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Review
. 2018 Jun 24:2018:1374821.
doi: 10.1155/2018/1374821. eCollection 2018.

Selective Progesterone Receptor Modulators for the Medical Treatment of Uterine Fibroids with a Focus on Ulipristal Acetate

Thomas Rabe  1 , Nicole Saenger  2 , Andreas D Ebert  3 , Thomas Roemer  4 , Hans-Rudolf Tinneberg  5 , Rudy Leon De Wilde  6 , Markus Wallwiener  7
Affiliations
Review

Selective Progesterone Receptor Modulators for the Medical Treatment of Uterine Fibroids with a Focus on Ulipristal Acetate

Thomas Rabe et al. Biomed Res Int. .

Erratum in

Abstract

Uterine fibroids are the most frequent benign tumours in women of child-bearing age. Their symptoms are diverse and the quality of life of the women affected can be significantly impaired. While treatment to date has been primarily by means of surgical intervention, selective progesterone receptor modulators (SPRMs) open up new medication-based treatment options. EMA's Pharmacovigilance Risk Assessment Committee (PRAC) has recently completed its review of ESMYA® (ulipristal acetate, 5 mg), following reports of serious liver injury, including liver failure leading to transplantation in postmarketing settings. We will provide some information on the PRAC's recommendations to minimize this risk. Nevertheless, the effectiveness and safety of the SPRM ulipristal acetate (UPA), both with regard to preoperative administration and with regard to an intermittent administration as long-term treatment for patients with symptomatic uterine fibroids, have been shown in several clinical studies (PEARL I-IV).

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Figures

Figure 1
Figure 1
Prevalence of fibroids according to age-group, as percentages (N = 2,270), according to Ahrendt et al. [7].
Figure 2
Figure 2
Mode of action of SPRMs according to Bouchard et al. [8]: SPRMs interact with coactivators and corepressors. In this way, the gene transcription is either inhibited or activated. This means that the stimulating or inhibiting effect of an SPRM is dependent on its chemical structure.
Figure 3
Figure 3
Effects of ulipristal acetate on the pituitary gland, endometrium, and fibroid according to Donnez and Dolmans [4].
Figure 4
Figure 4
Percentage of patients with amenorrhoea at the end of each treatment interval with 5 mg of UPA (PP4; PEARL IV).
Figure 5
Figure 5
Percentage of patients with bleeding control at the end of each treatment interval with 5 mg of UPA (PP4; PEARL IV).
Figure 6
Figure 6
Bleeding intensity (PBAC median) of the first menstruation following the completion of a treatment interval (FAS1; PEARL IV).
Figure 7
Figure 7
Volume change in the 3 largest fibroids (median) in comparison with the initial value.
Figure 8
Figure 8
Percentage of patients with clinically significant reduction of the volume of the fibroids of ≥ 25% (FAS1) [9].
Figure 9
Figure 9
Percentage of patients with amenorrhoea and clinically significant reduction of the volume of the fibroids of ≥ 25% [10].
Figure 10
Figure 10
Effect of 5 mg of UPA on the course of pain (VAS). Outline of the median values (FAS1) [11].
Figure 11
Figure 11
Effect of 5 mg of UPA on the quality of life (HR QoL). Outline of the median values (FAS1).
Figure 12
Figure 12
Percentage of patients with an endometrial thickness of > 16 mm (Safety Population) [10].
Figure 13
Figure 13
Percentage of patients with nonphysiological changes of the endometrium (PAEC) (Safety Population).
See this image and copyright information in PMC

References

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