RU54115, a tight-binding aromatase inhibitor potentially useful for the treatment of breast cancer.

Abstract

RU54115 is a new potent inhibitor of aromatase. In vitro, it inhibits the enzyme from human placental microsomes with a Ki of 0.5 nM, which places it among the tightest reported steroidal inhibitors of aromatase. In vivo, it lowers the amount of circulating estradiol in pregnant mare serum gonadotrophin (PMSG)-primed female rats with an ED50 of 0.4 mg/kg when given s.c. and 4 mg/kg when given orally. An oral dose of 25 mg/kg when given once daily to female rats was able to inhibit the growth of DMBA-induced mammary tumors.

• Authors: C Delaisi, B Doucet, C Hartmann, B Tric, J F Gourvest, D Lesuisse
• Journal: The Journal of steroid biochemistry and molecular biology (J Steroid Biochem Mol Biol) Vol. 41 Issue 3-8 Pg. 773-7 (Mar 1992) ISSN: 0960-0760 [Print] England
• PMID: 1562553 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Aromatase Inhibitors
• Estrenes
• Estrogen Antagonists
• Gonadotropins, Equine
• 10-methylthioethyl estra-4,9(11)-diene 3,17-dione
• Estradiol
• 9,10-Dimethyl-1,2-benzanthracene

Topics

• 9,10-Dimethyl-1,2-benzanthracene
• Animals
• Antineoplastic Agents (pharmacology, therapeutic use)
• Aromatase Inhibitors
• Breast Neoplasms (drug therapy)
• Estradiol (blood)
• Estrenes (pharmacology, therapeutic use)
• Estrogen Antagonists (pharmacology)
• Female
• Gonadotropins, Equine (pharmacology)
• Humans
• Kinetics
• Mammary Neoplasms, Experimental (chemically induced, drug therapy)
• Microsomes (enzymology)
• Molecular Structure
• Placenta (enzymology)
• Pregnancy
• Rats
• Rats, Inbred Strains