Entwicklung oraler nichtpeptidischer GnRH-Antagonisten

Zusammenfassung Elagolix ist ein neuer nichtpeptidischer GnRH(Gonadotropin-releasing Hormon)-Antagonist, der 2018 von der FDA (Food and Drug Administration) für die Behandlung mittlerer bis starker Schmerzen bei Endometriose zugelassen wurde. Im Gegensatz zu peptidischen GnRH-Antagonisten ist Elagolix oral verfügbar. In einer Serie von Phase-II- und Phase-III-Studien hat Elagolix eine vergleichbare Wirkung wie Gestagene und GnRH-Agonisten gezeigt. Das Wirkprinzip ist das gleiche wie bei allen GnRH-Analoga und basiert auf einer hypophysären Suppression mit konsekutiver hypoöstrogener Lage. Bezüglich der Nebenwirkungen ist Elagolix den GnRH-Agonisten ähnlich. Die kontrazeptive Sicherheit ist nicht belegt bzw. untersucht, sodass zusätzliche Maßnahmen zur Kontrazeption empfohlen werden. Abstract Elagolix is a new non-peptide gonadotropin-releasing hormone (GnRH) antagonist which was approved by the Food and Drug Administration (FDA) in 2018. It is registered for treatment of moderate to severe endometriosis-associated pain. In contrast to standard peptide GnRH antagonists, elagolix can be administered orally. In a series of phase II and phase III studies, elagolix demonstrated effectiveness comparable to GnRH agonists or progestins. Side effects were also similar to those of GnRH agonists. The mode of action is the same as for all GnRH analogues, and based on pituitary suppression followed by a hypoestrogenic state. Side effects of elagolix are comparable to those of GnRH agonists. Contraceptive safety has not been proven or investigated and additional contraceptive methods are thus recommended. Similar content being viewed by others Literatur Acs N, O’Brien C, Jiang P, Burke J, Jimenez R, Garner E, Chwalisz K (2015) Treatment of endometriosis-associated pain with elagolix, an oral gnrh antagonist: results from a phase 2, randomized controlled study. 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Gynäkologe 53, 510–516 (2020). https://doi.org/10.1007/s00129-020-04632-0 Published: Version of record: Issue date: DOI: https://doi.org/10.1007/s00129-020-04632-0