Tsukagoshi S
Cancer Institute, Japanese Found for Cancer Res., Toshima, Tokyo.
Gan To Kagaku Ryoho. 1995 Nov;22(13):1991-7.
Fadrozole (CGS 16949 A, brand name: Afema) is an aromatase inhibitor developed firstly in Japan. This compound reduces estrogen levels in the body after administration, suppressing the growth of breast cancer. In animal experiments, this showed an inhibitory activity in vivo against estrogen-depended mammary tumor and the effect was potentiated by the combination of tamoxifen cytrate. In the domestic clinical trials against post-menopausal advanced-recurrent breast cancer, irrespective of the cases with ER positive or negative and even including pretreated cases, the compound showed response rate of 19.3%, the rate of long NC of 18.2%, and the total response rate of 37.5%. The prognosis of NC cases was similar to the effective (CR + PR) cases. The median survival time was 323.5 days which were better than the previous endocrine therapies. The side effects mainly consisted of nausea, vomiting, loss of appetite, abdominal pain, and fatigue, but these were all the level of grade 1. This compound-seemed to be a promising drug for the treatment of patients with post-menopausal breast cancer.
法倔唑（CGS 16949 A，商品名：Afema）是一种最先在日本研发的芳香化酶抑制剂。该化合物给药后可降低体内雌激素水平，抑制乳腺癌生长。在动物实验中，它对雌激素依赖型乳腺肿瘤显示出体内抑制活性，且柠檬酸他莫昔芬联合使用可增强其效果。在针对绝经后晚期复发性乳腺癌的国内临床试验中，无论雌激素受体（ER）阳性或阴性病例，甚至包括经预处理的病例，该化合物的有效率为19.3%，长程稳定（NC）率为18.2%，总有效率为37.5%。NC病例的预后与有效（完全缓解+部分缓解）病例相似。中位生存时间为323.5天，优于以往的内分泌治疗。副作用主要包括恶心、呕吐、食欲不振、腹痛和疲劳，但均为1级。该化合物似乎是治疗绝经后乳腺癌患者的一种有前景的药物。
