Peringatan Keamanan

In case of overdose, monitor the patient for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed FDA Label. Common adverse reactions of elagolix include hot flush, headache, nausea, insomnia, mood alterations, amenorrhea, depression, anxiety, arthralgia, bone loss, changes in menstrual bleeding patterns, suicidal ideation and behavior, exacerbation of existing mood disorders, and/or hepatic transaminase elevations FDA Label.

The recommended duration of use for elagolix is up to 24 months for the 150 mg once daily dose and up to six months for the 200 mg twice daily dose, as it causes a dose-dependent decrease in bone mineral density (BMD) FDA Label. BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment FDA Label. For women with moderate hepatic impairment, the recommended dosage is 150 mg once daily for up to six months FDA Label.

Elagolix

DB11979

small molecule approved investigational

Deskripsi

Elagolix has been used in trials studying the basic science and treatment of Endometriosis, Folliculogenesis, Uterine Fibroids, Heavy Uterine Bleeding, and Heavy Menstrual Bleeding. As of 24 July 2018, however, the U.S. Food and Drug Administration (FDA) approved AbbVie's elagolix under the brand name Orilissa as the first and only oral gonadotropin-releasing hormone (GnRH) antagonist specifically developed for women with moderate to severe endometriosis pain F815.

It has been determined that endometriosis is one of the most common gynecologic disorders in the United States A35868, A35869, F801. In particular, estimates suggest that one in ten women of reproductive age is affected by endometriosis and experience debilitating pain symptoms A35868, A35869, F801. Moreover, women who are affected by this condition can suffer for up to six to ten years and visit multiple physicians before receiving a proper diagnosis A35868, A35869, F801. Subsequently, as Orilissa (elagolix) was approved by the FDA under priority review F815, this expedited new approval gives healthcare professionals another valuable option for treating the potentially unmet needs of women who are affected by endometriosis, depending on their specific type and severity of endometriosis pain.

Struktur Molekul 2D

Berat 631.6
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal phase elimination half-life of elagolix is recorded as being 4 to 6 hours [FDA Label].
Volume Distribusi The apparent volume of distribution at steady state (Vdss/F) of elagolix is reported to be 1674 for a 150 mg daily regimen and 881 for a 200 mg twice daily regimen [FDA Label].
Klirens (Clearance) The oral clearance (CL/F) of elagolix is 123 L/hr for a 150 mg once daily regimen and 144 L/hr for a 200 mg twice daily regimen [FDA Label].

Absorpsi

The Tmax of elagolix is reported as being 1.0 hours FDA Label. The effect of a high-fat meal (relative to fasting) can result in a reduction of the AUC and Cmax by as much as 24% and 36%, respectively FDA Label.

Metabolisme

Elagolix is predominantly metabolized by the CYP3A family of isoenzymes despite participating in minor metabolic pathways with the CYP2D6, CYP2C8, and uridine glucuronosyl transferases (UGTs) enzymes as well FDA Label. The primary metabolite of elagolix, referred to as NBI-61962 (R-(+)-4-{2-5-(2-fluoro-3-hydroxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl-1-phenyl-ethylamino}-butyrate) A35856, is not believed to possess any significant biologic activity due to its low plasma exposure and an observed potency that is exceptionally less than the parent elagolix compound (Ki value of 3.5 compared to 0.9 nM) A35855.

Rute Eliminasi

The primary route of elimination of elagolix is via hepatic metabolism FDA Label.

Interaksi Makanan

4 Data
  • 1. Administer calcium supplement. This will minimize the risk of bone mineral density loss.
  • 2. Administer vitamin supplements. Administer Vitamin D supplements to minimize the risk of bone mineral density loss.
  • 3. Take at the same time every day.
  • 4. Take with or without food.

Interaksi Obat

702 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Elagolix.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Elagolix.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Elagolix.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Elagolix.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Elagolix.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Elagolix.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Elagolix.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Elagolix.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Elagolix.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Elagolix.
Silodosin The excretion of Silodosin can be decreased when combined with Elagolix.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Elagolix.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Elagolix.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Elagolix.
Mifepristone The serum concentration of Elagolix can be increased when it is combined with Mifepristone.
Zidovudine The metabolism of Elagolix can be decreased when combined with Zidovudine.
Efavirenz The metabolism of Elagolix can be decreased when combined with Efavirenz.
Ethinylestradiol The metabolism of Elagolix can be decreased when combined with Ethinylestradiol.
Nelfinavir The excretion of Elagolix can be decreased when combined with Nelfinavir.
Mirabegron The serum concentration of Elagolix can be increased when it is combined with Mirabegron.
Capromab pendetide Elagolix may decrease effectiveness of Capromab pendetide as a diagnostic agent.
Vincristine The excretion of Vincristine can be decreased when combined with Elagolix.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Elagolix.
Lumacaftor The serum concentration of Elagolix can be decreased when it is combined with Lumacaftor.
Cyclosporine The metabolism of Elagolix can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Elagolix can be decreased when combined with Fluvoxamine.
Venlafaxine The metabolism of Elagolix can be decreased when combined with Venlafaxine.
Terfenadine The metabolism of Elagolix can be decreased when combined with Terfenadine.
Duloxetine The metabolism of Elagolix can be decreased when combined with Duloxetine.
Chlorpromazine The metabolism of Elagolix can be decreased when combined with Chlorpromazine.
Chloroquine The metabolism of Elagolix can be decreased when combined with Chloroquine.
Primaquine The metabolism of Elagolix can be decreased when combined with Primaquine.
Rolapitant The metabolism of Elagolix can be decreased when combined with Rolapitant.
Tipranavir The metabolism of Elagolix can be decreased when combined with Tipranavir.
Quinine The metabolism of Elagolix can be decreased when combined with Quinine.
Abiraterone The metabolism of Elagolix can be decreased when combined with Abiraterone.
Cholecalciferol The metabolism of Elagolix can be decreased when combined with Cholecalciferol.
Ketoconazole The metabolism of Elagolix can be decreased when combined with Ketoconazole.
Rucaparib The metabolism of Elagolix can be decreased when combined with Rucaparib.
Delavirdine The metabolism of Elagolix can be decreased when combined with Delavirdine.
Sulfaphenazole The metabolism of Elagolix can be decreased when combined with Sulfaphenazole.
Clozapine The serum concentration of Elagolix can be increased when it is combined with Clozapine.
Celecoxib The metabolism of Elagolix can be decreased when combined with Celecoxib.
Terbinafine The metabolism of Elagolix can be decreased when combined with Terbinafine.
Metoprolol The metabolism of Elagolix can be decreased when combined with Metoprolol.
Clobazam The serum concentration of Elagolix can be increased when it is combined with Clobazam.
Darifenacin The metabolism of Elagolix can be decreased when combined with Darifenacin.
Cimetidine The metabolism of Elagolix can be decreased when combined with Cimetidine.
Tranylcypromine The metabolism of Elagolix can be decreased when combined with Tranylcypromine.
Perhexiline The metabolism of Elagolix can be decreased when combined with Perhexiline.
Tegaserod The metabolism of Elagolix can be decreased when combined with Tegaserod.
Fusidic acid The metabolism of Elagolix can be decreased when combined with Fusidic acid.
Panobinostat The metabolism of Elagolix can be decreased when combined with Panobinostat.
Vilazodone The metabolism of Elagolix can be decreased when combined with Vilazodone.
Lumefantrine The metabolism of Elagolix can be decreased when combined with Lumefantrine.
Phenylbutyric acid The metabolism of Elagolix can be decreased when combined with Phenylbutyric acid.
Manidipine The metabolism of Elagolix can be decreased when combined with Manidipine.
Asunaprevir The metabolism of Elagolix can be decreased when combined with Asunaprevir.
Ritanserin The metabolism of Elagolix can be decreased when combined with Ritanserin.
Rhein The metabolism of Elagolix can be decreased when combined with Rhein.
Imipramine The metabolism of Elagolix can be decreased when combined with Imipramine.
Desipramine The metabolism of Elagolix can be decreased when combined with Desipramine.
Dosulepin The metabolism of Elagolix can be decreased when combined with Dosulepin.
Nicardipine The metabolism of Elagolix can be decreased when combined with Nicardipine.
Lorcaserin The metabolism of Elagolix can be decreased when combined with Lorcaserin.
Cisapride The metabolism of Elagolix can be decreased when combined with Cisapride.
Thioridazine The metabolism of Elagolix can be decreased when combined with Thioridazine.
Paroxetine The metabolism of Elagolix can be decreased when combined with Paroxetine.
Cinacalcet The metabolism of Elagolix can be decreased when combined with Cinacalcet.
Bupropion The metabolism of Elagolix can be decreased when combined with Bupropion.
Orphenadrine The metabolism of Elagolix can be decreased when combined with Orphenadrine.
Propafenone The metabolism of Elagolix can be decreased when combined with Propafenone.
Halofantrine The metabolism of Elagolix can be decreased when combined with Halofantrine.
Methotrimeprazine The metabolism of Elagolix can be decreased when combined with Methotrimeprazine.
Glycerol phenylbutyrate The metabolism of Elagolix can be decreased when combined with Glycerol phenylbutyrate.
Secobarbital The metabolism of Elagolix can be increased when combined with Secobarbital.
Rifampin The metabolism of Elagolix can be increased when combined with Rifampicin.
Bexarotene The metabolism of Elagolix can be decreased when combined with Bexarotene.
Levothyroxine The metabolism of Elagolix can be decreased when combined with Levothyroxine.
Medroxyprogesterone acetate The metabolism of Elagolix can be decreased when combined with Medroxyprogesterone acetate.
Irbesartan The metabolism of Elagolix can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Elagolix can be decreased when combined with Oxybutynin.
Fluvastatin The metabolism of Elagolix can be decreased when combined with Fluvastatin.
Pioglitazone The metabolism of Elagolix can be decreased when combined with Pioglitazone.
Topiroxostat The metabolism of Elagolix can be decreased when combined with Topiroxostat.
Teriflunomide The metabolism of Elagolix can be decreased when combined with Teriflunomide.
Genistein The metabolism of Elagolix can be decreased when combined with Genistein.
Diltiazem The metabolism of Elagolix can be decreased when combined with Diltiazem.
Loratadine The metabolism of Elagolix can be decreased when combined with Loratadine.
Trimethoprim The metabolism of Elagolix can be decreased when combined with Trimethoprim.
Fluticasone propionate The metabolism of Elagolix can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Elagolix can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Elagolix can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Elagolix can be decreased when combined with Salmeterol.
Felodipine The metabolism of Elagolix can be decreased when combined with Felodipine.
Gemfibrozil The metabolism of Elagolix can be decreased when combined with Gemfibrozil.
Fluticasone The metabolism of Elagolix can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Elagolix can be decreased when combined with Mometasone furoate.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Elagolix.
Vemurafenib The serum concentration of Elagolix can be increased when it is combined with Vemurafenib.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25581052
    Ezzati M, Carr BR: Elagolix, a novel, orally bioavailable GnRH antagonist under investigation for the treatment of endometriosis-related pain. Womens Health (Lond). 2015 Jan;11(1):19-28. doi: 10.2217/whe.14.68.
  • PMID: 19033369
    Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP: Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix. J Clin Endocrinol Metab. 2009 Feb;94(2):545-51. doi: 10.1210/jc.2008-1695. Epub 2008 Nov 25.
  • PMID: 27021205
    Melis GB, Neri M, Corda V, Malune ME, Piras B, Pirarba S, Guerriero S, Orru M, D'Alterio MN, Angioni S, Paoletti AM: Overview of elagolix for the treatment of endometriosis. Expert Opin Drug Metab Toxicol. 2016 May;12(5):581-8. doi: 10.1517/17425255.2016.1171316.
  • PMID: 20573927
    Giudice LC: Clinical practice. Endometriosis. N Engl J Med. 2010 Jun 24;362(25):2389-98. doi: 10.1056/NEJMcp1000274.
  • PMID: 21718982
    Nnoaham KE, Hummelshoj L, Webster P, d'Hooghe T, de Cicco Nardone F, de Cicco Nardone C, Jenkinson C, Kennedy SH, Zondervan KT: Impact of endometriosis on quality of life and work productivity: a multicenter study across ten countries. Fertil Steril. 2011 Aug;96(2):366-373.e8. doi: 10.1016/j.fertnstert.2011.05.090. Epub 2011 Jun 30.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Oriahnn
    Capsule; Kit • - • Oral • US • Approved
  • Oriahnn
    Capsule; Kit • - • Oral • US • Approved
  • Orilissa
    Tablet • 150 mg • Oral • Canada • Approved
  • Orilissa
    Tablet, film coated • 150 mg/1 • Oral • US • Approved
  • Orilissa
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Orilissa
    Tablet • 200 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

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