Peringatan Keamanan

There is no information regarding the acute toxicity and overdosage of resmetirom.

Resmetirom

DB12914

small molecule approved investigational

Deskripsi

Resmetirom is a thyroid hormone receptor-beta (THR-beta) agonist. On March 14, 2024, it was approved by the FDA as the first treatment of liver fibrosis due to noncirrhotic non-alcoholic steatohepatitis (NASH), which is a form of non-alcoholic fatty liver disease (NAFLD).L50336

Thyroid hormones directly regulate lipid metabolism in the liver; thus, impaired thyroid function, such as low serum thyroid hormone levels, is often observed in NAFLD.A263461 Resmetirom works to reduce liver fat by stimulating fatty acid degradation and oxidation.L50336

Struktur Molekul 2D

Berat 435.22
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median terminal plasma half-life is 4.5 hours.[L50331]
Volume Distribusi Resmetirom apparent volume of distribution (Vd/F) at steady-state is 68 (227%) L.[L50331]
Klirens (Clearance) The steady state apparent clearance (CL/F) is 17.5 (56.3%) L/h.[L50331]

Absorpsi

The median Tmax is approximately four hours following multiple daily doses of resmetirom 80 mg or 100 mg.L50331 Concomitant food administration resulted in a 33% decrease in Cmax, an 11% decrease in AUC, and a delay in median Tmax by about two hours compared to an under-fasted condition.L50331

Metabolisme

Resmetirom is metabolized by CYP2C8. MGL-3623 is a major metabolite with a 28-times lower potency for THR-? than resmetirom. MGL-3623 represents 33% to 51% of resmetirom AUC at steady-state following administration of 100 mg once daily.L50331

Rute Eliminasi

Following oral administration of a 100 mg radio-labeled dose of resmetirom, approximately 67% of the total radioactive dose was recovered in the feces, mostly as metabolites and 24% of the total radioactive dose was recovered in the urine. Unchanged labeled resmetirom was not detected in feces and accounted for 1% of the dose recovered in urine. A metabolite MGL-3623 accounted for 3.3% and 16% of the dose recovered in feces and urine, respectively. Oxalic acid metabolite was observed in plasma but not in urine.L50331

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high fat meal may reduce Cmax and AUC delay Tmax, but not to a clinically significant extent.

Interaksi Obat

315 Data
Mifepristone The serum concentration of Resmetirom can be increased when it is combined with Mifepristone.
Phenytoin The metabolism of Phenytoin can be decreased when combined with Resmetirom.
Secobarbital The metabolism of Resmetirom can be increased when combined with Secobarbital.
Rifampin The metabolism of Resmetirom can be increased when combined with Rifampin.
Troglitazone The serum concentration of Resmetirom can be increased when it is combined with Troglitazone.
Bexarotene The metabolism of Resmetirom can be decreased when combined with Bexarotene.
Diltiazem The metabolism of Resmetirom can be decreased when combined with Diltiazem.
Trimethoprim The metabolism of Resmetirom can be decreased when combined with Trimethoprim.
Levothyroxine The metabolism of Resmetirom can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Resmetirom can be decreased when combined with Loratadine.
Quinine The serum concentration of Resmetirom can be increased when it is combined with Quinine.
Ritonavir The metabolism of Resmetirom can be decreased when combined with Ritonavir.
Medroxyprogesterone acetate The metabolism of Resmetirom can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine The serum concentration of Resmetirom can be increased when it is combined with Nicardipine.
Efavirenz The metabolism of Resmetirom can be decreased when combined with Efavirenz.
Tamoxifen The metabolism of Resmetirom can be decreased when combined with Tamoxifen.
Ketoconazole The serum concentration of Resmetirom can be increased when it is combined with Ketoconazole.
Irbesartan The metabolism of Resmetirom can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Resmetirom can be decreased when combined with Oxybutynin.
Fluvastatin The serum concentration of Resmetirom can be increased when it is combined with Fluvastatin.
Pioglitazone The metabolism of Resmetirom can be decreased when combined with Pioglitazone.
Saquinavir The serum concentration of Resmetirom can be increased when it is combined with Saquinavir.
Genistein The serum concentration of Resmetirom can be increased when it is combined with Genistein.
Topiroxostat The metabolism of Resmetirom can be decreased when combined with Topiroxostat.
Abiraterone The metabolism of Resmetirom can be decreased when combined with Abiraterone.
Eltrombopag The serum concentration of Resmetirom can be increased when it is combined with Eltrombopag.
Teriflunomide The serum concentration of Resmetirom can be increased when it is combined with Teriflunomide.
Enzalutamide The metabolism of Resmetirom can be decreased when combined with Enzalutamide.
Pirtobrutinib The metabolism of Resmetirom can be decreased when combined with Pirtobrutinib.
Erlotinib The metabolism of Resmetirom can be decreased when combined with Erlotinib.
Fluticasone propionate The metabolism of Resmetirom can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Resmetirom can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Resmetirom can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Resmetirom can be decreased when combined with Salmeterol.
Felodipine The metabolism of Resmetirom can be decreased when combined with Felodipine.
Gemfibrozil The metabolism of Resmetirom can be decreased when combined with Gemfibrozil.
Dabrafenib The metabolism of Resmetirom can be decreased when combined with Dabrafenib.
Fluticasone The metabolism of Resmetirom can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Resmetirom can be decreased when combined with Mometasone furoate.
Cholic Acid The serum concentration of Resmetirom can be increased when it is combined with Cholic Acid.
Taurocholic acid The serum concentration of Resmetirom can be increased when it is combined with Taurocholic acid.
Apalutamide The serum concentration of Resmetirom can be decreased when it is combined with Apalutamide.
Cyclosporine The serum concentration of Resmetirom can be increased when it is combined with Cyclosporine.
Valsartan The serum concentration of Resmetirom can be increased when it is combined with Valsartan.
Erythromycin The serum concentration of Resmetirom can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Resmetirom can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Resmetirom can be increased when it is combined with Reserpine.
Pantoprazole The serum concentration of Resmetirom can be increased when it is combined with Pantoprazole.
Nelfinavir The serum concentration of Resmetirom can be increased when it is combined with Nelfinavir.
Indinavir The serum concentration of Resmetirom can be increased when it is combined with Indinavir.
Diethylstilbestrol The serum concentration of Resmetirom can be increased when it is combined with Diethylstilbestrol.
Conjugated estrogens The serum concentration of Resmetirom can be increased when it is combined with Conjugated estrogens.
Indomethacin The serum concentration of Resmetirom can be increased when it is combined with Indomethacin.
Digoxin The serum concentration of Resmetirom can be increased when it is combined with Digoxin.
Beclomethasone dipropionate The serum concentration of Resmetirom can be increased when it is combined with Beclomethasone dipropionate.
Progesterone The serum concentration of Resmetirom can be increased when it is combined with Progesterone.
Rosiglitazone The serum concentration of Resmetirom can be increased when it is combined with Rosiglitazone.
Cerivastatin The serum concentration of Resmetirom can be increased when it is combined with Cerivastatin.
Caspofungin The serum concentration of Resmetirom can be increased when it is combined with Caspofungin.
Vincristine The serum concentration of Resmetirom can be increased when it is combined with Vincristine.
Vinblastine The serum concentration of Resmetirom can be increased when it is combined with Vinblastine.
Levocarnitine The serum concentration of Resmetirom can be increased when it is combined with Levocarnitine.
Diclofenac The serum concentration of Resmetirom can be increased when it is combined with Diclofenac.
Ivermectin The serum concentration of Resmetirom can be increased when it is combined with Ivermectin.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Resmetirom.
Nystatin The serum concentration of Resmetirom can be increased when it is combined with Nystatin.
Amprenavir The serum concentration of Resmetirom can be increased when it is combined with Amprenavir.
Irinotecan The serum concentration of Resmetirom can be increased when it is combined with Irinotecan.
Roxithromycin The serum concentration of Resmetirom can be increased when it is combined with Roxithromycin.
Estradiol The serum concentration of Resmetirom can be increased when it is combined with Estradiol.
Sulfasalazine The serum concentration of Resmetirom can be increased when it is combined with Sulfasalazine.
Tacrolimus The serum concentration of Resmetirom can be increased when it is combined with Tacrolimus.
Sirolimus The serum concentration of Resmetirom can be increased when it is combined with Sirolimus.
Quinidine The serum concentration of Resmetirom can be increased when it is combined with Quinidine.
Tipranavir The serum concentration of Resmetirom can be increased when it is combined with Tipranavir.
Dipyridamole The serum concentration of Resmetirom can be increased when it is combined with Dipyridamole.
Telithromycin The serum concentration of Resmetirom can be increased when it is combined with Telithromycin.
Novobiocin The serum concentration of Resmetirom can be increased when it is combined with Novobiocin.
Atazanavir The serum concentration of Resmetirom can be increased when it is combined with Atazanavir.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Resmetirom.
Ouabain The serum concentration of Resmetirom can be increased when it is combined with Ouabain.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Resmetirom.
Clarithromycin The serum concentration of Resmetirom can be increased when it is combined with Clarithromycin.
Darunavir The serum concentration of Resmetirom can be increased when it is combined with Darunavir.
Bezafibrate The serum concentration of Resmetirom can be increased when it is combined with Bezafibrate.
Everolimus The serum concentration of Resmetirom can be increased when it is combined with Everolimus.
Lopinavir The serum concentration of Resmetirom can be increased when it is combined with Lopinavir.
Hyperforin The serum concentration of Resmetirom can be increased when it is combined with Hyperforin.
Fusidic acid The serum concentration of Resmetirom can be increased when it is combined with Fusidic acid.
Quercetin The serum concentration of Resmetirom can be increased when it is combined with Quercetin.
Roxadustat The serum concentration of Resmetirom can be increased when it is combined with Roxadustat.
Posizolid The serum concentration of Resmetirom can be increased when it is combined with Posizolid.
Dronedarone The serum concentration of Resmetirom can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Resmetirom can be increased when it is combined with Nilotinib.
Telaprevir The serum concentration of Resmetirom can be increased when it is combined with Telaprevir.
Dovitinib The serum concentration of Resmetirom can be increased when it is combined with Dovitinib.
Trofinetide The serum concentration of Resmetirom can be increased when it is combined with Trofinetide.
Acetylcysteine The serum concentration of Resmetirom can be increased when it is combined with Acetylcysteine.
Simeprevir The serum concentration of Resmetirom can be increased when it is combined with Simeprevir.
Pazopanib The serum concentration of Resmetirom can be increased when it is combined with Pazopanib.

Target Protein

Thyroid hormone receptor beta THRB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 36171155
    Hatziagelaki E, Paschou SA, Schon M, Psaltopoulou T, Roden M: NAFLD and thyroid function: pathophysiological and therapeutic considerations. Trends Endocrinol Metab. 2022 Nov;33(11):755-768. doi: 10.1016/j.tem.2022.08.001. Epub 2022 Sep 26.
  • PMID: 36746649
    Li L, Song Y, Shi Y, Sun L: Thyroid Hormone Receptor-beta Agonists in NAFLD Therapy: Possibilities and Challenges. J Clin Endocrinol Metab. 2023 Jun 16;108(7):1602-1613. doi: 10.1210/clinem/dgad072.
  • PMID: 37313239
    Karim G, Bansal MB: Resmetirom: An Orally Administered, Smallmolecule, Liver-directed, beta-selective THR Agonist for the Treatment of Non-alcoholic Fatty Liver Disease and Non-alcoholic Steatohepatitis. touchREV Endocrinol. 2023 May;19(1):60-70. doi: 10.17925/EE.2023.19.1.60. Epub 2023 May 1.
  • PMID: 31727409
    Harrison SA, Bashir MR, Guy CD, Zhou R, Moylan CA, Frias JP, Alkhouri N, Bansal MB, Baum S, Neuschwander-Tetri BA, Taub R, Moussa SE: Resmetirom (MGL-3196) for the treatment of non-alcoholic steatohepatitis: a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial. Lancet. 2019 Nov 30;394(10213):2012-2024. doi: 10.1016/S0140-6736(19)32517-6. Epub 2019 Nov 11.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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