Skip Navigation


Hum. Reprod. Advance Access originally published online on January 21, 2005
Human Reproduction 2005 20(4):1090-1099; doi:10.1093/humrep/deh738
This Article
Right arrow Full Text Freely available
Right arrow FREE Full Text (PDF ) Freely available
Right arrow All Versions of this Article:
20/4/1090    most recent
deh738v1
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in ISI Web of Science
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrow Search for citing articles in:
ISI Web of Science (22)
Right arrowRequest Permissions
Google Scholar
Right arrow Articles by Chwalisz, K.
Right arrow Articles by Larsen, L.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Chwalisz, K.
Right arrow Articles by Larsen, L.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© The Author 2005. Published by Oxford University Press on behalf of the European Society of Human Reproduction and Embryology. All rights reserved.

The effects of 1-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in healthy premenopausal women

Kristof Chwalisz1,4, Walter Elger2,3, Therese Stickler1, Cynthia Mattia-Goldberg1 and Lois Larsen1

1 TAP Pharmaceutical Products Inc., Lake Forest, IL, USA and 2 EnTec GmbH, Jena, Germany. 3 Current address: Schorlemerallee 12B, 14195 Berlin-Dahlem, Germany

4 To whom correspondence should be addressed at: TAP Pharmaceutical Products Inc., 675 N. Field Drive, Lake Forest, IL 60045, USA. Email: kristof.chwalisz{at}tap.com

BACKGROUND: Asoprisnil (J867) is a novel selective progesterone receptor modulator (SPRM) that exhibits partial agonist and antagonist activities and tissue selective effects. This double-blind, dose-escalation study was conducted to evaluate the effects of asoprisnil in 60 regularly cycling premenopausal women. METHODS: Asoprisnil or placebo was administered orally for 28 days starting at the beginning of the menstrual cycle in doses of 5 mg once daily (QD), 5 mg twice daily (BID), 10 mg QD, 25 mg QD, 25 mg BID and 50 mg BID. Within each dose group, two women were randomized to placebo and eight to asoprisnil. Progesterone concentrations indicative of luteinization were defined as at least one progesterone measurement during the luteal phase exceeding 3.5 ng/ml. RESULTS: Asoprisnil consistently prolonged the menstrual cycle at doses ≥10 mg QD. However, the effects on luteal phase progesterone indicative of luteinization were inconsistent and lacked dose dependency. Asoprisnil suppressed periovulatory estradiol but not below follicular phase levels. No significant changes were observed in cortisol and prolactin. Asoprisnil was well tolerated. CONCLUSIONS: Asoprisnil reversibly suppressed menstruation at doses ≥10 mg QD irrespective of the effect on luteal phase progesterone concentrations indicative of luteinization. It induces amenorrhea primarily by targeting the endometrium in the absence of estrogen deprivation.

Key words: asoprisnil/amenorrhea/endometrium/menstrual cycle prolongation/selective progesterone receptor modulator


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 Hum ReprodHome page
J. Wilkens, A.R.W. Williams, K. Chwalisz, C. Han, I.T. Cameron, and H.O.D. Critchley
Effect of asoprisnil on uterine proliferation markers and endometrial expression of the tumour suppressor gene, PTEN
Hum. Reprod., May 1, 2009; 24(5): 1036 - 1044.
[Abstract] [Full Text] [PDF]

Home page
 J. Clin. Endocrinol. Metab.Home page
J. Wilkens, K. Chwalisz, C. Han, J. Walker, I. T. Cameron, S. Ingamells, A. C. Lawrence, M. A. Lumsden, D. Hapangama, A. R. W. Williams, et al.
Effects of the Selective Progesterone Receptor Modulator Asoprisnil on Uterine Artery Blood Flow, Ovarian Activity, and Clinical Symptoms in Patients with Uterine Leiomyomata Scheduled for Hysterectomy
J. Clin. Endocrinol. Metab., December 1, 2008; 93(12): 4664 - 4671.
[Abstract] [Full Text] [PDF]

Home page
 Hum Reprod UpdateHome page
F. M. Horne and D. L. Blithe
Progesterone receptor modulators and the endometrium: changes and consequences
Hum. Reprod. Update, November 1, 2007; 13(6): 567 - 580.
[Abstract] [Full Text] [PDF]

Home page
 J. Clin. Endocrinol. Metab.Home page
N. Chabbert-Buffet, A. Pintiaux-Kairis, P. Bouchard, and on behalf of the VA2914 Study Group
Effects of the Progesterone Receptor Modulator VA2914 in a Continuous Low Dose on the Hypothalamic-Pituitary-Ovarian Axis and Endometrium in Normal Women: A Prospective, Randomized, Placebo-Controlled Trial
J. Clin. Endocrinol. Metab., September 1, 2007; 92(9): 3582 - 3589.
[Abstract] [Full Text] [PDF]

Home page
 Hum ReprodHome page
A.R.W. Williams, H.O.D. Critchley, J. Osei, S. Ingamells, I.T. Cameron, C. Han, and K. Chwalisz
The effects of the selective progesterone receptor modulator asoprisnil on the morphology of uterine tissues after 3 months treatment in patients with symptomatic uterine leiomyomata
Hum. Reprod., June 1, 2007; 22(6): 1696 - 1704.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Endocrinol.Home page
K. P. Madauss, E. T. Grygielko, S.-J. Deng, A. C. Sulpizio, T. B. Stanley, C. Wu, S. A. Short, S. K. Thompson, E. L. Stewart, N. J. Laping, et al.
A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator
Mol. Endocrinol., May 1, 2007; 21(5): 1066 - 1081.
[Abstract] [Full Text] [PDF]

Home page
 J. Clin. Endocrinol. Metab.Home page
W. Chen, N. Ohara, J. Wang, Q. Xu, J. Liu, A. Morikawa, H. Sasaki, S. Yoshida, D. A. Demanno, K. Chwalisz, et al.
A Novel Selective Progesterone Receptor Modulator Asoprisnil (J867) Inhibits Proliferation and Induces Apoptosis in Cultured Human Uterine Leiomyoma Cells in the Absence of Comparable Effects on Myometrial Cells
J. Clin. Endocrinol. Metab., April 1, 2006; 91(4): 1296 - 1304.
[Abstract] [Full Text] [PDF]

Home page
 Endocr. Rev.Home page
K. Chwalisz, M. C. Perez, D. DeManno, C. Winkel, G. Schubert, and W. Elger
Selective Progesterone Receptor Modulator Development and Use in the Treatment of Leiomyomata and Endometriosis
Endocr. Rev., May 1, 2005; 26(3): 423 - 438.
[Abstract] [Full Text] [PDF]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.