Giudici D, Ornati G, Briatico G, Buzzetti F, Lombardi P, di Salle E
Farmitalia C. Erba, R.&D./Oncology, Nerviano (MI), Italy.
J Steroid Biochem. 1988;30(1-6):391-4. doi: 10.1016/0022-4731(88)90129-x.
FCE 24304 (6-methylenandrosta-1,4-diene-3,17-dione), a new irreversible aromatase inhibitor, has been identified and characterized in vitro and in vivo. The compound caused time-dependent inactivation of human placental aromatase with a t1/2 of 13.9 min and ki of 26 nM. When tested in PMSG-treated rats, ovarian aromatase activity was reduced 24 h after dosing by both the s.c. (ED50 1.8 mg/kg) and the oral (ED50 3.7 mg/kg) routes. No interference with 5 alpha-reductase activity nor any significant binding affinity for estrogen receptor was found. Slight binding affinity for the androgen receptor (RBA 0.2% of DHT) was observed.
