Novel pharmacological therapies for the treatment of endometriosis

References

• Vercellini P, Buggio L, Berlanda N, et al. Estrogen-progestins and progestins for the management of endometriosis. Fertil Steril. 2016 Dec;106(7):1552–1571.e2.
   Google Scholar
• Tomassetti C, Johnson NP, Petrozza J, et al. International Working Group of AAGL, ESGE, ESHRE and WES. An international terminology for endometriosis, 2021. Hum Reprod Open. 2021Oct22;2021(4):hoab029.
   Google Scholar
• Vercellini P, Viganò P, Somigliana E, et al. Endometriosis: pathogenesis and treatment. Nat Rev Endocrinol. 2014 May;10(5):261–275.
   Google Scholar
• Barbara G, Buggio L, Facchin F, et al. Medical treatment for endometriosis: tolerability, quality of life and adherence. Front Glob Womens Health. 2021 Sep 27;2:729601.
   Google Scholar
• Soliman AM, Yang H, Du EX, et al. The direct and indirect costs associated with endometriosis: a systematic literature review. Hum Reprod. 2016 Apr;31(4):712–722.
   Google Scholar
• Facchin F, Buggio L, Ottolini F, et al. Preliminary insights on the relation between endometriosis, pelvic pain, and employment. Gynecol Obstet Invest. 2019;84(2):190–195.
   Google Scholar
• Archer DF, Soliman AM, Agarwal SK, et al. Elagolix in the treatment of endometriosis: impact beyond pain symptoms. Ther Adv Reprod Health. 2020 Dec 1;14:2633494120964517.
   Google Scholar
• Practice Committee of the American Society for Reproductive Medicine. Treatment of pelvic pain associated with endometriosis: a committee opinion. Fertil Steril. 2014 Apr;101(4):927–935.
   Google Scholar
• Buggio L, Somigliana E, Barbara G, et al. Oral and depot progestin therapy for endometriosis: towards a personalized medicine. Expert Opin Pharmacother. 2017 Oct;18(15):1569–1581.
   Google Scholar
• Becker CM, Bokor A, Heikinheimo O, et al. Members of the Endometriosis Guideline Core Group. ESHRE Endometriosis Guideline Group. ESHRE guideline: endometriosis. Hum Reprod Open. 2022 Feb 26;2022(2):hoac009.
   Google Scholar
• National Guideline Alliance (UK). Endometriosis: diagnosis and management. London: National Institute for Health and Care Excellence (NICE); 2017 Sep. PMID: 29787038.
   Google Scholar
• Vercellini P, Buggio L, Frattaruolo MP, et al. Medical treatment of endometriosis-related pain. Best Pract Res Clin Obstet Gynaecol. 2018 Aug;51:68–91.
   Google Scholar
• Donnez J, Dolmans MM. Endometriosis and medical therapy: from progestogens to progesterone resistance to GnRH antagonists: a review. J Clin Med. 2021 Mar 5;10(5):1085.
   Google Scholar
• Hornstein MD. An oral GnRH antagonist for endometriosis - a new drug for an old disease. N Engl J Med. 2017 Jul 6;377(1):81–83.
   Google Scholar
• Clemenza S, Sorbi F, Noci I, et al. From pathogenesis to clinical practice: emerging medical treatments for endometriosis. Best Pract Res Clin Obstet Gynaecol. 2018 Aug;51:92–101.
   Google Scholar
• Barbieri RL. Hormone treatment of endometriosis: the estrogen threshold hypothesis. Am J Obstet Gynecol. 1992 Feb;166(2):740–745.
   Google Scholar
• Donnez J, Taylor RN, Taylor HS. Partial suppression of estradiol: a new strategy in endometriosis management? Fertil Steril. 2017 Mar;107(3):568–570.
   Google Scholar
• Lamb YN. Elagolix: first global approval. Erratum in: Drugs. 2018 Nov 15. Drugs. 2018 Sep;78(14):1501–1508.
   Google Scholar
• Osuga Y, Seki Y, Tanimoto M, et al. Relugolix, an oral gonadotropin-releasing hormone receptor antagonist, reduces endometriosis-associated pain in a dose-response manner: a randomized, double-blind, placebo-controlled study. Fertil Steril. 2021 Feb;115(2):397–405.
   Google Scholar
• Osuga Y, Seki Y, Tanimoto M, et al. Relugolix, an oral gonadotropin-releasing hormone (GnRH) receptor antagonist, in women with endometriosis-associated pain: phase 2 safety and efficacy 24-week results. BMC Women's Health. 2021 Jun 21;21(1):250.
   Google Scholar
• Harada T, Osuga Y, Suzuki Y, et al. Relugolix, an oral gonadotropin-releasing hormone receptor antagonist, reduces endometriosis-associated pain compared with leuprorelin in Japanese women: a phase 3, randomized, double-blind, noninferiority study. Fertil Steril. 2022 Mar;117(3):583–592.
   Google Scholar
• Donnez J, Taylor HS, Taylor RN, et al. Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone-antagonist: a randomized clinical trial. Fertil Steril. 2020 Jul;114(1):44–55.
   Google Scholar
• Taylor HS, Giudice LC, Lessey BA, et al. Treatment of endometriosis-associated pain with elagolix, an oral GnRH antagonist. N Engl J Med. 2017 Jul;377(1):28–40.
   Google Scholar
• Surrey E, Taylor HS, Giudice L, et al. Long-term outcomes of elagolix in women with endometriosis: results from two extension studies. Obstet Gynecol. 2018 Jul;132(1):147–160. Erratum in: Obstet Gynecol. 2018 Dec;132(6):1507-1508.
   Google Scholar
• D’Hooghe T, Fukaya T, Osuga Y, et al. Efficacy and safety of ASP1707 for endometriosis-associated pelvic pain: the phase II randomized controlled TERRA study. Hum Reprod. 2019 May;34(5):813–823.
   Google Scholar
• As-Sanie S, Becker CM, Johnson N, et al. Efficacy and safety of relugolix combination therapy in women with endometriosis-associated pain: phase 3 randomized, double-blind, placebo-controlled study (spirit 2). Fertil Steril. 2020;114(3):e77.
   Google Scholar
• Giudice LC, As-Sanie S, Arjona Ferreira JC, et al. Once daily oral relugolix combination therapy versus placebo in patients with endometriosis-associated pain: two replicate phase 3, randomised, double-blind, studies (SPIRIT 1 and 2). Lancet. 2022 Jun;399(10343):2267–2279.
   Google Scholar
• Ng J, Chwalisz K, Carter DC, et al. Dose-dependent suppression of gonadotropins and ovarian hormones by elagolix in healthy premenopausal women. J Clin Endocrinol Metab. 2017 May 1;102(5):1683–1691.
   Google Scholar
• Pokrzywinski RM, Soliman AM, Chen J, et al. Achieving clinically meaningful response in endometriosis pain symptoms is associated with improvements in health-related quality of life and work productivity: analysis of 2 phase III clinical trials. Am J Obstet Gynecol. 2020 Jun;222(6):592.e1–592.e10.
   Google Scholar
• Taylor HS, Soliman AM, Johns B, et al. Health-related quality of life improvements in patients with endometriosis treated with elagolix. Obstet Gynecol. 2020 Sep;136(3):501–509.
   Google Scholar
• Surrey ES, Soliman AM, Palac HL, et al. Impact of elagolix on workplace and household productivity among women with moderate to severe pain associated with endometriosis: a pooled analysis of two phase III trials. Patient. 2019 Dec;12(6):651–660.
   Google Scholar
• Vercellini P, Viganò P, Barbara G, et al.; ‘Luigi Mangiagalli’ Endometriosis Study Group. Elagolix for endometriosis: all that glitters is not gold. Hum Reprod. 2019 Feb 1;34(2):193–199.
   Google Scholar
• Vannuccini S, Clemenza S, Rossi M, et al. Hormonal treatments for endometriosis: the endocrine background. Rev Endocr Metab Disord. 2022 Jun;23(3):333–355.
   Google Scholar
• Simon JMD, Kim JHMD, Thomas JMD, et al. Long-term safety of elagolix with hormonal add-back therapy in women with endometriosis-associated pain: 24-month results <Q86/&#x003E. Obstetrics Gynecol. 2022 May;139:25S–26S.
   Google Scholar
• Markham A. Relugolix: first global approval. Drugs. 2019 Apr;79(6):675–679.
   Google Scholar
• Dababou S, Garzon S, Laganà AS, et al. Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas. Expert Opin Investig Drugs. 2021 Sep;30(9):903–911.
   Google Scholar
• Singh SS, Belland L, Leyland N, et al. The past, present, and future of selective progesterone receptor modulators in the management of uterine fibroids. Am J Obstet Gynecol. 2018;218(6):563–572.e1.
   Google Scholar
• Oskari H, Kimmo K, Horacio C, et al. Plasma concentrations and receptor binding of RU 486 and its metabolites in humans. J Steroid Biochem. 1987;26(2):279–284.
   Google Scholar
• Md S I, Afrin S, Jones SI, et al. Selective progesterone receptor modulators-mechanisms and therapeutic utility. Endocr Rev. 2020 Oct 1;41(5):bnaa012.
   Google Scholar
• DeManno D, Elger W, Garg R, et al. Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy. Steroids. 2003;68(10–13):1019–1032.
   Google Scholar
• Blithe DL, Nieman LK, Blye RP, et al. Development of the selective progesterone receptor modulator CDB-2914 for clinical indications Steroids. Steroids. 2003;68(10–13):1013–1017.
   Google Scholar
• Kettel LM, Murphy AA, Morales AJ, et al. Treatment of endometriosis with the antiprogesterone mifepristone (RU486). Fertil Steril. 1996 Jan;65(1):23–28.
   Google Scholar
• Kettel LM, Murphy AA, Morales AJ, et al. Preliminary report on the treatment of endometriosis with low-dose mifepristone (RU 486). Am J Obstet Gynecol. 1998 Jun;178(6):1151–1156.
   Google Scholar
• Chwalisz K, Mattia-Goldberg C, Elger W, et al. Treatment of endometriosis with the novel selective progesterone receptor modulator (SPRM) asoprisnil. Fertil Steril. 2004;82:S83–4.
   Google Scholar
• Tosti C, Biscione A, Morgante G, et al. Hormonal therapy for endometriosis: from molecular research to bedside. Eur J Obstet Gynecol Reprod Biol. 2017 Feb;209:61–66.
   Google Scholar
• Gatti M, Poluzzi E, De Ponti F, et al. Liver injury with ulipristal acetate: exploring the underlying pharmacological basis. Drug Saf. 2020 Dec;43(12):1277–1285.
   Google Scholar
• European Medical Agency. Ulipristal acetate for uterine fibroids: EMA recommends restricting use. https://www.ema.europa.eu/en/documents/referral/ulipristal-acetate-5mg-medicinal-products-article-31-referral-ulipristal-acetate-uterine-fibroids_en.pdf. ( Accessed March 18, 2021).
   Google Scholar
• De Milliano I, Van Hattum D, Ket JCF, et al. Endometrial changes during ulipristal acetate use: a systematic review. Eur J Obstet Gynecol Reprod Biol. 2017 Jul;214:56–64.
   Google Scholar
• Singh SS, Evans D, McDonald S, et al. Ulipristal acetate prior to surgery for endometriosis. Reprod Sci. 2020 Sep;27(9):1707–1714.
   Google Scholar
• Delmas PD, Bjarnason NH, Mitlak BH, et al. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N Engl J Med. 1997 Dec 4;337(23):1641–1647.
   Google Scholar
• Simsa P, Mihalyi A, Kyama CM, et al. Selective estrogen-receptor modulators and aromatase inhibitors: promising new medical therapies for endometriosis? Womens Health (Lond). 2007 Sep;3(5):617–628.
   Google Scholar
• Francucci CM, Romagni P, Boscaro M. Raloxifene: bone and cardiovascular effects. J Endocrinol Invest. 2005;28(10 Suppl):85–89.
   Google Scholar
• Eng-Wong J, Zujewski JA. Raloxifene and its role in breast cancer prevention. Expert Rev Anticancer Ther. 2004 Aug;4(4):523–532.
   Google Scholar
• Van Hoesel MH, Chen YL, Zheng A, et al. Selective oestrogen receptor modulators (SERMs) for endometriosis. Cochrane Database Syst Rev. 2021 May 11;5(5):CD011169.
   Google Scholar
• Yao Z, Shen X, Capodanno I, et al. Validation of rat endometriosis model by using raloxifene as a positive control for the evaluation of novel SERM compounds. J Invest Surg. 2005 Jul-Aug;18(4):177–183.
   Google Scholar
• Altintas D, Kokcu A, Kandemir B, et al. Comparison of the effects of raloxifene and anastrozole on experimental endometriosis. Eur J Obstet Gynecol Reprod Biol. 2010 May;150(1):84–87.
   Google Scholar
• Stratton P, Sinaii N, Segars J, et al. Return of chronic pelvic pain from endometriosis after raloxifene treatment: a randomized controlled trial. Obstet Gynecol. 2008 Jan;111(1):88–96.
   Google Scholar
• Kulak JsJr, Fischer C, Komm B, et al. Treatment with bazedoxifene, a selective estrogen receptor modulator, causes regression of endometriosis in a mouse model. Endocrinology. 2011 Aug;152(8):3226–3232.
   Google Scholar
• Naqvi H, Sakr S, Presti T, et al. Treatment with bazedoxifene and conjugated estrogens results in regression of endometriosis in a murine model. Biol Reprod. 2014 Jun;90(6):121.
   Google Scholar
• Flores VA, Stachenfeld NS, Taylor HS. Bazedoxifene-Conjugated Estrogens for Treating Endometriosis. Obstet Gynecol. 2018 Aug;132(2):475–477.
   Google Scholar
• Taylor HS, Kotlyar AM, Flores VA. Endometriosis is a chronic systemic disease: clinical challenges and novel innovations. Lancet. 2021 Feb 27;397(10276):839–852.
   Google Scholar
• Harada T, Ohta I, Endo Y, et al. SR-16234, a novel selective estrogen receptor modulator for pain symptoms with endometriosis: an open-label clinical trial. Yonago Acta Med. 2018 Feb 5;60(4):227–233.
   Google Scholar
• Sibiude J, Santulli P, Marcellin L, et al. Association of history of surgery for endometriosis with severity of deeply infiltrating endometriosis. Obstet Gynecol. 2014 Oct;124(4):709–717.
   Google Scholar
• Goodman LR, Goldberg JM, Flyckt RL, et al. Effect of surgery on ovarian reserve in women with endometriomas, endometriosis and controls. Am J Obstet Gynecol. 2016 Nov;215(5):589.e1–589.e6.
   Google Scholar
• Carr B, Dmowski WP, O’Brien C, et al. An oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density. Reprod Sci. 2014 Nov;21(11):1341–1351.
   Google Scholar
• Hartner G, Husslein H, Kuessel L, et al. The latest advances in the pharmacological management of endometriosis. Expert Opin Pharmacother. 2022 Mar;1:1–13.
   Google Scholar