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Relugolix
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<h2 id="medical-uses">Medical uses</h2> <p>Relugolix is approved in the United States, Canada and the United Kingdom for the treatment of <a href="/facts/Prostate_cancer/Mx7XuDhm">prostate cancer</a> in men and in Japan for the treatment of <a href="/facts/Uterine_fibroid/xqGmDE2J">uterine fibroids</a> (uterine leiomyoma) in women.<a class="footnote-ref" id="fnref:17" href="#fn:17"><sup>17</sup></a><a class="footnote-ref" id="fnref:18" href="#fn:18"><sup>18</sup></a><a class="footnote-ref" id="fnref:19" href="#fn:19"><sup>19</sup></a> </p> <h3>Available forms</h3> <p>Relugolix is available in the form of 40 and 120 mg <a href="/facts/Oral_administration/vNQcvLVx">oral</a> <a href="/facts/Tablet_(pharmacy)/PcYmnjd0">tablets</a>.<a class="footnote-ref" id="fnref:20" href="#fn:20"><sup>20</sup></a><a class="footnote-ref" id="fnref:21" href="#fn:21"><sup>21</sup></a><a class="footnote-ref" id="fnref:22" href="#fn:22"><sup>22</sup></a> </p> <h2 id="side-effects">Side effects</h2> <p>The main <a href="/facts/Side_effect/PhuX2haY">side effects</a> of relugolix for uterine fibroids include <a href="/facts/Abnormal_uterine_bleeding/06n59DW5">abnormal uterine bleeding</a> (24.6–48.6% vs. 6.3% for placebo), <a href="/facts/Hot_flash/4XyMNyFH">hot flashes</a> (42.8–45.5% vs. 0% for placebo), <a href="/facts/Menorrhagia/cQUgAGNk">heavy menstrual bleeding</a> (12.1–49.3% vs. 9.4% for placebo), <a href="/facts/Headache/mdmmC9DP">headache</a> (12.3–15.2%), and <a href="/facts/Hyperhidrosis/koG3nCEn">excessive sweating</a> (9.4–15.2% vs. 0% for placebo).<a class="footnote-ref" id="fnref:23" href="#fn:23"><sup>23</sup></a><a class="footnote-ref" id="fnref:24" href="#fn:24"><sup>24</sup></a> In addition, <a href="/facts/Osteoporosis/xa1W00Tj">decreased bone mineral density</a> occurs with relugolix (21.7% decrease by week 12, 24.4% decrease by week 24).<a class="footnote-ref" id="fnref:25" href="#fn:25"><sup>25</sup></a> </p> <h2 id="pharmacology">Pharmacology</h2> <h3>Pharmacodynamics</h3> <p>Relugolix is a <a href="/facts/Binding_selectivity/RryTsdGv">selective</a> <a href="/facts/Receptor_antagonist/PuXHVNdV">antagonist</a> of the <a href="/facts/Gonadotropin-releasing_hormone_receptor/lTbY8l1S">gonadotropin-releasing hormone receptor</a> (GnRHR), with a <a href="/facts/Half-maximal_inhibitory_concentration/zdz6qVBP">half-maximal inhibitory concentration</a> (IC50) of 0.12 nM.<a class="footnote-ref" id="fnref:26" href="#fn:26"><sup>26</sup></a><a class="footnote-ref" id="fnref:27" href="#fn:27"><sup>27</sup></a><a class="footnote-ref" id="fnref:28" href="#fn:28"><sup>28</sup></a> </p><p>A dosage of relugolix of 40 mg once per day has been found to suppress estradiol levels to <a href="/facts/Postmenopause/b3Fz6NHb">postmenopausal</a> levels (<20 pg/mL) within 24 hours in premenopausal women.<a class="footnote-ref" id="fnref:29" href="#fn:29"><sup>29</sup></a> In the control group of women, estradiol levels fluctuated between 50 and 250 pg/mL.<a class="footnote-ref" id="fnref:30" href="#fn:30"><sup>30</sup></a> Estradiol levels have been found to return to normal concentrations within 4 weeks of discontinuation of relugolix in premenopausal women.<a class="footnote-ref" id="fnref:31" href="#fn:31"><sup>31</sup></a> The medication additionally suppresses levels of <a href="/facts/Progesterone/WEj2TGRm">progesterone</a>, <a href="/facts/Luteinizing_hormone/a6znte2S">luteinizing hormone</a>, and <a href="/facts/Follicle-stimulating_hormone/n6CwdebD">follicle-stimulating hormone</a> in premenopausal women.<a class="footnote-ref" id="fnref:32" href="#fn:32"><sup>32</sup></a> Relugolix at a dosage of 40 mg or more once per day has been found to reduce <a href="/facts/Testosterone/uUumdhAz">testosterone</a> levels to sustained <a href="/facts/Castration/QdBkfLCK">castrate</a> levels (<20 ng/dL) in men.<a class="footnote-ref" id="fnref:33" href="#fn:33"><sup>33</sup></a> It additionally suppresses luteinizing hormone and follicle-stimulating hormone levels in men.<a class="footnote-ref" id="fnref:34" href="#fn:34"><sup>34</sup></a> </p><p>Lower doses of relugolix (<40 mg/day) are under investigation for achieving partial <a href="/facts/Sex_hormone/mI6bkHII">sex hormone</a> suppression in the treatment of endometriosis and uterine fibroids.<a class="footnote-ref" id="fnref:35" href="#fn:35"><sup>35</sup></a> This is intended to reduce the incidence and severity of <a href="/facts/Menopausal_symptoms/b3Fz6NHb">menopausal symptoms</a> such as <a href="/facts/Hot_flush/4XyMNyFH">hot flushes</a> and <a href="/facts/Osteoporosis/xa1W00Tj">decreased bone mineral density</a> that are secondary to <a href="/facts/Estrogen_deficiency/mz2k8Hnl">estrogen deficiency</a>.<a class="footnote-ref" id="fnref:36" href="#fn:36"><sup>36</sup></a><a class="footnote-ref" id="fnref:37" href="#fn:37"><sup>37</sup></a> </p> <h3>Pharmacokinetics</h3> <p>A single 40-mg oral dose of relugolix has been found to result in <a href="/facts/Cmax_(pharmacology)/IceQcRQB">peak levels</a> of relugolix of 29 ng/mL (47 nmol/L) after 1.5 hours.<a class="footnote-ref" id="fnref:38" href="#fn:38"><sup>38</sup></a> <a href="/facts/Steady-state_levels/x4CUUnle">Steady-state levels</a> are reached within 7 days with 40 mg/day relugolix administration.<a class="footnote-ref" id="fnref:39" href="#fn:39"><sup>39</sup></a> There is an approximate 2-fold accumulation of relugolix by 2 weeks of continuous administration.<a class="footnote-ref" id="fnref:40" href="#fn:40"><sup>40</sup></a> Food diminishes the oral <a href="/facts/Bioavailability/9l6na9MV">bioavailability</a> of relugolix by about 50%.<a class="footnote-ref" id="fnref:41" href="#fn:41"><sup>41</sup></a> </p><p>Relugolix is a <a href="/facts/Substrate_(biochemistry)/6MnaV19h">substrate</a> for <a href="/facts/P-glycoprotein/RY6qLKjq">P-glycoprotein</a>, which may have a limiting effect on its <a href="/facts/Absorption_(pharmacokinetics)/LCezQPJK">absorption</a> and <a href="/facts/Distribution_(pharmacology)/f8Hkox6Q">distribution</a>.<a class="footnote-ref" id="fnref:42" href="#fn:42"><sup>42</sup></a> The <a href="/facts/Plasma_protein_binding/7u7qFYmb">plasma protein binding</a> of relugolix is approximately 68 to 71% over a concentration range of 0.05 to 5 μg/mL.<a class="footnote-ref" id="fnref:43" href="#fn:43"><sup>43</sup></a> </p><p>Relugolix is not a substrate for <a href="/facts/CYP3A4/MqD09gEj">CYP3A4</a>.<a class="footnote-ref" id="fnref:44" href="#fn:44"><sup>44</sup></a> The <a href="/facts/Elimination_half-life/7nB2JtMr">elimination half-life</a> of relugolix is 36 to 65 hours across a dosage range of 20 to 180 mg/day.<a class="footnote-ref" id="fnref:45" href="#fn:45"><sup>45</sup></a> There is moderate to high <a href="/facts/Interindividual_variability/f2wzYLbI">interindividual variability</a> in systemic exposure to relugolix.<a class="footnote-ref" id="fnref:46" href="#fn:46"><sup>46</sup></a> </p><p>Relugolix is <a href="/facts/Excretion/mspsTfnv">excreted</a> mainly in <a href="/facts/Feces/r9HDKB8G">feces</a> (83%) and to a small degree in <a href="/facts/Urine/oNUYVtvX">urine</a> (4%).<a class="footnote-ref" id="fnref:47" href="#fn:47"><sup>47</sup></a> Only about 6% of a dose of relugolix is excreted unchanged.<a class="footnote-ref" id="fnref:48" href="#fn:48"><sup>48</sup></a> </p> <h2 id="chemistry">Chemistry</h2> <p>Relugolix is a <a href="/facts/Non-peptide/kbwq3VBn">non-peptide</a>, <a href="/facts/Small-molecule/kbwq3VBn">small-molecule</a> <a href="/facts/Chemical_compound/37FXqqtv">compound</a>, and is structurally distinct from <a href="/facts/GnRH_analogue/nurNownG">GnRH analogues</a>.<a class="footnote-ref" id="fnref:49" href="#fn:49"><sup>49</sup></a> It is an <i>N</i>-<a href="/facts/Phenyl_group/Ql9Yx5uu">phenyl</a> <a href="/facts/Urea/6j84AoCG">urea</a> <a href="/facts/Chemical_derivative/JYcbLkbm">derivative</a>.<a class="footnote-ref" id="fnref:50" href="#fn:50"><sup>50</sup></a> </p> <h2 id="history">History</h2> <p>Relugolix was first described in 2004.<a class="footnote-ref" id="fnref:51" href="#fn:51"><sup>51</sup></a><a class="footnote-ref" id="fnref:52" href="#fn:52"><sup>52</sup></a> It superseded <a href="/facts/Sufugolix/voUl9DG4">sufugolix</a> (developmental code name TAK-013), which was developed by the same researchers.<a class="footnote-ref" id="fnref:53" href="#fn:53"><sup>53</sup></a> Relugolix was approved for the treatment of uterine fibroids in Japan in January 2019.<a class="footnote-ref" id="fnref:54" href="#fn:54"><sup>54</sup></a><a class="footnote-ref" id="fnref:55" href="#fn:55"><sup>55</sup></a> It was the second orally active GnRH antagonist to be introduced for medical use, following <a href="/facts/Elagolix/YFjcI3YI">elagolix</a> (brand name Orilissa) in July 2018.<a class="footnote-ref" id="fnref:56" href="#fn:56"><sup>56</sup></a><a class="footnote-ref" id="fnref:57" href="#fn:57"><sup>57</sup></a> Relugolix was approved for the treatment of prostate cancer in the United States on 18 December 2020.<a class="footnote-ref" id="fnref:58" href="#fn:58"><sup>58</sup></a><a class="footnote-ref" id="fnref:59" href="#fn:59"><sup>59</sup></a> </p><p>The FDA approved relugolix based on evidence from a clinical trial (NCT03085095) of 930 participants 48 to 97 years old with advanced prostate cancer.<a class="footnote-ref" id="fnref:60" href="#fn:60"><sup>60</sup></a> The trial was conducted at 155 sites in the United States, Canada, and countries in South America, Europe and the Asia Pacific region.<a class="footnote-ref" id="fnref:61" href="#fn:61"><sup>61</sup></a> All participants in the trial had advanced prostate cancer.<a class="footnote-ref" id="fnref:62" href="#fn:62"><sup>62</sup></a> Participants were randomly assigned to receive either one relugolix tablet daily (on the first day they received three tables) or an active control (leuprolide acetate) which was given as an injection under the skin every three months.<a class="footnote-ref" id="fnref:63" href="#fn:63"><sup>63</sup></a> The participants and healthcare providers were aware of which treatment was being given.<a class="footnote-ref" id="fnref:64" href="#fn:64"><sup>64</sup></a> The treatment lasted for 48 weeks.<a class="footnote-ref" id="fnref:65" href="#fn:65"><sup>65</sup></a> The efficacy of relugolix was assessed by the percentage of participants who achieved and maintained low testosterone level equal to castration.<a class="footnote-ref" id="fnref:66" href="#fn:66"><sup>66</sup></a> </p> <h2 id="society-and-culture">Society and culture</h2> <h3>Names</h3> <p><i>Relugolix</i> is the <a href="/facts/Generic_term/nENLNhIF">generic name</a> of the drug and its <a href="/facts/International_Nonproprietary_Name/wYL655x6">INN</a>Tooltip International Nonproprietary Name, <a href="/facts/United_States_Adopted_Name/5AFEKGfQ">USAN</a>Tooltip United States Adopted Name, and <a href="/facts/Japanese_Accepted_Name/2TWpxztK">JAN</a>Tooltip Japanese Accepted Name.<a class="footnote-ref" id="fnref:67" href="#fn:67"><sup>67</sup></a><a class="footnote-ref" id="fnref:68" href="#fn:68"><sup>68</sup></a> It is also known by its former developmental code names RVT-601 and TAK-385.<a class="footnote-ref" id="fnref:69" href="#fn:69"><sup>69</sup></a><a class="footnote-ref" id="fnref:70" href="#fn:70"><sup>70</sup></a> </p><p>Relugolix is sold under the brand name Orgovyx for the treatment of prostate cancer and under the brand name Relumina for the treatment of uterine fibroids.<a class="footnote-ref" id="fnref:71" href="#fn:71"><sup>71</sup></a><a class="footnote-ref" id="fnref:72" href="#fn:72"><sup>72</sup></a><a class="footnote-ref" id="fnref:73" href="#fn:73"><sup>73</sup></a><a class="footnote-ref" id="fnref:74" href="#fn:74"><sup>74</sup></a> Relugolix compounded with <a href="/facts/Ethinyl_estradiol/aYRGLz8n">ethinyl estradiol</a> and <a href="/facts/Norethindrone/G1DJxlre">norethindrone</a> is sold under the brand name <a href="/facts/Myfembree/t3XchNg7">Myfembree</a> for the treatment of uterine fibroids.<a class="footnote-ref" id="fnref:75" href="#fn:75"><sup>75</sup></a> </p> <h3>Availability</h3> <p>Relugolix is available in the United States and in Japan.<a class="footnote-ref" id="fnref:76" href="#fn:76"><sup>76</sup></a><a class="footnote-ref" id="fnref:77" href="#fn:77"><sup>77</sup></a><a class="footnote-ref" id="fnref:78" href="#fn:78"><sup>78</sup></a> </p> <h3>Legal status</h3> <p>In February 2022, the <a href="/facts/Committee_for_Medicinal_Products_for_Human_Use/yCkJTISe">Committee for Medicinal Products for Human Use</a> (CHMP) of the <a href="/facts/European_Medicines_Agency/h9FTtCYc">European Medicines Agency</a> adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Orgovyx, intended for the treatment of prostate cancer.<a class="footnote-ref" id="fnref:79" href="#fn:79"><sup>79</sup></a> The applicant for this medicinal product is Myovant Sciences Ireland Limited.<a class="footnote-ref" id="fnref:80" href="#fn:80"><sup>80</sup></a> Relugolix was approved for medical use in the European Union in April 2022,<a class="footnote-ref" id="fnref:81" href="#fn:81"><sup>81</sup></a><a class="footnote-ref" id="fnref:82" href="#fn:82"><sup>82</sup></a> and in the United Kingdom in July 2022<a class="footnote-ref" id="fnref:83" href="#fn:83"><sup>83</sup></a> (although not available in <a href="/facts/National_Health_Service/lTzheqYw">NHS</a> England until August 2024<a class="footnote-ref" id="fnref:84" href="#fn:84"><sup>84</sup></a>). </p> <h2 id="research">Research</h2> <p>Relugolix is under development for use in the treatment of <a href="/facts/Endometriosis/wKS0I8mc">endometriosis</a>.<a class="footnote-ref" id="fnref:85" href="#fn:85"><sup>85</sup></a><a class="footnote-ref" id="fnref:86" href="#fn:86"><sup>86</sup></a><a class="footnote-ref" id="fnref:87" href="#fn:87"><sup>87</sup></a><a class="footnote-ref" id="fnref:88" href="#fn:88"><sup>88</sup></a><a class="footnote-ref" id="fnref:89" href="#fn:89"><sup>89</sup></a><a class="footnote-ref" id="fnref:90" href="#fn:90"><sup>90</sup></a> </p> <h2 id="further-reading">Further reading</h2> <ul><li>Markham A (April 2019). "Relugolix: First Global Approval". <i>Drugs</i>. 79 (6): 675–679. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1007%2Fs40265-019-01105-0">10.1007/s40265-019-01105-0</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/30937733">30937733</a>. <a href="/facts/S2CID_(identifier)/ldJsHa2Y">S2CID</a> <a href="https://api.semanticscholar.org/CorpusID:89616869">89616869</a>.</li> <li>Elsharoud A, Ali M, Al-Hendy A (2019). "Relugolix. GnRH (LHRH) receptor antagonist, Treatment of uterine fibroids, Treatment of endometriosis-related pain, Treatment of prostate cancer". <i>Drugs of the Future</i>. 44 (2): 131. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1358%2Fdof.2019.44.2.2927590">10.1358/dof.2019.44.2.2927590</a>. <a href="/facts/ISSN_(identifier)/DPAflDvU">ISSN</a> <a href="https://search.worldcat.org/issn/0377-8282">0377-8282</a>. <a href="/facts/S2CID_(identifier)/ldJsHa2Y">S2CID</a> <a href="https://api.semanticscholar.org/CorpusID:87369995">87369995</a>.</li> <li>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". <i>Drugs of Today</i>. 55 (8): 503–512. <a href="/facts/Doi_(identifier)/muM9Etpq">doi</a>:<a href="https://doi.org/10.1358%2Fdot.2019.55.8.3020179">10.1358/dot.2019.55.8.3020179</a>. <a href="/facts/PMID_(identifier)/JlHAvMHt">PMID</a> <a href="https://pubmed.ncbi.nlm.nih.gov/31461087">31461087</a>. <a href="/facts/S2CID_(identifier)/ldJsHa2Y">S2CID</a> <a href="https://api.semanticscholar.org/CorpusID:201654739">201654739</a>.</li></ul> <h2 id="external-links">External links</h2> <ul><li>Clinical trial number <i><a href="https://www.clinicaltrials.gov/show/NCT03085095">NCT03085095</a></i> for "A Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer (HERO)" at <a href="/facts/ClinicalTrials.gov/X6WVgItm">ClinicalTrials.gov</a></li></ul> <h2 id="references">References</h2> <ol> <li id="fn:1"><p>"Orgovyx- relugolix tablet, film coated". DailyMed. Retrieved 25 May 2021. <a href="https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=077a92f6-9f1b-479a-87c7-c92b5db6aa9c" target="_blank">https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=077a92f6-9f1b-479a-87c7-c92b5db6aa9c</a> <a href="#fnref:1" class="footnote-back-ref">↩</a></p></li> <li id="fn:2"><p>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. S2CID 201654739. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:2" class="footnote-back-ref">↩</a></p></li> <li id="fn:3"><p>"Relumina (relugolix) Information" (PDF). ASKA Pharmaceutical (in Japanese). January 2019. Archived from the original (PDF) on 16 February 2019. Retrieved 16 February 2019. <a href="https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf" target="_blank">https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf</a> <a href="#fnref:3" class="footnote-back-ref">↩</a></p></li> <li id="fn:4"><p>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. S2CID 201654739. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:4" class="footnote-back-ref">↩</a></p></li> <li id="fn:5"><p>"Relumina (relugolix) Information" (PDF). ASKA Pharmaceutical (in Japanese). January 2019. Archived from the original (PDF) on 16 February 2019. Retrieved 16 February 2019. <a href="https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf" target="_blank">https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf</a> <a href="#fnref:5" class="footnote-back-ref">↩</a></p></li> <li id="fn:6"><p>"Relumina (relugolix) Information" (PDF). ASKA Pharmaceutical (in Japanese). January 2019. Archived from the original (PDF) on 16 February 2019. Retrieved 16 February 2019. <a href="https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf" target="_blank">https://web.archive.org/web/20190216153607/https://www.aska-pharma.co.jp/newitem/prd_relumina/data/info_new_relumina_1901_2.pdf</a> <a href="#fnref:6" class="footnote-back-ref">↩</a></p></li> <li id="fn:7"><p>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. S2CID 201654739. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:7" class="footnote-back-ref">↩</a></p></li> <li id="fn:8"><p>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. S2CID 201654739. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:8" class="footnote-back-ref">↩</a></p></li> <li id="fn:9"><p>Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, et al. (July 2011). "Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor". Journal of Medicinal Chemistry. 54 (14): 4998–5012. doi:10.1021/jm200216q. PMID 21657270. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:9" class="footnote-back-ref">↩</a></p></li> <li id="fn:10"><p>Nakata D, Masaki T, Tanaka A, Yoshimatsu M, Akinaga Y, Asada M, et al. (January 2014). "Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice". European Journal of Pharmacology. 723: 167–174. doi:10.1016/j.ejphar.2013.12.001. PMID 24333551. <a href="/wiki/Doi_(identifier)" target="_blank">/wiki/Doi_(identifier)</a> <a href="#fnref:10" class="footnote-back-ref">↩</a></p></li> <li id="fn:11"><p>Tukun FL, Olberg DE, Riss PJ, Haraldsen I, Kaass A, Klaveness J (December 2017). "Recent Development of Non-Peptide GnRH Antagonists". Molecules. 22 (12): 2188. doi:10.3390/molecules22122188. PMC 6149776. PMID 29232843. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6149776" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6149776</a> <a href="#fnref:11" class="footnote-back-ref">↩</a></p></li> <li id="fn:12"><p>Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. 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