Band P R, Deschamps M, Besner J G, Leclaire R, Gervais P, De Sanctis A
Oncology. 1984;41 Suppl 1:56-9. doi: 10.1159/000225887.
15 patients with metastatic cancer were treated with Lonidamine, a substituted indazole carboxylic acid active against the Lewis lung and Sarcoma 180 tumors. Single doses of 600 mg (350-400 mg/m2) mostly induced somnolence and gastro-intestinal side effects. Toxicity occurring during chronic administration of Lonidamine at doses ranging between 45 and 275 mg/m2 twice daily, mainly consisted of somnolence, myalgias, hyperesthesia and mild hair loss. Myalgias and hyperesthesias were markedly relieved with prednisone 5 mg twice daily. No laboratory abnormalities were seen. In 1 patient with breast cancer resistant to standard chemotherapeutic agents, a 30% reduction of measurable tumor masses was seen. In view of the lack of overlapping toxicity between Lonidamine and other chemotherapeutic drugs, and of its potential activity, it is suggested that phase II studies of Lonidamine be initiated at a dose of 135 mg/m2 twice daily.
15例转移性癌症患者接受了氯尼达明治疗，氯尼达明是一种取代吲唑羧酸，对Lewis肺癌和肉瘤180肿瘤具有活性。单次剂量600mg（350 - 400mg/m²）大多会引起嗜睡和胃肠道副作用。氯尼达明以每日两次、剂量范围在45至275mg/m²进行长期给药时出现的毒性，主要包括嗜睡、肌痛、感觉过敏和轻度脱发。每日两次服用5mg泼尼松可明显缓解肌痛和感觉过敏。未发现实验室异常情况。在1例对标准化疗药物耐药的乳腺癌患者中，可测量的肿瘤肿块缩小了30%。鉴于氯尼达明与其他化疗药物之间不存在重叠毒性，且具有潜在活性，建议以每日两次、135mg/m²的剂量开展氯尼达明的II期研究。
