Studies on the effect of the new non-steroidal aromatase inhibitor fadrozole hydrochloride in an endometriosis model in rats. 1996

S Yano, and Y Ikegami, and K Nakao
Drug Discovery Research Unit, Ciba-Geigy Japan Ltd., Takarazuka, Japan.

The therapeutic effect of the new nonsteroidal aromatase inhibitor fadrozole hydrochloride (4-(5,6,7,8-tetrahydro-imidazo[1,5a]pyridin-5-yl)benzonitrile monohydrochloride, fadrozole, CAS 102676-31-3, CGS16949A) was assessed using a surgically induced endometriosis model in rats. In nontreated rats, the endometrial transplants on the abdominal wall developed large cysts with fluid. In the fadrozole treated group, the cystic volume of the transplants decreased in a dose-dependent manner. The weights of the hemi-uteri were markedly reduced by fadrozole treatment. Fadrozole produced a dose-dependent increase in percentage of vaginal diestrous days. In ovariectomized group, the growth of the transplants was also suppressed, and the weights of the hemi-uteri decreased markedly. Histologically, the signs of growth suppression and/or atrophic changes such as minimization of luminal size, cuboidal piknotic epithelium and/or contraction of stroma were observed in ovariectomized or fadrozole treated groups. The right uterine horns also showed marked atrophic changes as with the transplants. The present study strongly indicates that the new selective aromatase inhibitor fadrozole should be useful for the treatment of endometriosis.

UI MeSH Term Description Entries
D010052 Ovariectomy The surgical removal of one or both ovaries. Castration, Female,Oophorectomy,Bilateral Ovariectomy,Bilateral Ovariectomies,Castrations, Female,Female Castration,Female Castrations,Oophorectomies,Ovariectomies,Ovariectomies, Bilateral,Ovariectomy, Bilateral
D004715 Endometriosis A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum. Endometrioma,Endometriomas,Endometrioses
D004717 Endometrium The mucous membrane lining of the uterine cavity that is hormonally responsive during the MENSTRUAL CYCLE and PREGNANCY. The endometrium undergoes cyclic changes that characterize MENSTRUATION. After successful FERTILIZATION, it serves to sustain the developing embryo. Endometria
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D005260 Female Females
D006728 Hormones Chemical substances having a specific regulatory effect on the activity of a certain organ or organs. The term was originally applied to substances secreted by various ENDOCRINE GLANDS and transported in the bloodstream to the target organs. It is sometimes extended to include those substances that are not produced by the endocrine glands but that have similar effects. Hormone,Hormone Receptor Agonists,Agonists, Hormone Receptor,Receptor Agonists, Hormone
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D017316 Fadrozole A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer. CGS 020286A,CGS-020286A,CGS-16949A,CGS020286A,FAD 286,FAD-286,FAD286,Fadrozole Hydrochloride,Fadrozole Monohydrochloride,CGS 16949A,CGS16949A,Hydrochloride, Fadrozole,Monohydrochloride, Fadrozole
D047072 Aromatase Inhibitors Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones. Aromatase Inhibitor,Inhibitor, Aromatase,Inhibitors, Aromatase

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