Müntzing J, Kirdani R Y, Saroff J, Murphy G P, Sandberg A A
Urology. 1977 Nov;10(5):439-45. doi: 10.1016/0090-4295(77)90131-5.
Estracyt (estramustine phosphate) injected intraperitoneally, 100 mg, per Kg. three days a week for four weeks, retarded growth of the R-3327 tumor in intact rats and in orchiectomized rats given androgen. The growth inhibition was accomplished by reduction of tumor deoxyribonucleic acid concentration and of the activities of acid phosphatase, leucine aminopeptidase, and other hydrolases. Histologic examination revealed cellular necrosis particularly prominent in the orchiectomized, androgen-treated rats. Estracyt did not affect the uptake of 65-Zn in the tumors but markedly reduced the high uptake in the dorsolateral prostate. There was no accumulation of 3H or 14C in the tumors after intravenous administration of 3H, 14C-labeled Estracyt, but the isotope concentrations decreased much in the same way as they decreased in the dorsolateral prostate. The isotopes were retained in the ventral prostate, where their concentrations were approximately twenty times higher than those in the muscle four hours after injection. The results demonstrate the value of the R-3327 tumor in the evaluation of drugs of potential clinical use for the treatment of prostatic cancer. The results also show that Estracyt has an antitumor effect which is not dependent on the antigonadotropic action of the drug.
癌腺治（磷酸雌莫司汀）以每千克100毫克的剂量每周三天腹腔注射，持续四周，可抑制完整大鼠和接受雄激素治疗的去势大鼠体内R-3327肿瘤的生长。这种生长抑制是通过降低肿瘤脱氧核糖核酸浓度以及酸性磷酸酶、亮氨酸氨肽酶和其他水解酶的活性来实现的。组织学检查显示，细胞坏死在接受雄激素治疗的去势大鼠中尤为明显。癌腺治不影响肿瘤对65锌的摄取，但显著降低了背外侧前列腺的高摄取。静脉注射3H、14C标记的癌腺治后，肿瘤中没有3H或14C的积累，但同位素浓度的下降方式与背外侧前列腺相同。同位素保留在腹侧前列腺中，注射后四小时其浓度比肌肉中的浓度高约二十倍。结果证明了R-3327肿瘤在评估前列腺癌潜在临床治疗药物方面的价值。结果还表明，癌腺治具有抗肿瘤作用，且该作用不依赖于药物的抗促性腺作用。
