title: A new aromatase inhibitor, FR901537. II. Pharmacological and antitumor effects.
abstract: The pharmacological and antitumor effects of FR901537, a new aromatase inhibitor, isolated from Bacillus sp. No. 3072, were studied. Treatment for four consecutive days with FR901537 inhibited the androstenedione-induced increase in the uterus weight in immature rats. FR901537 had no effect on the uterus, adrenal glands, ovary or pituitary weights in mature rats following 14 days of treatment. The antitumor activity of FR901537 on 7,12-dimethylbenz(a)anthracene-induced mammary tumors was studied in ovariectomized, testosterone propionate (TP)-treated rats as a postmenopausal tumor model. Ovariectomy caused the regression of the mammary tumors and the growth of tumors was remarkably stimulated following TP treatment. Further, in the rats treated with FR901537 and TP, the TP-induced tumor growth was significantly inhibited by FR901537. These results suggest that FR901537 is a promising drug in the treatment of estrogen-dependent mammary tumors in postmenopausal women.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Oohata
authors.forename: I
authors.initials: I
authors.lastname: Kawamura
authors.forename: E
authors.initials: E
authors.lastname: Lacey
authors.forename: F
authors.initials: F
authors.lastname: Nishigaki
authors.forename: S
authors.initials: S
authors.lastname: Matsumoto
authors.forename: S
authors.initials: S
authors.lastname: Tsujimoto
authors.forename: Y
authors.initials: Y
authors.lastname: Naoe
authors.forename: T
authors.initials: T
authors.lastname: Manda
authors.forename: K
authors.initials: K
authors.lastname: Shimomura
mesh_terms: D000616:Aminoglutethimide / Q000494:pharmacology; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology / Q000627:therapeutic use*; D047072:Aromatase Inhibitors; D001407:Bacillus; D001835:Body Weight / Q000187:drug effects; D005260:Female; D008325:Mammary Neoplasms, Experimental / Q000188:drug therapy*; D015394:Molecular Structure; D009929:Organ Size / Q000187:drug effects; D010204:Pantetheine / Q000031:analogs & derivatives* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000903:Antibiotics, Antineoplastic; D047072:Aromatase Inhibitors; D000616:Aminoglutethimide; C096595:FR 901537; D010204:Pantetheine