What are the effects of selective progesterone receptor modulators (SPRMs) for premenopausal women with uterine fibroids?

2017 ◽  
Keyword(s):  
Progesterone Receptor ◽  
Uterine Fibroids ◽  
Premenopausal Women ◽  
Receptor Modulators ◽  
Selective Progesterone Receptor Modulators ◽  
Progesterone Receptor Modulators

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.

scholarly journals Fibroid: A common problem and its advanced management

2020 ◽  
Vol 2 (Number 2) ◽  
pp. 28-37
Author(s):  
Shaikh Zinnat Ara Nasreen ◽  
Nusrat Mahjabeen ◽  
Naima Sharmin Haque ◽  
Tasmia Chowdhury
Keyword(s):  
Progesterone Receptor ◽  
Medical Treatment ◽  
Premenopausal Women ◽  
Definitive Treatment ◽  
Negative Consequences ◽  
Major Step ◽  
Receptor Modulators ◽  
Selective Progesterone Receptor Modulators ◽  
Progesterone Receptor Modulators

Uterine fibroids are the most common gynaecological disorder, classically requiring surgery when symptomatic. Although attempts at finding a nonsurgical cure date back to centuries, it is only around the middle of the last century that serious attempts at a medical treatment were carried out. Initially, both progestins and estrogen–progestin combinations have been utilized, although proof of their usefulness is lacking. A major step forward was achieved when peptide analogues of the GnRH were introduced, first those with super agonist properties and subsequently those acting as antagonists. Because both types of analogues produce hypoestrogenism, their use is limited to a maximum of 6 months and, so they can’t be used routinely but utilized as an adjuvant treatment before surgery with overall good results. Over the last decade, new, nonpeptidic, orally active GnRH-receptor blockers Elagolix and another development of selective progesterone receptor modulators, sometimes referred to as “antiprogestins of choice is Ulipristal acetate are promising.Large clinical trials have proven the effectiveness of Ulipristal in the long-term medical therapy of fibroids, caution must taken for liver complications. All selective progesterone receptor modulators produce unique endometrial changes that are today considered benign, reversible, and without negative consequences. Long-term medical treatment of fibroids seems possible today, especially in premenopausal women. Surgical treatments are myomectomy, radiofrequency ablation procedure, endometrial ablation, uterine artery embolization, magnetic resonance-guided focused ultrasound myolysis are effective and reserved for the women who desires to keep uterus, and morcellation . Still Hysterectomy is the definitive treatment for fibroid and the techniques of surgery is inclining towards minimum invasive surgery.

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

2018 ◽  
Vol 2018 ◽  
pp. 1-12 ◽  
Author(s):  
Thomas Rabe ◽  
Nicole Saenger ◽  
Andreas D. Ebert ◽  
Thomas Roemer ◽  
Hans-Rudolf Tinneberg ◽  
...  
Keyword(s):  
Progesterone Receptor ◽  
Treatment Options ◽  
Uterine Fibroids ◽  
Term Treatment ◽  
Ulipristal Acetate ◽  
Long Term Treatment ◽  
Benign Tumours ◽  
Receptor Modulators ◽  
Selective Progesterone Receptor Modulators ◽  
Progesterone Receptor Modulators

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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