ZK 119.010

ZK 119.010 is a **novel non-steroidal pure antiestrogen** developed for the treatment of estrogen-sensitive diseases. It is structurally distinct from steroidal antiestrogens and is classified as a nonsteroidal estrogen receptor antagonist. ZK 119.010 has **strong antioestrogenic effects** with only marginal intrinsic estrogenic activity in rats and mice, making it a "pure" antagonist in contrast to agents with mixed agonist/antagonist profiles such as tamoxifen. It binds to **estrogen receptors** (ER), inhibiting estrogen-induced proliferation and trophic effects, including uterotrophic and vaginotrophic responses. Unlike tamoxifen, ZK 119.010 showed greater efficacy in suppressing growth and metastasis of estrogen-dependent endometrial carcinoma in animal models, without measurable estrogenic stimulation in the endometrium or uterine tissues. ZK 119.010 does not significantly alter estrogen receptor levels in tumors, in contrast to tamoxifen, which caused receptor depletion along with its partial agonist effects. The compound was developed by **Schering AG** (Berlin, Germany). Its primary indication is experimental treatment of estrogen-dependent tumors, especially **endometrial carcinoma**. It has also served as a tool compound in research related to estrogen receptor pharmacology and modulation of IGF-I–induced cell proliferation[1][3][5][6][10].

Other names

2-(4-hydroxyphenyl)-3-methyl-1-[6-(1-pyrrolidinyl)-hexyl]-indol-5-ol