Vogel C L, Denefrio J M, Padgett D C, Silverman M A
Cancer Treat Rep. 1980 Oct-Nov;64(10-11):1153-6.
In a phase I trial, 2,3-dihydro-1H-imidazo[1,2-b]pyrazole was administered iv weekly at doses ranging from 0.1 to 3.0 g/m2/wk to patients with refractory metastatic solid tumors. Although gastrointestinal toxicity was tolerable and neither granulocyte nor platelet toxicity was seen, significant dose-limiting hemolysis was encountered at doses of 1.5 g/m2/wk. While no definite tumor regressions were seen in the 32 patients evaluable for response, two patients (squamous cell carcinoma of lung and tonsil) had clinically useful improvement.
在一项I期试验中，对难治性转移性实体瘤患者静脉注射2,3-二氢-1H-咪唑并[1,2-b]吡唑，剂量为0.1至3.0 g/m²/周，每周一次。尽管胃肠道毒性可以耐受，且未观察到粒细胞或血小板毒性，但在剂量为1.5 g/m²/周时出现了显著的剂量限制性溶血。在可评估反应的32例患者中，虽然未观察到明确的肿瘤消退，但有两名患者（肺癌和扁桃体鳞状细胞癌）有临床有用的改善。
