Bioequivalence of Elagolix/Estradiol/Norethindrone Acetate Fixed ‐Dose Combination Product: Phase 1 Results in Healthy Pre‐ and Postmenopausal Women
AbstractFixed-dose combination (FDC) therapies can enhance patient convenience and adherence to prescribed treatment regimens. Elagolix is a novel oral gonadotropin-releasing hormone receptor antagonist approved for management of moderate to severe pain associated with endometriosis and heavy menstrual bleeding associated with uterine fibroids. Hormonal add-back therapy can attenuate the reversible hypoestrogenic effects of elagolix. An FDC formulation containing elagolix/estradiol (E2)/norethindrone acetate (NETA) 300/1/0.5 mg as the morning dose and an elagolix 300 mg capsule as the evening dose, were evaluated in 2 b...
Source: Clinical Pharmacology in Drug Development - April 10, 2024 Category: Drugs & Pharmacology Authors: Mong ‐Jen Chen,
Patrick Marroum,
Yi‐Lin Chiu,
Melina Neenan,
Nael M. Mostafa,
Mohamad Shebley Tags: Original Article Source Type: research
Relugolix/Estradiol/Norethisterone Acetate: A Review in Endometriosis-Associated Pain
AbstractAn oral fixed-dose combination of relugolix/estradiol/norethisterone (also known as norethindrone) acetate [Myfembree® (USA); Ryeqo® (EU)] (hereafter referred to as relugolix combination therapy) has been approved in the USA for the management of moderate to severe pain associated with endometriosis in premenopausal women and in the EU for the symptomatic treatment of endometriosis in adult women of reproductive age with a history of previous medical or surgical treatment for their endometriosis. The gonadotropin-releasing hormone (GnRH) receptor antagonist relugolix decreases estradiol and progesterone levels, w...
Source: Drugs - April 9, 2024 Category: Drugs & Pharmacology Source Type: research
Oral GnRH Antagonists in Combination with Estradiol and Norethindrone Acetate for Pain Relief Associated with Endometriosis: A Review of Evidence of a Novel Class of Hormonal Agents
(Source: International Journal of Womens Health)
Source: International Journal of Womens Health - February 27, 2024 Category: OBGYN Tags: International Journal of Women's Health Source Type: research
10173 Long-Term Therapy of Elagolix + Add-Back Therapy in Women with Endometriosis-Associated Pain for 48 Months: Update on Bone Mineral Density
To report the 48-month bone mineral density data of a phase 3 study evaluating the long-term safety of elagolix 200 mg twice daily (ELA) with add-back therapy (AB, estradiol 1 mg/0.5 mg norethindrone acetate) for treatment of endometriosis-associated pain (EAP; NCT03213457). (Source: The Journal of Minimally Invasive Gynecology)
Source: The Journal of Minimally Invasive Gynecology - October 27, 2023 Category: OBGYN Authors: JH Kim, JA Simon, P Miller, J Ng, A Chan, J Thomas, M Snabes Source Type: research
Relugolix Combination Therapy in Black/African American Women with Symptomatic Uterine Fibroids: LIBERTY Long-Term Extension Study
In the LIBERTY Long-Term Extension study, once-daily relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) significantly improved uterine fibroid-associated heavy menstrual bleeding over the 52-week treatment period in the overall study population. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - October 18, 2023 Category: OBGYN Authors: Elizabeth A. STEWART, Ayman AL-HENDY, Andrea S. LUKES, O. Sandra MADUEKE-LAVEAUX, Emily ZHU, Sarah PROEHL, Thierry SCHULMANN, Erica E. MARSH Tags: Original Research: Gynecology Source Type: research
Bone mineral density after two years of treatment with relugolix combination therapy and one-year post-treatment follow-up in women with endometriosis: spirit program
To evaluate bone mineral density (BMD) changes in women with endometriosis (EM)-associated pain treated with relugolix combination therapy (Rel-CT: relugolix 40 mg, estradiol 1 mg and norethindrone acetate 0.5 mg) in the SPIRIT long-term extension (LTE) study through 104 weeks and post-treatment follow-up (PTFU) for 12 months. (Source: Fertility and Sterility)
Source: Fertility and Sterility - October 1, 2023 Category: Reproduction Medicine Authors: Michael R. McClung, Neil Johnson, Steven R. Cummings, Serge L. Ferrari, Julie S. Perry, Yi Zhong, Rachel B. Wagman Source Type: research
36-month bone mineral density results in women treated with elagolix + add-back therapy for heavy menstrual bleeding associated with uterine fibroids
To evaluate the long-term (36-month) effect of elagolix 300 mg twice daily in combination with add-back therapy (estradiol 1 mg/norethindrone acetate 0.5 mg; ELA+AB) on bone mineral density (BMD) in premenopausal women treated for HMB associated with UF enrolled in an ongoing phase 3b, 48-month study for UF-associated HMB (NCT03271489). (Source: Fertility and Sterility)
Source: Fertility and Sterility - October 1, 2023 Category: Reproduction Medicine Authors: Vicki L. Schnell, Juki Ng, Eric Brown, Liesl K. Bredeson, James W. Thomas, Anna Chan, Michael C. Snabes Source Type: research
Long-term therapy of elagolix + add-back therapy in women with endometriosis-associated pain for 48 months: a safety update on bone mineral density data of a phase 3 study
To report the 48-month bone mineral density data of a phase 3 study evaluating the long-term safety of elagolix 200 mg twice daily (ELA) with add-back therapy (AB, estradiol 1 mg/0.5 mg norethindrone acetate) for treatment of endometriosis-associated pain (EAP; NCT03213457). (Source: Fertility and Sterility)
Source: Fertility and Sterility - October 1, 2023 Category: Reproduction Medicine Authors: James A. Simon, Jin Hee Kim, James W. Thomas, Juki Ng, Paul B. Miller, Anna Chan, Michael C. Snabes Source Type: research
LIBERTY Randomized Withdrawal Study: Relugolix Combination Therapy for Heavy Menstrual Bleeding Associated With Uterine Fibroids
In the pivotal LIBERTY 1 and 2 trials and long-term extension (LTE) study, once-daily relugolix combination therapy (relugolix CT: relugolix 40 mg, estradiol 1 mg, norethindrone acetate 0.5 mg) reduced menstrual blood loss (MBL) volume and pain in women with uterine fibroids (UF). Relugolix CT was well tolerated, with preservation of bone mineral density (BMD) through 52 weeks. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - September 2, 2023 Category: OBGYN Authors: Ayman AL-HENDY, Roberta VENTURELLA, Juan Camilo ARJONA FERREIRA, Yulan Li, Graziella SOULBAN, Rachel B. WAGMAN, Andrea S. LUKES Tags: Original Research: Gynecology Source Type: research
A Randomized Open-Label Study of Relugolix Alone or Relugolix Combination Therapy in Premenopausal Women
ConclusionsRelugolix 40 mg in combination with E2 1 mg and NETA 0.5 mg provided systemic E2 concentrations within a range expected to minimize the risk of undesirable effects of hypoestrogenism associated with the administration of relugolix alone.Clinical Trial RegistrationClinicaltrials.gov identifier no. NCT04978688. Trial registration date: 27 July, 2021; retrospectively registered. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - June 26, 2023 Category: Drugs & Pharmacology Source Type: research
Virtual Bioequivalence Assessment of Elagolix Formulations Using Physiologically Based Pharmacokinetic Modeling
AbstractIn lieu of large bioequivalence studies and exposing healthy postmenopausal women to additional drug exposure for elagolix coadministered with hormonal add-back therapy, physiologically based pharmacokinetic (PBPK) modeling was used within vitro dissolution data to test for virtual bioequivalence. For endometriosis, elagolix is approved at doses of 150 mg once daily and 200 mg twice daily as a tablet. As a combination therapy, two individual tablets, consisting of an elagolix tablet and an estradiol/norethindrone acetate 1/0.5 mg (E2/NETA) tablet, were utilized in Phase 3 endometriosis trials. However, the comm...
Source: The AAPS Journal - March 22, 2023 Category: Drugs & Pharmacology Source Type: research
Correction: Relugolix/Estradiol/Norethisterone (Norethindrone) Acetate: A Review in Symptomatic Uterine Fibroids
(Source: Drugs)
Source: Drugs - November 23, 2022 Category: Drugs & Pharmacology Source Type: research
Long-term Relugolix Combination Therapy for Symptomatic Uterine Leiomyomas
CONCLUSION: Improvements in heavy menstrual bleeding and anemia and reduction of uterine leiomyoma-associated symptom burden were sustained through up to 52 weeks of treatment with relugolix combination therapy in women with uterine leiomyomas. No new safety concerns were identified, and BMD was maintained.CLINICAL TRIALS REGISTRATION: ClinicalTrials.gov, NCT03049735; NCT03103087; NCT03412890.FUNDING SOURCE: Myovant Sciences GmbH.PMID:36357960 | DOI:10.1097/AOG.0000000000004988 (Source: Obstetrics and Gynecology)
Source: Obstetrics and Gynecology - November 11, 2022 Category: OBGYN Authors: Ayman Al-Hendy Andrea S Lukes Alfred N Poindexter Roberta Venturella Claudio Villarroel Laura McKain Yulan Li Rachel B Wagman Elizabeth A Stewart Source Type: research
