。使用肾包膜下测定法对LY 186641的抗癌活性进行临床前评估，该评估在来自87例不同癌症患者的新鲜人肿瘤样本中进行，70份（80%）样本可评估。LY 186641的总体化学敏感性率为37%，恶性淋巴瘤、食管癌和结直肠癌的平均肿瘤生长抑制率（TGIRs）分别为51±19%、51±20%和48±12%。在此测定中同时评估的情况下，LY 186641所获得的抗肿瘤效果与包括阿霉素、5 - 氟尿嘧啶和顺铂在内的标准抗癌药物相当。基于这些结果，LY 186641被认为对某些人类癌症具有抗肿瘤活性。
