Overview of elagolix for the treatment of endometriosis

References

• Schally AV, Arimura A, Baba Y, et al. Isolation and properties of the FSH and LH-releasing hormone. Biochem Biopsy Res Commun. 1971;43:393–399.
   PubMed Web of Science ®Google Scholar
• Knobil E. The neuroendocrine control of the menstrual cycle. Recent Prog Horm Res. 1980;36:53–88.
   PubMedGoogle Scholar
• Kaiser UB, Conn PM, Chin WW. Studies of gonadotropin-releasing hormone (GnRH) action using GnRH receptor-expressing pituitary cell lines. Endocr Rev. 1997;18:46–70.
   PubMed Web of Science ®Google Scholar
• Lemay A, Maheux R, Faure N, et al. Reversible hypogonadism induced by a luteinizing hormone-releasing hormone (LH-RH) agonist (Buserelin) as a new therapeutic approach for endometriosis. Fertil Steril. 1984;41:863–871.
   PubMed Web of Science ®Google Scholar
• Schally AV, Comaru-Schally AM. Hypothalamic and other peptide hormones. In: Holland JF, Frei E, editors. Cancer medicine, 7th ed. Hamilton: Decker; 2006, p. 802–816.
   Google Scholar
• Engel JB, Schally AV. Drug insight: clinical use of agonists and antagonists of luteinizing-hormone-releasing hormone. Nat Clin Pract Endocrinol Metab. 2007;3:157–167.
   PubMedGoogle Scholar
• Conn PM, Crowley WF Jr. Gonadotropin-releasing hormone and its analogues. N Engl J Med. 1991;324:93–103.
   PubMed Web of Science ®Google Scholar
• Tan O, Bukulmez O. Biochemistry, molecular biology and cell biology of gonadotropin-releasing hormone antagonists. Curr Opin Obstet Gynecol. 2011;23:238–244.
   PubMed Web of Science ®Google Scholar
• Chillik C, Acosta A. The role of LHRH agonists and antagonists. Reprod Biomed Online. 2001;2:120–128.
   PubMedGoogle Scholar
• Huirne JA, Lambalk CB. Gonadotropin-releasing-hormone receptor antagonists. Lancet. 2001;358:1793–1803.
   PubMed Web of Science ®Google Scholar
• Fujimoto VY, Monroe SE, Nelson LR, et al. Dose-related suppression of serum luteinizing hormone in women by a potent new gonadotropin-releasing hormone antagonist (Ganirelix) administered by intranasal spray. Fertil Steril. 1997;67:469–473.
   PubMed Web of Science ®Google Scholar
• Albano C, Smitz J, Camus M, et al. Comparison of different doses of gonadotropin-releasing hormone antagonist Cetrorelix during controlled ovarian hyperstimulation. Fertil Steril. 1997;67:917–922.
   PubMed Web of Science ®Google Scholar
• Reissmann T, Felberbaum R, Diedrich K, et al. Development and applications of luteinizing hormone-releasing hormone antagonists in the treatment of infertility: an overview. Hum Reprod. 1995;10:1974–1981.
   PubMed Web of Science ®Google Scholar
• Reissmann T, Schally AV, Bouchard P, et al. The LHRH antagonist cetrorelix: a review. Hum Reprod Update. 2000;6:322–331.
   PubMed Web of Science ®Google Scholar
• Kolibianakis EM, Zikopoulos K, Schiettecatte J, et al. Profound LH suppression after GnRH antagonist administration is associated with a significantly higher ongoing pregnancy rate in IVF. Hum Reprod. 2004;19:2490–2496.
   PubMed Web of Science ®Google Scholar
• Boccon-Gibod L, van der Meulen E, Persson B-E. An update on the use of gonadotropin-releasing hormone antagonists in prostate cancer. Ther Adv Urol. 2011;3:127–140.
   PubMedGoogle Scholar
• Diedrich K, Diedrich C, Santos E, et al. Suppression of the endogenous LH surge by the LH-RH antagonist cetrorelix during ovarian stimulation. Hum Reprod. 1994;9:788–791.
   PubMed Web of Science ®Google Scholar
• Nelson LR, Fujimoto VY, Jaffe RB, et al. Suppression of follicular phase pituitary-gonadal function by a potent new gonadotropin-releasing hormone antagonist with reduced histamine-releasing properties (ganirelix). Fertil Steril. 1995;63:963–969.
   PubMed Web of Science ®Google Scholar
• Porter RN, Smith W, Craft IL, et al. Induction of ovulation for in vitro fertilisation using buserelin and gonadotropins. Lancet. 1984;2:1284–1285.
   PubMed Web of Science ®Google Scholar
• Daya S. Gonadotropin releasing hormone agonist protocols for pituitary desensitization in in vitro fertilization and gamete intrafallopian transfer cycles. Cochrane Database Syst Rev. 2000;(2). art. No CD001299. doi:10.1002/14651858.cd001299
   Google Scholar
• Wilcox J, Potter D, Moore M, et al. Prospective, randomized trial comparing cetrorelix acetate and ganirelix acetate in a programmed, flexible protocol for premature luteinizing hormone surge prevention in assisted reproductive technologies. Fertil Steril. 2005;84:108–117.
   PubMed Web of Science ®Google Scholar
• Al-Inany H, Aboulghar M. GnRH antagonist in assisted reproduction: a Cochrane review. Hum Reprod. 2002;17:874–885.
   PubMed Web of Science ®Google Scholar
• Kaufmann M, Jonat W, Kleeberg U, et al. Goserelin, a depot gonadotrophin-releasing hormone agonist in the treatment of premenopausal patients with metastatic breast cancer. German Zoladex Trial Group. J Clin Oncol. 1989;7:1113–1119.
   PubMed Web of Science ®Google Scholar
• Klijn JG, Blamey RW, Boccardo F, et al. Combined tamoxifen and luteinizing hormone-releasing hormone (LHRH) agonist versus LHRH agonist alone in premenopausal advanced breast cancer: a meta-analysis of four randomized trials. J Clin Oncol. 2001;19:343–353.
   PubMed Web of Science ®Google Scholar
• Forward DP, Cheung KL, Jackson L, et al. Clinical and endocrine data for goserelin plus anastrozole as second-line endocrine therapy for premenopausal advanced breast cancer. Br J Cancer. 2004;90:590–594.
   PubMed Web of Science ®Google Scholar
• Jonat W, Kaufmann M, Sauerbrei W, et al. Goserelin versus cyclophosphamide, methotrexate, and fluorouracil as adjuvant therapy in premenopausal patients with node-positive breast cancer: the Zoladex Early Breast Cancer Research Association Study. J Clin Oncol. 2002;20:4628–4635.
   PubMed Web of Science ®Google Scholar
• Jakesz R, Hausmaninger H, Kubista E, et al. Randomized adjuvant trial of tamoxifen and goserelin versus cyclophosphamide, methotrexate, and fluorouracil: evidence for the superiority of treatment with endocrine blockade in premenopausal patients with hormone-responsive breast cancer-Austrian Breast and Colorectal Cancer Study Group Trial 5. J Clin Oncol. 2002;20:4621–4627.
   PubMed Web of Science ®Google Scholar
• Noci I, Coronnello M, Borri P, et al. Inhibitory effect of luteinising hormone-releasing hormone analogues on human endometrial cancer in vitro. Cancer Lett. 2000;150:71–78.
   PubMed Web of Science ®Google Scholar
• Emons G, Heyl W. Hormonal treatment of endometrial cancer. J Cancer Res Clin Oncol. 2000;126:619–623.
   PubMed Web of Science ®Google Scholar
• Gründker C, Günthert AR, Millar RP, et al. Expression of gonadotropin-releasing hormone II (GnRH-II) receptor in human endometrial and ovarian cancer cells and effects of GnRH-II on tumor cell proliferation. J Clin Endocrinol Metab. 2002;87:1427–1430.
   PubMed Web of Science ®Google Scholar
• Fister S, Günthert AR, Emons G, et al. Gonadotropin-releasing hormone type II antagonists induce apoptotic cell death in human endometrial and ovarian cancer cells in vitro and in vivo. Cancer Res. 2007;67:1750–1756.
   PubMed Web of Science ®Google Scholar
• Yu B, Ruman J, Christman G. The role of peripheral gonadotropin-releasing hormone receptors in female reproduction. Fertil Steril. 2011;95:465–473.
   PubMed Web of Science ®Google Scholar
• Chen H, Li J, Cui T. Adjuvant gonadotropin releasing hormone analogues for chemotherapy induced premature ovarian in premenopausal women. Cochrane Rev. 2011;11:CD008018.
   PubMed Web of Science ®Google Scholar
• Maruo T, Ohara N, Wang J, et al. Sex steroidal regulation of uterine leiomyoma growth and apoptosis. Hum Reprod Update. 2004;10:207–220.
   PubMed Web of Science ®Google Scholar
• Ishikawa H, Ishi K, Serna VA, et al. Progesterone is essential for maintenance and growth of uterine leiomyoma. Endocrinology. 2010;151:2433–2442.
   PubMed Web of Science ®Google Scholar
• Lethaby A, Vollenhoven B, Sowter M. Efficacy of pre-operative gonadotrophin hormone releasing analogues for women with uterine fibroids undergoing hysterectomy or myomectomy: a systematic review. BJOG. 2002;109:1097–1108.
   PubMed Web of Science ®Google Scholar
• Felberbaum RE, Küpker W, Krapp M, et al. Preoperative reduction of uterine fibroids in only 16 days by administration of a gonadotrophin-releasing hormone antagonist (Cetrotide). Reprod Biomed Online. 2001;3:14–18.
   PubMedGoogle Scholar
• Flierman PA, Oberyé JJ, Van Der Hulst VP, et al. Rapid reduction of leiomyoma volume during treatment with the GnRH antagonist ganirelix. BJOG. 2005;112:638–642.
   PubMed Web of Science ®Google Scholar
• US Clinical Trial Registry. Safety and efficacy in premenopausal women with heavy menstrual bleeding (HMB) associated with uterine fibroids (UF) [Internet]. [cited 2016 Apr 16]. Available from: https://clinicaltrials.gov/ct2/show/NCT01817530?term=elagolix&rank=7; https://clinicaltrials.gov/ct2/show/record/NCT01441635?term=elagolix&rank=6; https://clinicaltrials.gov/ct2/show/NCT02654054?term=elagolix&rank=2; https://clinicaltrials.gov/ct2/show/NCT02691494?term=elagolix&rank=3.
   Google Scholar
• Meldrum DR, Chang RJ, Lu J, et al. “Medical Oophorectomy”using a long-acting GnRH agonist - a possible new approach to the treatment of endometriosis. J Clin Endocrinol Metab. 1982;54:1081–1083.
   PubMed Web of Science ®Google Scholar
• Kupker W, Schultze-Mosgau A, Diedrich K. Paracrine changes in the peritoneal environment of women with endometriosis. Hum Reprod Update. 1998;4:719–723.
   PubMed Web of Science ®Google Scholar
• Kiilholma P, Tuimala R, Kivinen S, et al. Comparison of the gonadotropin-releasing hormone agonist goserelin acetate alone versus goserelin combined with estrogen–progestogen add-back therapy in the treatment of endometriosis. Fertil Steril. 1995;5:903–908.
   Google Scholar
• Ezzati M, Carr BR. Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond Engl). 2015;11:19–28.
   PubMedGoogle Scholar
• Leone Roberti Maggiore U, Ferrero S. An overview of early drug development for endometriosis. Expert Opin Investig Drugs. 2016;25:227–247.
   PubMed Web of Science ®Google Scholar
• Tafi E, Leone Roberti Maggiore U, Alessandri F, et al. Advances in pharmacotherapy for treating endometriosis. Expert Opin Pharmacother. 2015;16:2465–2483.
   PubMed Web of Science ®Google Scholar
• Dunselman GA, Vermeulen N, Becker C, et al. European Society of Human Reproduction and Embryology. ESHRE guideline: management of women with endometriosis. Hum Reprod. 2014;29:400–412.
   PubMed Web of Science ®Google Scholar
• Küpker W, Felberbaum RE, Krapp M, et al. Use of GnRH antagonists in the treatment of endometriosis. Reprod Biomed Online. 2002;5:12–16.
   PubMedGoogle Scholar
• Cho N, Harada M, Imaeda T, et al. Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. J Med Chem. 1998;41:4190–4195.
   PubMed Web of Science ®Google Scholar
• Armer RE, Smelt KH. Non-peptidic GnRH receptor antagonists. Curr Med Chem. 2004;11:3017–3028.
   PubMed Web of Science ®Google Scholar
• Struthers RS, Chen T, Campbell B, et al. Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902). J Clin Endocrinol Metab. 2006;91:3903–3907.
   PubMed Web of Science ®Google Scholar
• Diamond MP, Carr B, Dmowski WP, et al. Elagolix treatment for endometriosis-associated pain: results from a phase 2, randomized, double-blind, placebo-controlled study. Reprod Sci. 2014;21:363–371.
   PubMed Web of Science ®Google Scholar
• Carr B, Chwalisz K, Jimenez R, et al. A novel oral GnRH antagonist, elagolix, is effective for reducing endometriosis-associated pelvic pain: results of a 24-week randomized study. Fertil Steril. 2011;96:S45.
   Web of Science ®Google Scholar
• Imani R, Thai-Cuarto D, Jimenez R, et al. Petal study: safety, tolerability and effectiveness of elagolix, an oral GnRH antagonist for endometriosis. Fertil Steril. 2009;92:S111–S112.
   Google Scholar
• Struthers RS, Nicholls AJ, Grundy J, et al. Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin releasing hormone antagonist elagolix. J Clin Endocrinol Metab. 2009;94:545–551.
   PubMed Web of Science ®Google Scholar
• Boyce M, Clark E, Johnston A, et al. Effects of single and repeated oral doses of TAK-013, a new non-peptide gonadotropin-releasing hormone (GnRH) antagonist, in healthy post-menopausal women. Fertil Steril. 2002;78:S281–S282.
   Web of Science ®Google Scholar
• Chen C, Wu D, Guo Z, et al. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008;51:7478–7485.
   PubMed Web of Science ®Google Scholar
• Duijkers IJ, Klipping C, Willemsen WN, et al. Single and multiple dose pharmacokinetics and pharmacodynamics of the gonadotrophin-releasing hormone antagonist cetrorelix in healthy female volunteers. Hum Reprod. 1998;13:2392–2398.
   PubMed Web of Science ®Google Scholar
• Carr B, Dmowski WP, O’Brien C, et al. Elagolix, an oral GnRH antagonist, versus subcutaneous depot medroxyprogesterone acetate for the treatment of endometriosis: effects on bone mineral density. Reprod Sci. 2014;21:1341–1351.
   PubMed Web of Science ®Google Scholar
• Carr B, Giudice L, Dmowski WP, et al. Elagolix, an oral GnRH antagonist for endometriosis-associated pain: a randomized controlled study. Journal of Endometriosis and Pelvic Pain Disorders. 2013;5:105–115.
   PubMedGoogle Scholar
• US Clinical Trial Registry. A clinical study to evaluate the safety and efficacy of elagolix in subjects with moderate to severe endometriosis-associated pain [Internet]. [cited 2016 Apr 16]. Available from: https://clinicaltrials.gov/ct2/show/NCT01620528?term=M12-665&rank=1
   Google Scholar
• Elagolix: a potential treatment for endometriosis [Internet]. [cited 2016 Apr 16]. Available from: http://www.neurocrine.com/pipeline/elagolix-gnrh-antagonist/endometriosis/clinical-trials
   Google Scholar
• US Clinical Trial Registry. A global phase 3 study to evaluate the safety and efficacy of elagolix in subjects with moderate to severe endometriosis-associated pain [Internet]. [cited 2016 Apr 16]. Available from: https://clinicaltrials.gov/ct2/show/NCT01931670?term=M12-671&rank=2
   Google Scholar
• Felix Wong WS, Danforn Lim CE. Hormonal treatment for endometriosis associated pelvic pain. Iran J Reprod Med. 2011;9:163–170.
   PubMedGoogle Scholar
• Vercellini P, De Giorgi O, Oldani S, et al. Depot medroxyprogesterone acetate versus an oral contraceptive combined with very-low-dose danazol for long-term treatment of pelvic pain associated with endometriosis. Am J Obstet Gynecol. 1996;175:396–401.
   PubMed Web of Science ®Google Scholar
• Harada T, Momoeda M, Taketani Y, et al. Low-dose oral contraceptive pill for dysmenorrhea associated with endometriosis: a placebo-controlled, double-blind, randomized trial. Fertil Steril. 2008;90:1583–1588.
   PubMed Web of Science ®Google Scholar
• Berlanda N, Somigliana E, Viganò P, et al. Safety of medical treatments for endometriosis. Expert Opin Drug Saf. 2015;10:1–10.
   Google Scholar
• Strowitzki T, Marr J, Gerlinger C, et al. Detailed analysis of a randomized, multicenter, comparative trial of dienogest versus leuprolide acetate in endometriosis. Int J Gynaecol Obstet. 2012;117:228–233.
   PubMed Web of Science ®Google Scholar