Endocrine changes with the aromatase inhibitor @entity2628 in XXXX .

@entity1 @entity1369 @entity2628 @entity0 @entity19517 @entity2931 @entity1372 @entity53 @entity4418 @entity7042 @entity972 @entity2671
@entity2628 is a potent aromatase inhibitor with proven clinical effectiveness. However, its optimal dose and its effects on serum @entity1369 levels/electrolyte balance have been disputed. To resolve these issues, a double-blind randomised endocrine study of three doses of @entity2628 [0.5 mg twice daily (bd); 1.0 mg bd; 2.0 mg bd] was conducted in 80 (68 evaluable) postmenopausal @entity1 with @entity0 over a period of 3 months. There were substantial falls in the serum levels of @entity53 , @entity7042 and @entity19517 . For @entity7042 only, there was a significant effect of dose (on-treatment means: 0.5 mg, 38.0 pmol/l; 1.0 mg, 25.0 pmol/l; 2.0 mg, 23.9 pmol/l). All @entity2931 showed a similar pattern in relation to time, with the 3-month mean being higher than those at 1 and 2 months, and this was significant for @entity53 (P = 0.012). There was an indication that complete suppression of @entity53 and @entity7042 was not maintained throughout the 12-h dosing period, but the data and its interpretation are complicated by a minor diurnal rhythm in these parameters. There were significant increases in @entity4418 and @entity2671 which may be due to a block of 11 beta-hydroxylase. There was a statistically non-significant fall in @entity1369 levels (P = 0.06) during treatment (median pretreatment, 446 pmol/l; median decrease, 125 pmol/l). However, the concurrent significant fall in the plasma @entity1372 : @entity972 ratio indicated that changes in @entity1369 secretion did occur. None of these effects on adrenal pathways was of a degree which is likely to have clinically relevant consequences. It is concluded that @entity2628 achieves near maximal suppression of @entity2931 at 1 mg bd, and that its effects on @entity1369 synthesis are unlikely to be of clinical significance.
