2. Academic Validation
  3. Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas

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. doi: 10.1080/13543784.2021.1957830.
Susan Dababou 1,  Simone Garzon 1,  Antonio Simone Laganà 2,  Simone Ferrero 3 4,  Giulio Evangelisti 3 4,  Marco Noventa 5,  Maurizio Nicola D'Alterio 6,  Stefano Palomba 7,  Stefano Uccella 1,  Massimo Franchi 1,  Fabio Barra 3 4
Affiliations

Affiliations

  • 1 Department of Obstetrics and Gynecology, AOUI Verona, University of Verona, Verona, Italy.
  • 2 Department of Obstetrics and Gynecology, "Filippo Del Ponte" Hospital, University of Insubria, Varese (VA), Italy.
  • 3 Department of Neurosciences, Rehabilitation, Ophthalmology, Genetics, Maternal and Child Health (Dinogmi), University of Genova, Italy.
  • 4 Academic Unit of Obstetrics and Gynecology, IRCCS Ospedale Policlinico San Martino, Genova, Italy.
  • 5 Department of Women and Children's Health, Clinic of Gynecology and Obstetrics, University of Padua, Padua, Italy.
  • 6 Department of Surgical Sciences, Section of Obstetrics & Gynecology, University of Cagliari, Monserrato, Italy.
  • 7 Department of Experimental and Clinical Medicine, University Magna Graecia of Catanzaro, Catanzaro, Italy.
PMID: 34278887 DOI: 10.1080/13543784.2021.1957830
Abstract

Introduction: Uterine myomas and endometriosis are benign hormone-dependent diseases affecting women of reproductive age. Substantial efforts have been made to develop innovative medical options for treating these gynecologic diseases. Elagolix and relugolix have been approved in some countries for treating endometriosis and myomas, respectively; however, linzagolix (OBE 2109, KLH 2109) is a new oral gonadotropin-releasing hormone (GnRH) antagonist in phase II-III trials. Treatment options for women with contraindications for hormonal therapies or who refuse particular options, are the driving force behind the development of new drugs in this area.

Area covered: This drug evaluation highlights definitive and preliminary results from previous and ongoing studies of linzagolix for the treatment of endometriosis and myomas.

Expert opinion: Linzagolix showed a dose-dependent and rapidly reversible action on the pituitary-gonadal axis. In a recent phase II trial (EDELWEISS), linzagolix significantly reduced pain related to endometriosis and improved quality of life at single daily doses of 75-200 mg. The preliminary results of international, double-blind phase III trials (PRIMROSE 1 and 2) reported its efficacy in treating heavy menstrual bleeding related to myomas with a good safety profile. Further studies will determine the necessity of add-back therapy during long-term use of linzagolix.

Keywords

Endometriosis; GnRH antagonist; KLH 2109; OBE 2109; heavy menstrual bleeding; hormonal therapy; linzagolix; uterine myomas.

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