Literature DB >> 30527839

Vilaprisan in women with uterine fibroids: the randomized phase 2b ASTEROID 1 study.

Linda D Bradley1, Sukhbir S Singh2, James Simon3, Kristina Gemzell-Danielsson4, Kathrin Petersdorf5, Esther Groettrup-Wolfers5, Xiaowei Ren6, Michal Zvolanek5, Christian Seitz5.   

Abstract

OBJECTIVES: To assess the safety and efficacy of four vilaprisan doses (0.5-4.0 mg) in women with uterine fibroids.
DESIGN: Randomized, double-blind, placebo-controlled, multicenter trial.
SETTING: Ninety-eight centers in 12 countries. PATIENT(S): Women aged 18-50 years with uterine fibroids and heavy menstrual bleeding were randomized equally to oral vilaprisan at 0.5, 1.0, 2.0, or 4.0 mg or placebo once daily. INTERVENTION(S): Treatment for 12 weeks, 24-week follow-up. MAIN OUTCOME MEASURE(S): Primary end point was absence of scheduled or unscheduled bleeding/spotting. Key secondary efficacy end points included volume of menstrual blood loss and change in fibroid volume. RESULT(S): A total of 309 patients were randomized, and 300 received treatment. Complete absence of bleeding/spotting was observed in 30%, 56%, 54%, and 60% of patients in the vilaprisan 0.5, 1.0, 2.0, and 4.0 mg groups, respectively, versus 1.7% with placebo. After 12 weeks, >83% of women achieved amenorrhea (<2 mL/28 days) with ≥1.0 mg vilaprisan versus 9% with placebo. Heavy menstrual bleeding stopped (but returned at a lower volume after treatment cessation) with ≥1.0 mg vilaprisan treatment. Reductions in fibroid volume of up to 41% were observed. Most patients receiving vilaprisan reported improvements in symptom severity. No safety concerns were identified in general safety, endometrial safety (by biopsy), laboratory values, and ultrasound examinations. CONCLUSION(S): ASTEROID 1 supports the efficacy of vilaprisan for the treatment of heavy menstrual bleeding associated with uterine fibroids. Daily oral treatment with vilaprisan 0.5-4.0 mg was well tolerated, and vilaprisan 2.0 mg once daily has been selected for further investigation. CLINICAL TRIAL REGISTRATION NUMBER: NCT02131662.
Copyright © 2018 The Authors. Published by Elsevier Inc. All rights reserved.

Entities:  

Keywords:  BAY1002670; heavy menstrual bleeding; leiomyoma; uterine fibroids; vilaprisan

Mesh:

Substances:

Year:  2018        PMID: 30527839     DOI: 10.1016/j.fertnstert.2018.10.012

Source DB:  PubMed          Journal:  Fertil Steril        ISSN: 0015-0282            Impact factor:   7.329


  11 in total

Review 1.  Selective Progesterone Receptor Modulators-Mechanisms and Therapeutic Utility.

Authors:  Md Soriful Islam; Sadia Afrin; Sara Isabel Jones; James Segars
Journal:  Endocr Rev       Date:  2020-10-01       Impact factor: 19.871

2.  Effect of hepatic impairment on the pharmacokinetics of vilaprisan: An open-label, single-dose, parallel-group study.

Authors:  Niladri Chattopadhyay; Kai Riecke; Sandra Ligges; Torsten Zimmermann; Atef Halabi; Marcus-Hillert Schultze-Mosgau
Journal:  Br J Clin Pharmacol       Date:  2019-07-10       Impact factor: 4.335

3.  Validation of a menstrual pictogram and a daily bleeding diary for assessment of uterine fibroid treatment efficacy in clinical studies.

Authors:  Claudia Haberland; Anna Filonenko; Christian Seitz; Matthias Börner; Christoph Gerlinger; Helen Doll; Dorothea Wessiepe
Journal:  J Patient Rep Outcomes       Date:  2020-11-13

4.  Markers of Cellular Proliferation, Apoptosis, Estrogen/Progesterone Receptor Expression and Fibrosis in Selective Progesterone Receptor Modulator (Ulipristal Acetate)-Treated Uterine Fibroids.

Authors:  Iwona Szydłowska; Marta Grabowska; Jolanta Nawrocka-Rutkowska; Małgorzata Piasecka; Andrzej Starczewski
Journal:  J Clin Med       Date:  2021-02-03       Impact factor: 4.241

5.  Assessment of the safe and efficacious dose of the selective progesterone receptor modulator vilaprisan for the treatment of patients with uterine fibroids by exposure-response modelling and simulation.

Authors:  Gabriele Sutter; Matthias Frei; Marcus-Hillert Schultze-Mosgau; Kathrin Petersdorf; Christian Seitz; Bart A Ploeger
Journal:  Br J Clin Pharmacol       Date:  2021-08-25       Impact factor: 3.716

6.  Progesterone receptor ligands for the treatment of endometriosis: the mechanisms behind therapeutic success and failure.

Authors:  Fernando M Reis; Larissa M Coutinho; Silvia Vannuccini; Frédéric Batteux; Charles Chapron; Felice Petraglia
Journal:  Hum Reprod Update       Date:  2020-06-18       Impact factor: 15.610

7.  Pharmacokinetics and Safety of the Novel Selective Progesterone Receptor Modulator Vilaprisan in Participants With Renal Impairment.

Authors:  Marcus-Hillert Schultze-Mosgau; Kenneth C Lasseter; Thomas Marbury; Stephanie Loewen; Kai Riecke
Journal:  J Clin Pharmacol       Date:  2020-03-30       Impact factor: 3.126

8.  Pharmacokinetics and Safety of the Selective Progesterone Receptor Modulator Vilaprisan in Chinese Healthy Postmenopausal Women.

Authors:  Hongzhong Liu; Ji Jiang; Zhaozhao Chen; Yunhui Zhang; Jinyi Li; Joachim Hoechel; Beate Rohde; Torsten Zimmermann; Marcus-Hillert Schultze-Mosgau
Journal:  Clin Pharmacol Drug Dev       Date:  2020-07-27

Review 9.  Clinical Pharmacokinetics and Pharmacodynamics of the Selective Progesterone Receptor Modulator Vilaprisan: A Comprehensive Overview.

Authors:  Marcus-Hillert Schultze-Mosgau; Bart A Ploeger; Matthias Frei; Joachim Höchel; Antje Rottmann
Journal:  Clin Pharmacokinet       Date:  2021-09-27       Impact factor: 6.447

10.  Effect of Food Intake on the Pharmacokinetics of the Selective Progesterone Receptor Modulator Vilaprisan: A Randomized Clinical Study in Healthy Postmenopausal Women.

Authors:  Marcus-Hillert Schultze-Mosgau; Andreas Kaiser; Frank S Zollmann
Journal:  Clin Pharmacol Drug Dev       Date:  2020-10-05
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