Pharmacokinetic evaluation of  ulipristal acetate  for uterine leiomyoma treatment.
BACKGROUND
Progesterone (P), and its receptors (PRs), play a key role in uterine leiomyoma growth. Selective progesterone receptor modulators exert mixed antagonist and agonist effects on the PRs. Mifepristone, a PR-antagonist, reduces leiomyoma volume and related symptoms. Ulipristal acetate (UPA) exerts a potent antiprogestin activity, with less antiglucocorticoid activity compared to mifepristone. This property provides potential advantages for long-term use.


METHODS
This paper focuses on the effect of UPA on leiomyoma's growth and related symptoms in women. The authors also evaluate UPA's efficacy in reducing leiomyoma's size and menorrhagia in Phase II/III trials.


CONCLUSIONS
In the authors' opinion, UPA (5 mg/day) over 3 months can be used to plan the surgery in women with symptomatic leiomyomas. The tolerability and the safety of treatment over a period longer than 3 months have to be evaluated. The results of the follow-up treatment suggest that further studies could successfully evaluate the efficacy and the tolerability of intermittent 3-month courses of treatment.
University of Cagliari, Clinica Ginecologica Ostetrica e di Fisiopatologia della Riproduzione Umana, Via Ospedale 54 Cagliari Sardinia 09124, Italy. gineca.gbmelis@tiscali.it
Gian Benedetto
GB
Melis
Bruno
B
Piras
Maria Francesca
MF
Marotto
Marisa Margherita
MM
Orru'
Giovanni
G
Maricosu
Monica
M
Pilloni
Stefano
S
Guerriero
Marco
M
Angiolucci
Stefano
S
Lello
Anna Maria
AM
Paoletti
D000328:Adult; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D005260:Female; D006727:Hormone Antagonists / Q000627:therapeutic use; D006801:Humans; D007889:Leiomyoma / Q000188:drug therapy* / Q000601:surgery; D008595:Menorrhagia / Q000188:drug therapy; D015735:Mifepristone / Q000627:therapeutic use; D009649:Norpregnadienes / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011374:Progesterone / Q000378:metabolism; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors / Q000378:metabolism; D014594:Uterine Neoplasms / Q000188:drug therapy* / Q000601:surgery
D006727:Hormone Antagonists; D009649:Norpregnadienes; D011980:Receptors, Progesterone; D015735:Mifepristone; D011374:Progesterone; C555622:ulipristal acetate