| ID Source | ID |
|---|---|
| PubMed CID | 11250647 |
| CHEMBL ID | 1208155 |
| CHEBI ID | 177453 |
| SCHEMBL ID | 1642523 |
| MeSH ID | M0534044 |
| Synonym |
|---|
| 4-[[(1r)-2-[5-(2-luoro-3-methoxyphenyl)-3-[[2-luoro-6-(triluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid |
| CHEBI:177453 |
| elagolix , |
| elagolix (usan/inn) |
| 834153-87-6 |
| D09335 |
| butanoic acid, 4-(((1r)-2-(5-(2-fluoro-3-methoxyphenyl)-3-((2-fluoro-6-(trifluoromethyl)phenyl)methyl)-3,6-dihydro-4-methyl-2,6-dioxo-1(2h)-pyrimidinyl)-1-phenylethyl)amino)- |
| elagolix [usan:inn] |
| 5b2546mb5z , |
| nbi-56418 |
| abt-620 |
| 4-(((1r)-2-(5-(2-fluoro-3-methoxyphenyl)-3-((2-fluoro-6-(trifluoromethyl)phenyl)methyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2h)-yl)-1-phenylethyl)amino)butanoic acid |
| unii-5b2546mb5z |
| CHEMBL1208155 |
| elagolix [who-dd] |
| elagolix [mi] |
| butanoic acid, 4-(((1r)-2-(5-(2-fluoro-3-methoxyphenyl)-3-((2-fluoro-6-(trifluoromethyl)phenyl)methyl)-3,6-dihydro-4-methyl-2,6-dioxo-1(2h)-pyrimidinyl)-1- phenylethyl)amino)- |
| elagolix [inn] |
| elagolix [usan] |
| 4-(((1r)-2-(5-(2-fluoro-3-methoxyphenyl)-3-((2-fluoro-6-(trifluoromethyl)phenyl)methyl)- 4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2h)-yl)-1-phenylethyl)amino)butanoic acid |
| orilissa |
| SCHEMBL1642523 |
| CS-5329 |
| HY-14789 |
| (r)-elagolix |
| DTXSID40232348 , |
| compound 10b [pmid 19006286] |
| gtpl8362 |
| nbi56418 |
| AC-30676 |
| 4-{[(1r)-2-[5-(2-fluoro-3-methoxyphenyl)-3-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-4-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-1-yl]-1-phenylethyl]amino}butanoic acid |
| EX-A1765 |
| DB11979 |
| BCP08827 |
| Q21098999 |
| AMY16504 |
| 834153-87-6 (free acid) |
| (r)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2h)-yl)-1-phenylethyl)amino)butanoic acid |
| MS-30861 |
| f5o , |
| 4-[[(1r)-2-[5-(2-fluoranyl-3-methoxy-phenyl)-3-[[2-fluoranyl-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-bis(oxidanylidene)pyrimidin-1-yl]-1-phenyl-ethyl]amino]butanoic acid |
| nbi-56418nbi-56418 |
| EN300-19807339 |
| heauokzivmzvql-vwlotqadsa-n |
| h01cc03 |
| elagolixum |
| compound 10b (pmid 19006286) |
| dtxcid40154839 |
| AKOS040733086 |
Elagolix sodium (ELS) is a marketed product using to release moderate to severe endometriosis-associated pain. ElagolIX is a gonadotropin-releasing hormone (GnRH) modulator and used for pain relief from endometria.
Treatment with elagolix 150 mg once daily was generally well-tolerated in this study, with no new safety signals. Elaglix treatment resulted in a decrease in COL1A1 production at 24 but not 48 hours.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Elagolix treatment resulted in a decrease in COL1A1 production at 24 but not 48 hours." | ( Relugolix and elagolix directly inhibit leiomyoma extracellular matrix production in 2-dimesnional and 3-dimensional cell cultures. Britten, J; Catherino, WH; Malik, M; Wright, D, 2022) | 1.8 |
| "Treatment with elagolix 150 mg once daily was generally well-tolerated in this study, with no new safety signals." | ( Low-Dose Elagolix for the Treatment of Heavy Menstrual Bleeding in Patients With Uterine Leiomyomas: A Randomized Controlled Trial. Brown, E; Kroll, R; Li, H; Ng, J; Pinsky, B; Rodriguez, JW; Snabes, MC; Thomas, J, 2023) | 1.67 |
| "Treatment with elagolix improved endometriosis-related workplace and household productivity impairments." | ( Impact of Elagolix on Workplace and Household Productivity Among Women with Moderate to Severe Pain Associated with Endometriosis: A Pooled Analysis of Two Phase III Trials. Agarwal, SK; Palac, HL; Soliman, AM; Surrey, ES, 2019) | 1.27 |
Coadministration of elagolix 150 mg once daily with oral contraceptives containing EE and norgestimate, or norethindrone, resulted in small pharmacokinetic changes in the oral contraceptive components. The aim of this analysis was to develop a physiologically based pharmacokinetically (PBPK) model that describes the enzyme-transporter interplay involved in the disposition of elAGolix.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Therefore, a robust model was developed to describe elagolix population pharmacokinetics and to evaluate factors affecting elagolix pharmacokinetic parameters." | ( Population Pharmacokinetics of Elagolix in Healthy Women and Women with Endometriosis. Degner, J; Klein, CE; Liu, M; Mostafa, NM; Nader, A; Ng, J; Noertersheuser, P; Polepally, AR; Winzenborg, I, 2018) | 1.02 |
| " Intensive pharmacokinetic blood samples were collected." | ( Elagolix Pharmacokinetic Profiles in Women With Renal or Hepatic Impairment. Duan, WR; Klein, CE; Marbury, T; Ng, J; Schmidt, JM, 2019) | 1.96 |
| " The aim of this analysis was to develop a physiologically based pharmacokinetic (PBPK) model that describes the enzyme-transporter interplay involved in the disposition of elagolix and to predict the magnitude of drug-drug interaction (DDI) potential of elagolix as an inhibitor of P-glycoprotein (P-gp) and inducer of cytochrome P450 (CYP) 3A4." | ( Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling. Chiney, MS; Gibbs, JP; Ng, J; Shebley, M, 2020) | 1.05 |
| "In study 1, pharmacokinetic exposures for EE in period 2 increased by 30% and the norgestimate metabolites decreased by approximately 15% when coadministered with elagolix." | ( Pharmacokinetic and Pharmacodynamic Profiles of Ethinylestradiol/Norgestimate Combination or Norethindrone upon Coadministration with Elagolix 150 mg Once Daily in Healthy Premenopausal Women. Chiu, YL; Feldman, RA; Klein, CE; Ng, J, 2021) | 1.02 |
| "Coadministration of elagolix 150 mg once daily with oral contraceptives containing EE and norgestimate, or norethindrone, resulted in small pharmacokinetic changes in the oral contraceptive components." | ( Pharmacokinetic and Pharmacodynamic Profiles of Ethinylestradiol/Norgestimate Combination or Norethindrone upon Coadministration with Elagolix 150 mg Once Daily in Healthy Premenopausal Women. Chiu, YL; Feldman, RA; Klein, CE; Ng, J, 2021) | 1.15 |
| "The aim of this analysis was to use a physiologically based pharmacokinetic (PBPK) model to predict the impact of changes in dissolution rates on elagolix exposures and define clinically relevant acceptance criteria for dissolution." | ( Physiologically based pharmacokinetic modeling and simulations to inform dissolution specifications and clinical relevance of release rates on elagolix exposure. Chiney, MS; Ju, TR; Marroum, P; Mukherjee, D; Shao, X; Shebley, M, 2022) | 1.12 |
| "In 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 with in vitro dissolution data to test for virtual bioequivalence." | ( Virtual Bioequivalence Assessment of Elagolix Formulations Using Physiologically Based Pharmacokinetic Modeling. Chen, MJ; Ju, TR; Marroum, P; Mukherjee, D; Shao, X; Shebley, M, 2023) | 1.39 |
Elagolix is an oral gonadotropin-releasing hormone receptor antagonist. It is indicated for the management of endometriosis-associated pain and in combination with estradiol/norethindrone acetate.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The aim of this analysis was to develop a physiologically based pharmacokinetic (PBPK) model that describes the enzyme-transporter interplay involved in the disposition of elagolix and to predict the magnitude of drug-drug interaction (DDI) potential of elagolix as an inhibitor of P-glycoprotein (P-gp) and inducer of cytochrome P450 (CYP) 3A4." | ( Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling. Chiney, MS; Gibbs, JP; Ng, J; Shebley, M, 2020) | 1.05 |
| "No change in norethindrone maximum plasma concentration or area under the concentration-time curve was observed when oral E2/NETA was administered with elagolix." | ( Drug-Drug Interaction Studies of Elagolix with Oral and Transdermal Low-Dose Hormonal Add-Back Therapy. Ali, F; Mostafa, NM; Nader, A; Shebley, M, 2021) | 1.1 |
| "Elagolix is an oral gonadotropin-releasing hormone receptor antagonist indicated for the management of endometriosis-associated pain and in combination with estradiol/norethindrone acetate indicated for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women." | ( Assessment of Clinical Drug-Drug Interactions of Elagolix, a Gonadotropin-Releasing Hormone Receptor Antagonist. Carter, DC; Dufek, MB; Kamradt, K; Mostafa, NM; Ng, JW; Parikh, A; Polepally, AR; Salem, AH; Shebley, M, 2020) | 2.26 |
18a revealed improved bioavailability and superior gonadotropic suppression activity compared with Elagolix. Out of the covariates tested, only organic anion transporting polypeptide 1B1 genotype status and body weight had a statistically significant but no clinically meaningful effect.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pharmacokinetic and pharmacodynamic evaluations of 18a revealed improved bioavailability and superior gonadotropic suppression activity compared with Elagolix, the most clinically advanced compound." | ( Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. Ann, J; Han, MY; Kim, EJ; Kim, SM; Lee, J; Lee, M; Lee, SM; Lee, SY; Park, E; Yoo, T; Yoon, S, 2016) | 0.63 |
| " Out of the covariates tested on elagolix apparent clearance, apparent volume of distribution, and/or relative bioavailability, only organic anion transporting polypeptide 1B1 genotype status and body weight had a statistically significant but no clinically meaningful effect on elagolix relative bioavailability and apparent volume of distribution, respectively." | ( Population Pharmacokinetics of Elagolix in Combination with Low-Dose Estradiol/Norethindrone Acetate in Women with Uterine Fibroids. Beck, D; Degner, J; Liu, M; Mostafa, NM; Noertersheuser, P; Shebley, M; Winzenborg, I, 2022) | 1.29 |
Elagolix was administered orally for 3 continuous 28-day dosing intervals at 100 to 200 mg once daily (QD), 100 to 300 mg twice daily (BID), and 300 mg BID plus estradiol/norethindrone acetate (E2/NETA) 1/0. Placebo patients were rerandomized to elaglix and elagolIX patients continued their dosing assignment for 12 additional weeks.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Placebo patients were rerandomized to elagolix and elagolix patients continued their dosing assignment for 12 additional weeks; the primary efficacy measure was changed from baseline in the monthly mean numerical rating scale for pain at week 12." | ( Elagolix treatment for endometriosis-associated pain: results from a phase 2, randomized, double-blind, placebo-controlled study. Burke, J; Carr, B; Chwalisz, K; Diamond, MP; Dmowski, WP; Garner, E; Jiang, P; Jimenez, R; Koltun, W; O'Brien, C, 2014) | 2.11 |
| " No dosage adjustment was needed in women with renal impairment or women with mild hepatic impairment." | ( Elagolix Pharmacokinetic Profiles in Women With Renal or Hepatic Impairment. Duan, WR; Klein, CE; Marbury, T; Ng, J; Schmidt, JM, 2019) | 1.96 |
| "Elagolix was administered orally for 3 continuous 28-day dosing intervals at 100 to 200 mg once daily (QD), 100 to 300 mg twice daily (BID), and 300 mg BID plus estradiol/norethindrone acetate (E2/NETA) 1/0." | ( Elagolix Suppresses Ovulation in a Dose-Dependent Manner: Results From a 3-Month, Randomized Study in Ovulatory Women. Archer, DF; Chiu, YL; Chwalisz, K; Feinberg, EC; Feldman, RA; Klein, CE; Miller, CE; Ng, J, 2020) | 3.44 |
| "A PBPK model of elagolix was developed, verified, and applied to characterize the disposition interplay between CYP3A4 and OATP1B1, and to predict the DDI potential of elagolix as a perpetrator under dosing conditions that were not tested clinically." | ( Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling. Chiney, MS; Gibbs, JP; Ng, J; Shebley, M, 2020) | 1.2 |
| " These studies enabled a comprehensive understanding of elagolix mechanism of action and the downstream pharmacodynamic (PD) effects on gonadotropin and ovarian hormones, as well as full characterization of the PK/PD (PKPD) relationships of elagolix at various dosages, including the approved 150 mg once daily and 200 mg twice daily dosing regimens for the management of moderate to severe pain associated with endometriosis." | ( Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis. Gibbs, MA; Klein, CE; Mostafa, NM; Nader, A; Ng, JW; Noertersheuser, P; Polepally, AR; Shebley, M; Winzenborg, I, 2020) | 1.11 |
| " The availability of two dosing options allows for individualization of treatment based on baseline clinical factors and response to therapy." | ( A Clinician's Guide to the Treatment of Endometriosis with Elagolix. Advincula, AP; Estes, SJ; Lessey, BA; Leyland, N; Taylor, HS, 2021) | 0.86 |
| "The 200 mg twice daily dosage of elagolix is more likely to be preferred over leuprolide by patients with moderate to severe endometriosis-related pain in all scenarios explored in the evaluation and sensitivity analyses." | ( Patient preferences for elagolix and leuprolide for treating endometriosis-related pain in the United States. Agarwal, SK; Poulos, C; Soliman, AM; Tekin, S, 2021) | 1.21 |
| " A dose-response model that describes the relationship between elagolix dosages and average E2 levels was combined with a previously published quantitative systems pharmacology (QSP) model of calcium homeostasis to predict bone mineral density (BMD) changes during and following elagolix treatment." | ( Validation of a quantitative systems pharmacology model of calcium homeostasis using elagolix Phase 3 clinical trial data in women with endometriosis. Mostafa, NM; Nader, A; Ng, J; Noertersheuser, P; Polepally, AR; Shebley, M; Stodtmann, S; Suleiman, AA; Winzenborg, I, 2021) | 1.08 |
| " Serial blood samples for assay of omeprazole and its metabolites were collected for 24 h after dosing on days 1 and 11." | ( Effects of elagolix on the pharmacokinetics of omeprazole and its metabolites in healthy premenopausal women. Kim, E; Mostafa, NM; Nader, A; Shebley, M, 2022) | 1.11 |
| " Almost all efficacy- and safety-related outcomes showed a dose-response relationship." | ( Oral gonadotropin-releasing hormone antagonists for treating endometriosis-associated pain: a systematic review and network meta-analysis. Dai, Y; Gu, Z; Leng, J; Li, X; Shi, J; Wu, Y; Yan, H; Zhang, C; Zhang, J, 2022) | 0.72 |
| "The forced degradation study suggested that the developed method is specific and stability-indicating and can be used for related substance analysis of elagolix drug substance and its dosage forms." | ( LC-MS-Compatible Chromatographic Method for Quantification of Potential Organic Impurities of Elagolix Sodium in Tablet Dosage Form with Identification of Major Degradation Products. Chokshi, A; Desai, P; Prajapati, R, 2023) | 1.33 |
| "08 µg/mL) HPLC method for quantification of all probable impurities of elagolix in tablet dosage forms." | ( LC-MS-Compatible Chromatographic Method for Quantification of Potential Organic Impurities of Elagolix Sodium in Tablet Dosage Form with Identification of Major Degradation Products. Chokshi, A; Desai, P; Prajapati, R, 2023) | 1.36 |
| Class | Description |
|---|---|
| organooxygen compound | An organochalcogen compound containing at least one carbon-oxygen bond. |
| organonitrogen compound | Any heteroorganic entity containing at least one carbon-nitrogen bond. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346002 | Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (2.53) | 29.6817 |
| 2010's | 30 (37.97) | 24.3611 |
| 2020's | 47 (59.49) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (74.90) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 21 (26.25%) | 5.53% |
| Reviews | 20 (25.00%) | 6.00% |
| Case Studies | 3 (3.75%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 36 (45.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||