Kuttenn F, Mauvais-Jarvis P
C R Acad Sci III. 1985;300(12):457-62.
(3H)-4 hydroxytamoxifen (4O H Tam), the active metabolite of the antiestrogen tamoxifen (Tam) was dissolved in ethanol and locally percutaneously administered on 4 human breast carcinomas before surgery. 12, 24, 72 hrs. and 7 days later, (3H)-4O H Tam was recovered in cytosol and nuclear fractions of the tumor. Only traces of radioactivity were recovered in plasma. From these results it appears clearly that the percutaneous administration of 4O H Tam on the mammary gland yields a local antiestrogen effect without the systemic effects observed in case of oral administration of Tam.
抗雌激素他莫昔芬（Tam）的活性代谢产物（3H）-4-羟基他莫昔芬（4OH Tam）溶解于乙醇中，在手术前对4例人类乳腺癌进行局部经皮给药。12小时、24小时、72小时和7天后，在肿瘤的胞质溶胶和核级分中回收了（3H）-4OH Tam。血浆中仅回收了微量放射性物质。从这些结果可以清楚地看出，在乳腺上经皮给予4OH Tam会产生局部抗雌激素作用，而没有口服给予Tam时观察到的全身作用。
