Elagolix - a novel drug for management of endometriosis and uterine fibroids

Abstract

Endometriosis and uterine fibroids are two hormone-dependent gynecological disorders that significantly impact women’s health impairing their quality of life. Traditional medical therapies used to control symptoms have side effects such as initial symptom flare and hypoestrogenic complications which limit their use. Elagolix is an oral non-peptide gonadotropin releasing hormone receptor (GnRH) antagonist. It is a new therapeutic approach which acts by directly and reversibly suppressing pituitary gonadotropin secretion. It acts by binding competitively to GnRH receptors in pituitary gland which leads to a rapid dose dependent suppression of LH and FSH leading to reduction in production of ovarian sex hormones (estrogen and progesterone). Alternative medications like GnRH agonists cause a transient hormone flare which is complete and long lasting before down regulation. Elagolix immediately inhibits GnRH receptor signaling, avoiding this flare phenomenon. The degree of hormonal suppression can be adjusted by dosing, allowing partial or near-complete suppression of estradiol levels, which is beneficial for tailoring therapy to minimize hypoestrogenic side effects. Elagolix, offers a safe and effective approach in the management of uterine fibroids and endometriosis. Clinical trials have demonstrated that Elagolix significantly reduces fibroid-associated heavy menstrual bleeding and alleviates endometriosis-related pelvic pain. Its rapid onset of action and adjustable dosing regimen allow individualized therapy aimed at balancing efficacy and minimizing hypoestrogenic adverse effects such as bone mineral density loss and vasomotor symptoms.