Comparing the pharmacokinetic and pharmacodynamic qualities of current and future therapies for uterine fibroids

Giulio Evangelisti; Fabio Barra; Umberto Perrone; Nadine Di Donato; Stefano Bogliolo; Marcello Ceccaroni; Simone Ferrero

doi:10.1080/17425255.2022.2113381

Comparing the pharmacokinetic and pharmacodynamic qualities of current and future therapies for uterine fibroids

Giulio Evangelisti, Fabio Barra, Umberto Perrone, Nadine Di Donato, Stefano Bogliolo, Marcello Ceccaroni, Simone Ferrero

Expert opinion on drug metabolism & toxicology · 2022 · vol. 18(7-8) , pp. 441–457 · doi:10.1080/17425255.2022.2113381 · PMID:35968602 · W4291168252

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⚙ AI-generated summary by claude@2026-06, 2026-06-07 ⓘ

This review compares the pharmacokinetic and pharmacodynamic properties of current uterine fibroid treatments, such as GnRH antagonists and SPRMs, with emerging investigational drugs like linzagolix and vilaprisan.

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Abstract

INTRODUCTION: Uterine fibroids are the most common benign gynecological tumors affecting women of reproductive ages. Although surgery is the definitive treatment choice, several medical approaches have been investigated to control their symptoms. The main issue of currently employed drugs for uterine fibroids is the long-term safety and tolerability profile. Today, new emerging options represent hopeful alternatives that could potentially overcome these limitations. AREAS COVERED: This manuscript aims to give an updated overview of the pharmacodynamic and pharmacokinetic properties of current and new investigational medical drugs for the treatment of symptomatic uterine fibroids. The bibliographic research was conducted by searching alone or combined keywords on the following electronic databases: Medline, PubMed, Embase, Science Citation Index via Web of Science. EXPERT OPINION: The most recent therapeutic strategies for uterine fibroids are represented by gonadotropin-releasing hormone antagonists (GnRH-ants; elagolix and relugolix) and selective progesterone receptor modulators (SPRM; ulipristal acetate). After early promising results, studies on innovative drugs, such as linzagolix (GnRH-ant) and vilaprisan (SPRM) are demanding. In the near future, a deeper knowledge of biological mechanisms at the basis of the genesis and growth of uterine fibroids could pave the way for the development of innovative targeted therapies.

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MeSH descriptors

Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Leiomyoma Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms Uterine Neoplasms

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References (100)

A comprehensive review of hormonal and biological therapies for endometriosis: latest developments via openalex
Clinical outcome, fertility and uterine artery Doppler scans in women with obstetric bilateral internal iliac artery ligation or embolisation via openalex
Development of the selective progesterone receptor modulator CDB-2914 for clinical indications via openalex
Drug–Drug Interaction Studies of Elagolix with Oral and Transdermal Low-Dose Hormonal Add-Back Therapy via openalex
Effect of Food Intake on the Pharmacokinetics of the Selective Progesterone Receptor Modulator Vilaprisan: A Randomized Clinical Study in Healthy Postmenopausal Women via openalex
Effect of SKI2670, a novel, orally active, non-peptide GnRH antagonist, on hypothalamic–pituitary–gonadal axis via openalex
Effects of combined GnRH receptor antagonist linzagolix and hormonal add-back therapy on vaginal bleeding—delayed add-back onset does not improve bleeding pattern via openalex
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 via openalex
Efficacy of Every-Other-Day Administration of Conjugated Equine Estrogen and Medroxyprogesterone Acetate on Gonadotropin-Releasing Hormone Agonists Treatment in Women with Endometriosis via openalex
Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain via openalex
Elagolix: First Global Approval via openalex
Elagolix Pharmacokinetic Profiles in Women With Renal or Hepatic Impairment via openalex
Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review via openalex
Gonadotrophin-releasing hormone analogues for endometriosis: bone mineral density via openalex
Gonadotropin-releasing hormone agonist plus “add-back” hormone replacement therapy for treatment of endometriosis: a prospective, randomized, placebo-controlled, double-blind trial via openalex
Gonadotropin releasing hormone agonists: Expanding vistas via openalex
Gonadotropin-Releasing Hormone Receptor Antagonist Mono- and Combination Therapy With Estradiol/Norethindrone Acetate Add-Back: Pharmacodynamics and Safety of OBE2109 via openalex
Hormonal contraception in women with endometriosis: a systematic review via openalex
Innovative Oral Treatments of Uterine Leiomyoma via openalex
Linzagolix choline. Gonadotropin-releasing hormone, (GnRH) receptor antagonist, Treatment of uterine fibroids, Treatment of endometriosis via openalex
Lupron depot (leuprolide acetate for depot suspension) in the treatment of endometriosis: a randomized, placebo-controlled, double-blind study via openalex
Population Pharmacokinetics of Elagolix in Healthy Women and Women with Endometriosis via openalex
Relugolix: First Global Approval via openalex
Review of the safety, efficacy and patient acceptability of the levonorgestrel-releasing intrauterine system via openalex
Suppression of Gonadotropins and Estradiol in Premenopausal Women by Oral Administration of the Nonpeptide Gonadotropin-Releasing Hormone Antagonist Elagolix via openalex
The Mirena(R) levonorgestrel system via openalex
TISSUE CONCENTRATIONS OF LEVONORGESTREL IN WOMEN USING A LEVONORGESTREL‐RELEASING IUD via openalex
Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone–antagonist: a randomized clinical trial via openalex
Triptorelin for the treatment of endometriosis via openalex
doi:10.1016/j.ejogrb.2014.07.040 via openalex
doi:10.1007/s00404-013-2797-9 via openalex
doi:10.1210/jcem.86.11.8026 via openalex
doi:10.1517/17425255.2012.695775 via openalex
doi:10.1210/en.2009-1225 via openalex
doi:10.1517/14740338.2015.1021773 via openalex
doi:10.1055/s-0035-1563672 via openalex
doi:10.1016/0010-7824(81)90075-5 via openalex
doi:10.1016/j.fertnstert.2003.05.022 via openalex
doi:10.1046/j.1365-2125.2001.01358.x via openalex
doi:10.1016/s0039-128x(00)00176-8 via openalex
doi:10.1073/pnas.1313650110 via openalex
doi:10.1148/rg.326125514 via openalex
doi:10.1016/s0010-7824(03)00044-1 via openalex
doi:10.1210/jc.2015-2770 via openalex
doi:10.1517/13543784.16.11.1851 via openalex
doi:10.1016/j.fertnstert.2010.01.072 via openalex
doi:10.1111/j.1471-0528.2002.01225.x via openalex
doi:10.1016/j.anireprosci.2005.05.005 via openalex
doi:10.1097/00004347-198609000-00005 via openalex
doi:10.1016/0002-9378(92)91707-h via openalex
doi:10.1056/nejmoa1103180 via openalex
doi:10.1016/j.fertnstert.2007.11.006 via openalex
doi:10.1016/j.ejogrb.2013.09.010 via openalex
doi:10.1016/j.bpobgyn.2006.08.002 via openalex
doi:10.1016/s0015-0282(16)49397-0 via openalex
doi:10.1016/s0960-0760(03)00384-4 via openalex
doi:10.1038/bjc.1996.94 via openalex
doi:10.1016/0010-7824(87)90060-6 via openalex
doi:10.1016/j.steroids.2014.05.002 via openalex
doi:10.1007/s12325-012-0042-8 via openalex
doi:10.1016/0002-9378(90)90559-p via openalex
doi:10.1016/j.contraception.2010.02.011 via openalex
doi:10.1093/humupd/dmu048 via openalex
doi:10.1016/s1472-6483(10)60246-5 via openalex
doi:10.1023/b:bebm.0000010962.35909.a1 via openalex
doi:10.1016/0039-128x(90)90062-g via openalex
doi:10.1002/bdd.273 via openalex
doi:10.1016/j.contraception.2010.03.002 via openalex
doi:10.1002/cncr.10908 via openalex
doi:10.1056/nejmoa1103182 via openalex
doi:10.1016/s0140-6736(94)92692-1 via openalex
doi:10.1016/0010-7824(94)90109-0 via openalex
doi:10.1016/j.contraception.2007.01.012 via openalex
doi:10.1016/s0960-0760(03)00360-1 via openalex
doi:10.3109/07853899009147248 via openalex
doi:10.1097/01.aog.0000279151.20878.60 via openalex
doi:10.1210/jc.2008-2327 via openalex
doi:10.1111/j.1471-0528.1988.tb06821.x via openalex
doi:10.1080/13697130500148875 via openalex
doi:10.1016/s0015-0282(16)43212-7 via openalex
doi:10.1016/s0093-7754(03)00305-1 via openalex
doi:10.1042/bj3120617 via openalex
doi:10.1177/1933719117728802 via openalex
doi:10.1007/978-1-4939-0659-8_13 via openalex
doi:10.1097/ogx.0000000000000764 via openalex
doi:10.1016/j.ejogrb.2016.08.021 via openalex
doi:10.1358/dot.2019.55.8.3020179 via openalex
doi:10.1358/dot.2019.55.4.2930713 via openalex
doi:10.1016/j.fertnstert.2020.09.017 via openalex
doi:10.1016/j.jmig.2016.08.004 via openalex
doi:10.1021/acs.jmedchem.6b01071 via openalex
doi:10.1210/jc.2016-3845 via openalex
doi:10.1007/s40262-021-01073-3 via openalex
doi:10.1016/j.jogoh.2017.06.002 via openalex
doi:10.1016/j.ejogrb.2020.05.043 via openalex
doi:10.1517/14740338.2010.515977 via openalex
doi:10.1111/bcp.15014 via openalex
doi:10.1007/s40262-019-00840-7 via openalex
doi:10.1042/cs0880563 via openalex
doi:10.1016/j.fertnstert.2020.07.028 via openalex

Cited by (1)

A review of phase II and III drugs for the treatment and management of endometriosis 2023

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License: CC0 · commercial use OK

[1] A comprehensive review of hormonal and biological therapies for endometriosis: latest developments via openalex

[2] Clinical outcome, fertility and uterine artery Doppler scans in women with obstetric bilateral internal iliac artery ligation or embolisation via openalex

[3] Development of the selective progesterone receptor modulator CDB-2914 for clinical indications via openalex

[4] Drug–Drug Interaction Studies of Elagolix with Oral and Transdermal Low-Dose Hormonal Add-Back Therapy via openalex

[5] Effect of Food Intake on the Pharmacokinetics of the Selective Progesterone Receptor Modulator Vilaprisan: A Randomized Clinical Study in Healthy Postmenopausal Women via openalex

[6] Effect of SKI2670, a novel, orally active, non-peptide GnRH antagonist, on hypothalamic–pituitary–gonadal axis via openalex

[7] Effects of combined GnRH receptor antagonist linzagolix and hormonal add-back therapy on vaginal bleeding—delayed add-back onset does not improve bleeding pattern via openalex

[8] 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 via openalex

[9] Efficacy of Every-Other-Day Administration of Conjugated Equine Estrogen and Medroxyprogesterone Acetate on Gonadotropin-Releasing Hormone Agonists Treatment in Women with Endometriosis via openalex

[10] Elagolix, a Novel, Orally Bioavailable GnRH Antagonist under Investigation for the Treatment of Endometriosis-Related Pain via openalex

[11] Elagolix: First Global Approval via openalex

[12] Elagolix Pharmacokinetic Profiles in Women With Renal or Hepatic Impairment via openalex

[13] Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review via openalex

[14] Gonadotrophin-releasing hormone analogues for endometriosis: bone mineral density via openalex

[15] Gonadotropin-releasing hormone agonist plus “add-back” hormone replacement therapy for treatment of endometriosis: a prospective, randomized, placebo-controlled, double-blind trial via openalex

[16] Gonadotropin releasing hormone agonists: Expanding vistas via openalex

[17] Gonadotropin-Releasing Hormone Receptor Antagonist Mono- and Combination Therapy With Estradiol/Norethindrone Acetate Add-Back: Pharmacodynamics and Safety of OBE2109 via openalex

[18] Hormonal contraception in women with endometriosis: a systematic review via openalex

[19] Innovative Oral Treatments of Uterine Leiomyoma via openalex

[20] Linzagolix choline. Gonadotropin-releasing hormone, (GnRH) receptor antagonist, Treatment of uterine fibroids, Treatment of endometriosis via openalex

[21] Lupron depot (leuprolide acetate for depot suspension) in the treatment of endometriosis: a randomized, placebo-controlled, double-blind study via openalex

[22] Population Pharmacokinetics of Elagolix in Healthy Women and Women with Endometriosis via openalex

[23] Relugolix: First Global Approval via openalex

[24] Review of the safety, efficacy and patient acceptability of the levonorgestrel-releasing intrauterine system via openalex

[25] Suppression of Gonadotropins and Estradiol in Premenopausal Women by Oral Administration of the Nonpeptide Gonadotropin-Releasing Hormone Antagonist Elagolix via openalex

[26] The Mirena(R) levonorgestrel system via openalex

[27] TISSUE CONCENTRATIONS OF LEVONORGESTREL IN WOMEN USING A LEVONORGESTREL‐RELEASING IUD via openalex

[28] Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone–antagonist: a randomized clinical trial via openalex

[29] Triptorelin for the treatment of endometriosis via openalex

[30] doi:10.1016/j.ejogrb.2014.07.040 via openalex

[31] doi:10.1007/s00404-013-2797-9 via openalex

[32] doi:10.1210/jcem.86.11.8026 via openalex

[33] doi:10.1517/17425255.2012.695775 via openalex

[34] doi:10.1210/en.2009-1225 via openalex

[35] doi:10.1517/14740338.2015.1021773 via openalex

[36] doi:10.1055/s-0035-1563672 via openalex

[37] doi:10.1016/0010-7824(81)90075-5 via openalex

[38] doi:10.1016/j.fertnstert.2003.05.022 via openalex

[39] doi:10.1046/j.1365-2125.2001.01358.x via openalex

[40] doi:10.1016/s0039-128x(00)00176-8 via openalex

[41] doi:10.1073/pnas.1313650110 via openalex

[42] doi:10.1148/rg.326125514 via openalex

[43] doi:10.1016/s0010-7824(03)00044-1 via openalex

[44] doi:10.1210/jc.2015-2770 via openalex

[45] doi:10.1517/13543784.16.11.1851 via openalex

[46] doi:10.1016/j.fertnstert.2010.01.072 via openalex

[47] doi:10.1111/j.1471-0528.2002.01225.x via openalex

[48] doi:10.1016/j.anireprosci.2005.05.005 via openalex

[49] doi:10.1097/00004347-198609000-00005 via openalex

[50] doi:10.1016/0002-9378(92)91707-h via openalex

[51] doi:10.1056/nejmoa1103180 via openalex

[52] doi:10.1016/j.fertnstert.2007.11.006 via openalex

[53] doi:10.1016/j.ejogrb.2013.09.010 via openalex

[54] doi:10.1016/j.bpobgyn.2006.08.002 via openalex

[55] doi:10.1016/s0015-0282(16)49397-0 via openalex

[56] doi:10.1016/s0960-0760(03)00384-4 via openalex

[57] doi:10.1038/bjc.1996.94 via openalex

[58] doi:10.1016/0010-7824(87)90060-6 via openalex

[59] doi:10.1016/j.steroids.2014.05.002 via openalex

[60] doi:10.1007/s12325-012-0042-8 via openalex

[61] doi:10.1016/0002-9378(90)90559-p via openalex

[62] doi:10.1016/j.contraception.2010.02.011 via openalex

[63] doi:10.1093/humupd/dmu048 via openalex

[64] doi:10.1016/s1472-6483(10)60246-5 via openalex

[65] doi:10.1023/b:bebm.0000010962.35909.a1 via openalex

[66] doi:10.1016/0039-128x(90)90062-g via openalex

[67] doi:10.1002/bdd.273 via openalex

[68] doi:10.1016/j.contraception.2010.03.002 via openalex

[69] doi:10.1002/cncr.10908 via openalex

[70] doi:10.1056/nejmoa1103182 via openalex

[71] doi:10.1016/s0140-6736(94)92692-1 via openalex

[72] doi:10.1016/0010-7824(94)90109-0 via openalex

[73] doi:10.1016/j.contraception.2007.01.012 via openalex

[74] doi:10.1016/s0960-0760(03)00360-1 via openalex

[75] doi:10.3109/07853899009147248 via openalex

[76] doi:10.1097/01.aog.0000279151.20878.60 via openalex

[77] doi:10.1210/jc.2008-2327 via openalex

[78] doi:10.1111/j.1471-0528.1988.tb06821.x via openalex

[79] doi:10.1080/13697130500148875 via openalex

[80] doi:10.1016/s0015-0282(16)43212-7 via openalex

[81] doi:10.1016/s0093-7754(03)00305-1 via openalex

[82] doi:10.1042/bj3120617 via openalex

[83] doi:10.1177/1933719117728802 via openalex

[84] doi:10.1007/978-1-4939-0659-8_13 via openalex

[85] doi:10.1097/ogx.0000000000000764 via openalex

[86] doi:10.1016/j.ejogrb.2016.08.021 via openalex

[87] doi:10.1358/dot.2019.55.8.3020179 via openalex

[88] doi:10.1358/dot.2019.55.4.2930713 via openalex

[89] doi:10.1016/j.fertnstert.2020.09.017 via openalex

[90] doi:10.1016/j.jmig.2016.08.004 via openalex

[91] doi:10.1021/acs.jmedchem.6b01071 via openalex

[92] doi:10.1210/jc.2016-3845 via openalex

[93] doi:10.1007/s40262-021-01073-3 via openalex

[94] doi:10.1016/j.jogoh.2017.06.002 via openalex

[95] doi:10.1016/j.ejogrb.2020.05.043 via openalex

[96] doi:10.1517/14740338.2010.515977 via openalex

[97] doi:10.1111/bcp.15014 via openalex

[98] doi:10.1007/s40262-019-00840-7 via openalex

[99] doi:10.1042/cs0880563 via openalex

[100] doi:10.1016/j.fertnstert.2020.07.028 via openalex