Peringatan Keamanan

Data regarding overdose of relugolix are unavailable.

Relugolix

DB11853

small molecule approved investigational

Deskripsi

Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions. It was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids,A225816 and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer.L27991,L27996 This branded product was later approved by the European Commission on April 29, 2022.L42150 Relugolix has also been studied in the symptomatic treatment of endometriosis.A225761

Relugolix is the first (and currently only) orally-administered GnRH receptor antagonist approved for the treatment of prostate cancer - similar therapies such as degarelix require subcutaneous administration - and therefore provides a less burdensome therapeutic option for patients who might otherwise require clinic visits for administration by healthcare professionals.L27996 In addition to its relative ease-of-use, relugolix was shown to be superior in the depression of testosterone levels when compared to leuprolide, another androgen deprivation therapy used in the treatment of prostate cancer.A225926 In May 2021, the FDA approved the combination product made up of relugolix, estradiol, and norethindrone under the market name Myfembree for the first once-daily treatment for the management of heavy menstrual bleeding associated with uterine fibroids in premenopausal women.L34289

Struktur Molekul 2D

Berat 623.64
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average effective half-life of relugolix is 25 hours, while the average terminal elimination half-life is 60.8 hours.[L27991]
Volume Distribusi -
Klirens (Clearance) The average renal clearance of relugolix is 8 L/h with a total clearance of 26.4 L/h.[L27991]

Absorpsi

The Cmax and AUC of orally-administered relugolix increase proportionally following single doses - in contrast, with repeat dosing the AUC remains proportional to the dose while the Cmax increases greater than proportionally to the dose.L27991 Following the administration of 120mg once daily, the steady-state AUC and Cmax of relugolix were 407 (± 168) ng.hr/mL and 70 (± 65) ng/mL, respectively. The absolute oral bioavailability of relugolix is approximately 12% and the median Tmax following oral administration is 2.25 hours.L27991

Metabolisme

Relugolix is metabolized mainly by the CYP3A subfamily of P450 enzymes, with a smaller contribution by CYP2C8.L27991

Rute Eliminasi

Approximately 81% of an orally administered dose was recovered in the feces, of which 4.2% was unchanged parent drug, while 4.1% of the dose was recovered in the urine, of which 2.2% remained unchanged.L27991

Interaksi Makanan

1 Data
  • 1. Take with or without food. Administration with food does not result in any clinically meaningful differences in pharmacokinetics.

Interaksi Obat

732 Data
Choline C 11 Relugolix may decrease effectiveness of Choline C 11 as a diagnostic agent.
Capromab pendetide Relugolix may decrease effectiveness of Capromab pendetide as a diagnostic agent.
Leuprolide The risk or severity of QTc prolongation can be increased when Relugolix is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Goserelin.
Azithromycin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Relugolix is combined with Sulfisoxazole.
Amitriptyline The risk or severity of QTc prolongation can be increased when Relugolix is combined with Amitriptyline.
Methadone The risk or severity of QTc prolongation can be increased when Relugolix is combined with Methadone.
Clozapine The metabolism of Relugolix can be decreased when combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Relugolix is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Relugolix is combined with Droperidol.
Imipramine The serum concentration of Imipramine can be increased when it is combined with Relugolix.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Chlorpromazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Oxaliplatin.
Ciprofloxacin The metabolism of Relugolix can be decreased when combined with Ciprofloxacin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Relugolix is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Relugolix is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Atropine.
Chloroquine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Chloroquine.
Adenosine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Relugolix is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Relugolix is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Relugolix is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Cinoxacin.
Granisetron The risk or severity of QTc prolongation can be increased when Relugolix is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Relugolix is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Relugolix is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Relugolix is combined with Dimenhydrinate.
Emedastine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Emedastine.
Primaquine The metabolism of Relugolix can be decreased when combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Ofloxacin.
Flecainide The risk or severity of QTc prolongation can be increased when Relugolix is combined with Flecainide.
Quetiapine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Quetiapine.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Relugolix is combined with Levacetylmethadol.
Clomipramine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Clomipramine.
Probucol The risk or severity of QTc prolongation can be increased when Relugolix is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Relugolix is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Relugolix is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Relugolix is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Telavancin.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Relugolix.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Nemonoxacin.
Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Relugolix.
Nilvadipine The metabolism of Relugolix can be decreased when combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Relugolix is combined with Antazoline.
Bedaquiline The risk or severity of QTc prolongation can be increased when Relugolix is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Relugolix is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Relugolix is combined with Eperisone.
Butriptyline The risk or severity of QTc prolongation can be increased when Relugolix is combined with Butriptyline.
Ceritinib The serum concentration of Ceritinib can be increased when it is combined with Relugolix.
Lenvatinib The serum concentration of Relugolix can be increased when it is combined with Lenvatinib.
Melperone The risk or severity of QTc prolongation can be increased when Relugolix is combined with Melperone.
Benidipine The metabolism of Relugolix can be decreased when combined with Benidipine.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Relugolix is combined with Dexchlorpheniramine maleate.
Delamanid The risk or severity of QTc prolongation can be increased when Relugolix is combined with Delamanid.
Amifampridine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Amifampridine.
Encorafenib The serum concentration of Relugolix can be increased when it is combined with Encorafenib.
Mocetinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Entinostat.
Gilteritinib The serum concentration of Gilteritinib can be increased when it is combined with Relugolix.
CUDC-101 The risk or severity of QTc prolongation can be increased when Relugolix is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Relugolix is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Relugolix is combined with Abexinostat.
Oxatomide The risk or severity of QTc prolongation can be increased when Relugolix is combined with Oxatomide.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Relugolix is combined with Sitafloxacin.
Sultopride The risk or severity of QTc prolongation can be increased when Relugolix is combined with Sultopride.
Otilonium The risk or severity of QTc prolongation can be increased when Relugolix is combined with Otilonium.
Nizofenone The risk or severity of QTc prolongation can be increased when Relugolix is combined with Nizofenone.
Bunaftine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Bunaftine.
Lorcainide The risk or severity of QTc prolongation can be increased when Relugolix is combined with Lorcainide.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Relugolix is combined with Dexchlorpheniramine.
Penfluridol The risk or severity of QTc prolongation can be increased when Relugolix is combined with Penfluridol.
Dexverapamil The risk or severity of QTc prolongation can be increased when Relugolix is combined with Dexverapamil.
Berotralstat The metabolism of Relugolix can be decreased when combined with Berotralstat.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR

Referensi & Sumber

Synthesis reference: Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T: Discovery of 1-{4-1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl-3-(6-methoxypyridazin-3-yl )-2,4-dioxo-1,2,3,4-tetrahydrothieno2,3-dpyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23.
Artikel (PubMed)
  • PMID: 32912633
    Osuga Y, Seki Y, Tanimoto M, Kusumoto T, Kudou K, Terakawa N: Relugolix, an oral gonadotropin-releasing hormone receptor antagonist, reduces endometriosis-associated pain in a dose-response manner: a randomized, double-blind, placebo-controlled study. Fertil Steril. 2020 Sep 7. pii: S0015-0282(20)30716-0. doi: 10.1016/j.fertnstert.2020.07.055.
  • PMID: 21657270
    Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T: Discovery of 1-{4-1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl-3-(6-methoxypyridazin-3-yl )-2,4-dioxo-1,2,3,4-tetrahydrothieno2,3-dpyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23.
  • PMID: 31461087
    Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S: Relugolix for the treatment of uterine fibroids. Drugs Today (Barc). 2019 Aug;55(8):503-512. doi: 10.1358/dot.2019.55.8.3020179.
  • PMID: 26502357
    MacLean DB, Shi H, Faessel HM, Saad F: Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. doi: 10.1210/jc.2015-2770. Epub 2015 Oct 26.
  • PMID: 26622322
    Michaud JE, Billups KL, Partin AW: Testosterone and prostate cancer: an evidence-based review of pathogenesis and oncologic risk. Ther Adv Urol. 2015 Dec;7(6):378-87. doi: 10.1177/1756287215597633.
  • PMID: 30937733
    Markham A: Relugolix: First Global Approval. Drugs. 2019 Apr;79(6):675-679. doi: 10.1007/s40265-019-01105-0.
  • PMID: 30632129
    Kittai AS, Blank J, Graff JN: Gonadotropin-Releasing Hormone Antagonists in Prostate Cancer. Oncology (Williston Park). 2018 Dec 17;32(12):599-602, 604-6.
  • PMID: 32469183
    Shore ND, Saad F, Cookson MS, George DJ, Saltzstein DR, Tutrone R, Akaza H, Bossi A, van Veenhuyzen DF, Selby B, Fan X, Kang V, Walling J, Tombal B: Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer. N Engl J Med. 2020 Jun 4;382(23):2187-2196. doi: 10.1056/NEJMoa2004325. Epub 2020 May 29.

Contoh Produk & Brand

Produk: 10 • International brands: 2
Produk
  • Myfembree
    Tablet • - • Oral • Canada • Approved
  • Myfembree
    Tablet, film coated • - • Oral • US • Approved
  • Orgovyx
    Tablet • 120 mg • Oral • Canada • Approved
  • Orgovyx
    Tablet, film coated • 120 mg • Oral • EU • Approved
  • Orgovyx
    Tablet, film coated • 120 mg/1 • Oral • US • Approved
  • Orgovyx
    Tablet, film coated • 120 mg • Oral • EU • Approved
  • Ryeqo
    Tablet, film coated • - • Oral • EU • Approved
  • Ryeqo
    Tablet, film coated • - • Oral • EU • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Orgovyx
  • Relumina

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul