scholarly journals Selective Progesterone Receptor Modulator(ulipristal acetate – a new option in the pharmacological treatment of uterine fibroids in women

2013 ◽  
Vol 84 (3) ◽  
Author(s):  
Marian Szamatowicz ◽  
Jan Kotarski
Keyword(s):  
Progesterone Receptor ◽  
Pharmacological Treatment ◽  
Uterine Fibroids ◽  
Ulipristal Acetate ◽  
Receptor Modulator

scholarly journals Predictive Factors of Response to Selective Progesterone Receptor Modulator (Ulipristal Acetate) in the Pharmacological Treatment of Uterine Fibroids

2020 ◽  
Vol 17 (3) ◽  
pp. 798
Author(s):  
Iwona Szydłowska ◽  
Aleksandra Marciniak ◽  
Jolanta Nawrocka-Rutkowska ◽  
Aleksandra Rył ◽  
Andrzej Starczewski
Keyword(s):  
Blood Flow ◽  
Progesterone Receptor ◽  
Predictive Factors ◽  
Uterine Fibroids ◽  
Volume Number ◽  
Ulipristal Acetate ◽  
Uterine Arteries ◽  
Receptor Modulator ◽  
Estradiol Concentration ◽  
Status Of Women

Background: Selective progesterone receptor modulator ulipristal acetate (UPA) is a drug used in management of symptomatic myomas. It was observed that the response to UPA treatment in uterine myomas varied amongst patients. An attempt was thus made at establishing predictive factors conducive to better reaction to treatment with UPA. The aim of this study was to assess the efficacy of UPA treatment in women with myomas, depending on pretreatment myomas’ volume, number of myomas, age of patients, estrogenic status of women, and pretreatment blood flow in uterine arteries. Materials and methods: The study included patients with one to four myomas. The UPA treatment was a preparation stage for surgical treatment in all patients. The study group was divided into the subgroups according to pretreatment myomas’ volume, number of myomas, age of patients, estrogenic status of women, and pretreatment blood flow in uterine arteries. Results: A better effect of reduction in size of myomas after UPA treatment was noted when pretreatment myomas’ volume was lower than 30 cm3. A significant reduction in fibroids’ size was observed after UPA therapy independently of the number of myomas and age of patients. A good response after the UPA therapy was observed when pretreatment estradiol concentration was below 50 pg/mL and when uterine artery resistance index (RI) was above 0.8. Conclusions: Our research demonstrates that treatment with ulipristal acetate is an efficient method in preoperative preparation of patients with uterine fibroids. The most important factor of positive response to UPA therapy is myoma volume. The number of myomas and patient’s age do not interfere with effects of UPA therapy. Pretreatment estradiol concentration is significant, yet secondary for the effects of therapy. The UPA therapy has no impact on blood flow in the uterine arteries and no adverse influence on estradiol concentrations.

scholarly journals Markers of Inflammation and Vascular Parameters in Selective Progesterone Receptor Modulator (Ulipristal Acetate)-Treated Uterine Fibroids

2021 ◽  
Vol 10 (16) ◽  
pp. 3721
Author(s):  
Iwona Szydłowska ◽  
Marta Grabowska ◽  
Jolanta Nawrocka-Rutkowska ◽  
Andrzej Kram ◽  
Małgorzata Piasecka ◽  
...  
Keyword(s):  
Progesterone Receptor ◽  
Inflammatory Markers ◽  
Uterine Fibroids ◽  
Response To Treatment ◽  
Control Group ◽  
Ulipristal Acetate ◽  
Weak Response ◽  
Receptor Modulator ◽  
Markers Of Inflammation ◽  
Response Group

The exact mechanism of selective progesterone receptor modulator action in leiomyoma still challenges researchers. The aim of the study was to assess the effects of ulipristal acetate (UPA) on immunoexpression of inflammatory markers and vascularization in fibroids. UPA-treated patients were divided into three groups: (1) good response (≥25% reduction in volume of fibroid), (2) weak response (insignificant volume reduction), (3) and no response to treatment (no decrease or increase in fibroid volume). The percentage of TGFβ, IL6, IL10, CD117, and CD68-positive cells were significantly lower in the group with a good response to treatment vs. the control group. Moreover, the percentage of IL10 and CD68-positive cells in the group with a good response to treatment were also significantly lower compared to the no response group. Additionally, a significant decrease in the percentage of IL10-positive cells was found in the good response group vs. the weak response group. There were no statistical differences in the percentage of TNFα-positive cells and vessel parameters between all compared groups. The results of the study indicate that a good response to UPA treatment may be associated with a decrease of inflammatory markers, but it does not influence myoma vascularization.

scholarly journals Effect of a Selective Progesterone Receptor Modulator on Induction of Apoptosis in Uterine Fibroids In Vivo

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Petr Horak ◽  
Michal Mara ◽  
Pavel Dundr ◽  
Kristyna Kubinova ◽  
David Kuzel ◽  
...  
Keyword(s):  
Uterine Fibroids ◽  
Premenopausal Women ◽  
Hormonal Treatment ◽  
Control Groups ◽  
Ulipristal Acetate ◽  
Receptor Modulator ◽  
Positive Clinical Effect ◽  
The Mean ◽  
And Control

Aim. To determine if hormonal treatment induces apoptosis in uterine fibroids.Methods. Immunohistochemical examination of fibroid tissue, using avidin-biotin complex and cleaved caspase-3 antibody for detecting apoptosis, was performed in premenopausal women who underwent 12-week treatment with oral SPRM (6 patients with 5 mg and 5 patients with 10 mg of ulipristal acetate per day) or gonadoliberin agonist (GnRHa, 17 patients) and subsequent myomectomy or hysterectomy for symptomatic uterine fibroids. Ten patients with no presurgical hormonal treatment were used as controls.Results. Apoptosis was present in a significantly higher proportion of patients treated with ulipristal acetate compared to GnRHa (P=0.01) and to patients with no hormonal treatment (P=0.01). In contrast to an AI of 158.9 in SPRM patients, the mean AI was 27.5 and 2.0 in GnRHa and control groups, respectively. No statistical difference in the AI was observed between the two groups of patients treated with ulipristal acetate (5 mg or 10 mg).Conclusion. Treatment with ulipristal acetate induces apoptosis in uterine fibroid cells. This effect of SPRM may contribute to their positive clinical effect on uterine fibroids.

scholarly journals Selective Progesterone Receptor Modulators—Mechanisms and Therapeutic Utility

2020 ◽  
Vol 41 (5) ◽  
pp. 643-694 ◽  
Author(s):  
Md Soriful Islam ◽  
Sadia Afrin ◽  
Sara Isabel Jones ◽  
James Segars
Keyword(s):  
Progesterone Receptor ◽  
Critical Role ◽  
Uterine Fibroids ◽  
In Vivo Studies ◽  
Current Evidence ◽  
Ulipristal Acetate ◽  
Cancer Multiple ◽  
Receptor Modulators ◽  
Selective Progesterone Receptor Modulators ◽  
Progesterone Receptor Modulators

Abstract Selective progesterone receptor modulators (SPRMs) are a new class of compounds developed to target the progesterone receptor (PR) with a mix of agonist and antagonist properties. These compounds have been introduced for the treatment of several gynecological conditions based on the critical role of progesterone in reproduction and reproductive tissues. In patients with uterine fibroids, mifepristone and ulipristal acetate have consistently demonstrated efficacy, and vilaprisan is currently under investigation, while studies of asoprisnil and telapristone were halted for safety concerns. Mifepristone demonstrated utility for the management of endometriosis, while data are limited regarding the efficacy of asoprisnil, ulipristal acetate, telapristone, and vilaprisan for this condition. Currently, none of the SPRMs have shown therapeutic success in treating endometrial cancer. Multiple SPRMs have been assessed for efficacy in treating PR-positive recurrent breast cancer, with in vivo studies suggesting a benefit of mifepristone, and multiple in vitro models suggesting the efficacy of ulipristal acetate and telapristone. Mifepristone, ulipristal acetate, vilaprisan, and asoprisnil effectively treated heavy menstrual bleeding (HBM) in patients with uterine fibroids, but limited data exist regarding the efficacy of SPRMs for HMB outside this context. A notable class effect of SPRMs are benign, PR modulator-associated endometrial changes (PAECs) due to the actions of the compounds on the endometrium. Both mifepristone and ulipristal acetate are effective for emergency contraception, and mifepristone was approved by the US Food and Drug Administration (FDA) in 2012 for the treatment of Cushing’s syndrome due to its additional antiglucocorticoid effect. Based on current evidence, SPRMs show considerable promise for treatment of several gynecologic conditions.

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