Peringatan Keamanan

No data regarding overdosage with linzagolix are available. In the event of a suspected overdose, patients should be monitored closely. Institute symptomatic and supportive measures as clinically indicated.

Linzagolix

DB17083

small molecule approved

Deskripsi

Linzagolix is a non-peptide, selective antagonist of the gonadotropin-releasing hormone (GnRH) receptor. It has been studied for the treatment of estrogen-dependent conditions such as uterine fibroids and endometriosis.A253642,A253647 It is similar to other GnRH receptor antagonists like cetrorelix, relugolix, and elagolix.

Uterine fibroids occur in >70% of women of reproductive age, and when symptomatic are associated with heavy menstrual bleeding, anemia, abdominal pain and pressure, bloating, increased urinary frequency, and reproductive dysfunction.A253662 As these fibroids are essentially estrogen-dependent phenomena, hormone therapies which suppress estrogen activity - including GnRH receptor antagonists like linzagolix - are thought to be beneficial by preventing intramyometrial growths in the endometrial glands.A253667

Linzagolix was approved for use in the European Union in June 2022 for the management of symptoms caused by uterine fibroids.L43627

Struktur Molekul 2D

Berat 508.42
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of linzagolix following multiple doses is approximately 15 hours.[L43627]
Volume Distribusi After seven days of oral administration of linzagolix 100mg or 200mg, the volume of distribution was 11.067 L and 11.178 L, respectively.[L43627]
Klirens (Clearance) The geometric mean apparent clearance following multiple oral doses of linzagolix 100mg or 200mg was 0.522 L/h and 0.499 L/h, respectively.[L43627]

Absorpsi

Linzagolix is quickly absorbed following oral administration, with Cmax occurring approximately 2 hours following administration.L43627

Metabolisme

Up to seven metabolites of linzagolix have been quantified in patient plasma, urine, and feces, although plasma metabolites represent less than 10% of the total linzagolix-related exposure.L43627 Two primary demethylated metabolites - KP017 and KP046 - have been identified, with CYP2C9 primarily responsible for the formation of KP017 and CYP2C8, CYP2C9, and CYP3A4 are primarily responsible for the formation of KP046.L43637 Unchanged parent drug is the predominant circulating component in human plasma and in the urine, and one of the major components in the feces.L43627

Rute Eliminasi

Linzagolix is primarily excreted in the urine, with approximately one-third eliminated via the feces.L43627

Interaksi Makanan

1 Data
  • 1. Take with or without food. The co-administration of linzagolix with food does not effect its pharmacokinetics to a clinically significant extent.

Interaksi Obat

129 Data
Troglitazone The serum concentration of Troglitazone can be increased when it is combined with Linzagolix.
Torasemide The serum concentration of Torasemide can be increased when it is combined with Linzagolix.
Dapsone The serum concentration of Dapsone can be increased when it is combined with Linzagolix.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Linzagolix.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Linzagolix.
Theophylline The serum concentration of Theophylline can be increased when it is combined with Linzagolix.
Morphine The serum concentration of Morphine can be increased when it is combined with Linzagolix.
Amitriptyline The serum concentration of Amitriptyline can be increased when it is combined with Linzagolix.
Diltiazem The serum concentration of Diltiazem can be increased when it is combined with Linzagolix.
Trimethadione The serum concentration of Trimethadione can be increased when it is combined with Linzagolix.
Sulfadiazine The serum concentration of Sulfadiazine can be increased when it is combined with Linzagolix.
Treprostinil The serum concentration of Treprostinil can be increased when it is combined with Linzagolix.
Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Linzagolix.
Eszopiclone The serum concentration of Eszopiclone can be increased when it is combined with Linzagolix.
Rosiglitazone The serum concentration of Rosiglitazone can be increased when it is combined with Linzagolix.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Linzagolix.
Lansoprazole The serum concentration of Lansoprazole can be increased when it is combined with Linzagolix.
Ketorolac The serum concentration of Ketorolac can be increased when it is combined with Linzagolix.
Quinine The serum concentration of Quinine can be increased when it is combined with Linzagolix.
Montelukast The serum concentration of Montelukast can be increased when it is combined with Linzagolix.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Linzagolix.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Linzagolix.
Erlotinib The serum concentration of Erlotinib can be increased when it is combined with Linzagolix.
Cyclophosphamide The serum concentration of Cyclophosphamide can be increased when it is combined with Linzagolix.
Mephenytoin The serum concentration of Mephenytoin can be increased when it is combined with Linzagolix.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Linzagolix.
Piroxicam The serum concentration of Piroxicam can be increased when it is combined with Linzagolix.
Diclofenac The serum concentration of Diclofenac can be increased when it is combined with Linzagolix.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Linzagolix.
Chloroquine The serum concentration of Chloroquine can be increased when it is combined with Linzagolix.
Amodiaquine The serum concentration of Amodiaquine can be increased when it is combined with Linzagolix.
Paramethadione The serum concentration of Paramethadione can be increased when it is combined with Linzagolix.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Linzagolix.
Nicardipine The serum concentration of Nicardipine can be increased when it is combined with Linzagolix.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Linzagolix.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Linzagolix.
Apomorphine The serum concentration of Apomorphine can be increased when it is combined with Linzagolix.
Estradiol The serum concentration of Estradiol can be increased when it is combined with Linzagolix.
Naproxen The serum concentration of Naproxen can be increased when it is combined with Linzagolix.
Tazarotene The serum concentration of Tazarotene can be increased when it is combined with Linzagolix.
Propofol The serum concentration of Propofol can be increased when it is combined with Linzagolix.
Loperamide The serum concentration of Loperamide can be increased when it is combined with Linzagolix.
Terbinafine The serum concentration of Terbinafine can be increased when it is combined with Linzagolix.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Linzagolix.
Almotriptan The serum concentration of Almotriptan can be increased when it is combined with Linzagolix.
Buprenorphine The serum concentration of Buprenorphine can be increased when it is combined with Linzagolix.
Phenprocoumon The serum concentration of Phenprocoumon can be increased when it is combined with Linzagolix.
Azelastine The serum concentration of Azelastine can be increased when it is combined with Linzagolix.
Ethinylestradiol The serum concentration of Ethinylestradiol can be increased when it is combined with Linzagolix.
Irbesartan The serum concentration of Irbesartan can be increased when it is combined with Linzagolix.
Selegiline The serum concentration of Selegiline can be increased when it is combined with Linzagolix.
Ibuprofen The serum concentration of Ibuprofen can be increased when it is combined with Linzagolix.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Linzagolix.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Linzagolix.
Amiodarone The serum concentration of Amiodarone can be increased when it is combined with Linzagolix.
Tolbutamide The serum concentration of Tolbutamide can be increased when it is combined with Linzagolix.
Pioglitazone The serum concentration of Pioglitazone can be increased when it is combined with Linzagolix.
Ifosfamide The serum concentration of Ifosfamide can be increased when it is combined with Linzagolix.
Domperidone The serum concentration of Domperidone can be increased when it is combined with Linzagolix.
Zopiclone The serum concentration of Zopiclone can be increased when it is combined with Linzagolix.
Anastrozole The serum concentration of Anastrozole can be increased when it is combined with Linzagolix.
Halofantrine The serum concentration of Halofantrine can be increased when it is combined with Linzagolix.
Ketamine The serum concentration of Ketamine can be increased when it is combined with Linzagolix.
Paclitaxel The serum concentration of Paclitaxel can be increased when it is combined with Linzagolix.
Lapatinib The serum concentration of Lapatinib can be increased when it is combined with Linzagolix.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Linzagolix.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Linzagolix.
Mestranol The serum concentration of Mestranol can be increased when it is combined with Linzagolix.
Aminophenazone The serum concentration of Aminophenazone can be increased when it is combined with Linzagolix.
Antipyrine The serum concentration of Antipyrine can be increased when it is combined with Linzagolix.
Hydroxychloroquine The serum concentration of Hydroxychloroquine can be increased when it is combined with Linzagolix.
Licofelone The serum concentration of Licofelone can be increased when it is combined with Linzagolix.
Roxadustat The serum concentration of Roxadustat can be increased when it is combined with Linzagolix.
Beraprost The serum concentration of Beraprost can be increased when it is combined with Linzagolix.
Eltrombopag The serum concentration of Eltrombopag can be increased when it is combined with Linzagolix.
Muraglitazar The serum concentration of Muraglitazar can be increased when it is combined with Linzagolix.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Linzagolix.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Linzagolix.
Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Linzagolix.
Ketobemidone The serum concentration of Ketobemidone can be increased when it is combined with Linzagolix.
Seratrodast The serum concentration of Seratrodast can be increased when it is combined with Linzagolix.
Benzyl alcohol The serum concentration of Benzyl alcohol can be increased when it is combined with Linzagolix.
Cabazitaxel The serum concentration of Cabazitaxel can be increased when it is combined with Linzagolix.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Linzagolix.
Capravirine The serum concentration of Capravirine can be increased when it is combined with Linzagolix.
Enzalutamide The serum concentration of Enzalutamide can be increased when it is combined with Linzagolix.
Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Linzagolix.
Dabrafenib The serum concentration of Dabrafenib can be increased when it is combined with Linzagolix.
Perospirone The serum concentration of Perospirone can be increased when it is combined with Linzagolix.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Linzagolix.
Vortioxetine The serum concentration of Vortioxetine can be increased when it is combined with Linzagolix.
Olodaterol The serum concentration of Olodaterol can be increased when it is combined with Linzagolix.
Dasabuvir The serum concentration of Dasabuvir can be increased when it is combined with Linzagolix.
Lobeglitazone The serum concentration of Lobeglitazone can be increased when it is combined with Linzagolix.
Netoglitazone The serum concentration of Netoglitazone can be increased when it is combined with Linzagolix.
Rivoglitazone The serum concentration of Rivoglitazone can be increased when it is combined with Linzagolix.
Ciglitazone The serum concentration of Ciglitazone can be increased when it is combined with Linzagolix.
Dexibuprofen The serum concentration of Dexibuprofen can be increased when it is combined with Linzagolix.
Tegafur The serum concentration of Tegafur can be increased when it is combined with Linzagolix.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Linzagolix.

Target Protein

Gonadotropin-releasing hormone receptor GNRHR

Referensi & Sumber

Synthesis reference: Ohno, K., Miyagi, T., Ozawa, T., & Fushimi, N. (2007, April 26). Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof . WO2007046392A1.
Artikel (PubMed)
  • PMID: 32505383
    Donnez J, Taylor HS, Taylor RN, Akin MD, Tatarchuk TF, Wilk K, Gotteland JP, Lecomte V, Bestel E: Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone-antagonist: a randomized clinical trial. Fertil Steril. 2020 Jul;114(1):44-55. doi: 10.1016/j.fertnstert.2020.02.114. Epub 2020 Jun 4.
  • PMID: 34278887
    Dababou S, Garzon S, Lagana AS, Ferrero S, Evangelisti G, Noventa M, D'Alterio MN, Palomba S, Uccella S, Franchi M, Barra F: Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas. Expert Opin Investig Drugs. 2021 Sep;30(9):903-911. doi: 10.1080/13543784.2021.1957830. Epub 2021 Aug 4.
  • PMID: 34945090
    Donnez J, Donnez O, Tourniaire J, Brethous M, Bestel E, Garner E, Charpentier S, Humberstone A, Loumaye E: Uterine Adenomyosis Treated by Linzagolix, an Oral Gonadotropin-Releasing Hormone Receptor Antagonist: A Pilot Study with a New 'Hit Hard First and then Maintain' Regimen of Administration. J Clin Med. 2021 Dec 10;10(24). pii: jcm10245794. doi: 10.3390/jcm10245794.
  • PMID: 35690889
    Tezuka M, Tamai Y, Kuramochi Y, Kobayashi K, Fushimi N, Kiguchi S: Pharmacological characterization of linzagolix, a novel, orally active, non-peptide antagonist of gonadotropin-releasing hormone receptors. Clin Exp Pharmacol Physiol. 2022 Oct;49(10):1082-1093. doi: 10.1111/1440-1681.13688. Epub 2022 Jul 12.
  • PMID: 35997940
    Keam SJ: Linzagolix: First Approval. Drugs. 2022 Aug;82(12):1317-1325. doi: 10.1007/s40265-022-01753-9.
  • PMID: 34639243
    Donnez J, Stratopoulou CA, Dolmans MM: Uterine Adenomyosis: From Disease Pathogenesis to a New Medical Approach Using GnRH Antagonists. Int J Environ Res Public Health. 2021 Sep 22;18(19). pii: ijerph18199941. doi: 10.3390/ijerph18199941.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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