Hirano M, Shirakawa S
Gan No Rinsho. 1986 Sep;32(11):1491-4.
Bestrabucil, a chlorambucil-estradiol conjugate known to accumulate in malignant cells irrespective of the presence or absence of estrogen receptor, was administered to a 41-year-old man with follicular lymphoma, medium-sized cell type (LSG classification) stage IV (leukemic). A daily dose of 100 mg was given for two weeks and then 200 mg for a week. The WBC dropped from 43,100/mm3 with 82% abnormal lymphocytes to 12,800/mm3, and the drug was discontinued. It was resumed two weeks later at a daily dose of 50 mg. Four weeks thereafter, complete remission was obtained with the disappearance of all peripheral adenopathies and abnormal cells from the bone marrow. The patient remains disease-free for more than eight months on a maintenance dose of 50 mg per day. Transient erythema and gynecomastia have been the only side effects so far observed.
苯丁酸氮芥,一种已知无论有无雌激素受体均能在恶性细胞中蓄积的苯丁酸氮芥 - 雌二醇共轭物,被用于一名41岁的滤泡性淋巴瘤(中等大小细胞型,LSG分类,IV期(白血病期))男性患者。每日剂量100毫克给药两周,然后200毫克给药一周。白细胞计数从43,100/mm³(异常淋巴细胞占82%)降至12,800/mm³,药物停用。两周后以每日50毫克的剂量恢复用药。此后四周,所有外周淋巴结肿大消失,骨髓中异常细胞消失,实现完全缓解。患者以每日50毫克的维持剂量保持无病状态超过八个月。到目前为止,仅观察到短暂性红斑和男性乳腺增生这两种副作用。