{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,7,30]],"date-time":"2025-07-30T10:07:14Z","timestamp":1753870034955,"version":"3.41.2"},"reference-count":31,"publisher":"Wiley","issue":"1","license":[{"start":{"date-parts":[[2025,1,30]],"date-time":"2025-01-30T00:00:00Z","timestamp":1738195200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Pharmacology Res &amp; Perspec"],"published-print":{"date-parts":[[2025,2]]},"abstract":"<jats:title>ABSTRACT<\/jats:title><jats:p>Relugolix is an oral gonadotropin\u2010releasing hormone receptor antagonist that suppresses sex steroid hormones and is approved as monotherapy for prostate cancer and as a fixed\u2010dose combination with estradiol\/norethindrone for the treatment of endometriosis and uterine fibroids. The aim of this postmarketing study was to determine the pharmacokinetics and quantify the amount of relugolix excreted into breast milk of healthy lactating women. Following a single, oral dose of 40\u2009mg relugolix, breast milk was sampled over 120\u2009h. Pharmacokinetic parameters were determined, including the cumulative amount of relugolix excreted into breast milk to derive the total infant dose. The safety and tolerability of relugolix were also assessed. Eight healthy lactating women were enrolled and completed the study per protocol. Relugolix was safe and well tolerated based on adverse events and other safety data. It was excreted into breast milk with a median time to peak concentration (<jats:italic>t<\/jats:italic><jats:sub>max<\/jats:sub>) of 5.81\u2009h and a geometric mean peak concentration (<jats:italic>C<\/jats:italic><jats:sub>max<\/jats:sub>) of 15.7\u2009ng\/mL, similar to corresponding plasma data from previous clinical studies. The mean cumulative amount of relugolix excreted was 0.0051\u2009mg over 24\u2009h and 0.0067\u2009mg over 120\u2009h, corresponding to 0.0128% and 0.0167% of the maternal dose, respectively. The body weight\u2010adjusted relative daily infant dose of approximately 0.25% suggests a 400\u2010fold lower newborn than maternal relugolix exposure. Relevant effects of relugolix on the breastfed child appear unlikely given its limited excretion into breast milk of lactating women but cannot be fully excluded in the absence of infant safety data.<\/jats:p>","DOI":"10.1002\/prp2.70067","type":"journal-article","created":{"date-parts":[[2025,1,31]],"date-time":"2025-01-31T04:03:59Z","timestamp":1738296239000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Transfer of the Oral Gonadotropin\u2010Releasing Hormone Receptor Antagonist Relugolix Into Breast Milk of Healthy Lactating Women"],"prefix":"10.1002","volume":"13","author":[{"given":"Darin B.","family":"Brimhall","sequence":"first","affiliation":[{"name":"PPD Incorporation\u2014Thermo Fisher Scientific  Waltham Massachusetts USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yu\u2010Luan","family":"Chen","sequence":"additional","affiliation":[{"name":"Sumitomo Pharma America  Marlborough Massachusetts USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sarah","family":"Lee","sequence":"additional","affiliation":[{"name":"Sumitomo Pharma America  Marlborough Massachusetts USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kazumasa","family":"Yoshida","sequence":"additional","affiliation":[{"name":"Sumitomo Pharma Co. Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6637-4406","authenticated-orcid":false,"given":"Mike","family":"Ufer","sequence":"additional","affiliation":[{"name":"Sumitomo Pharma Switzerland GmbH  Basel Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2025,1,30]]},"reference":[{"issue":"2","key":"e_1_2_11_2_1","doi-asserted-by":"crossref","first-page":"73","DOI":"10.1016\/j.xfre.2022.11.010","article-title":"Development of Relugolix Combination Therapy as a Medical Treatment Option for Women With Uterine Fibroids or Endometriosis","volume":"4","author":"Arjona Ferreira J. 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