Peringatan Keamanan

There are limited information on the LD50 values of roxadustat.

Single doses of roxadustat 5 mg/kg (up to 510 mg) in healthy subjects led to a transient increase in heart rate, an increased frequency of mild to moderate musculoskeletal pain, headaches, sinus tachycardia, and less commonly, low blood pressure. All these effects were non-serious in nature. Roxadustat overdose can elevate hemoglobin levels above the desired level (10 - 12 g/dL), which should be managed with discontinuation of roxadustat treatment or reduction of drug dosage with careful monitoring and appropriate supportive treatment. Roxadustat and its metabolites are not significantly removed by hemodialysis.L40318

Roxadustat

DB04847

small molecule approved investigational

Deskripsi

Roxadustat is a first-in-class hypoxia-inducible factor prolyl hydroxylase inhibitor used to treat anemia associated with chronic kidney disease. It works by reducing the breakdown of the hypoxia-inducible factor (HIF), which is a transcription factor that stimulates red blood cell production in response to low oxygen levels.A245393 Roxadustat was first approved by the European Commission in August 2021.L40323

Struktur Molekul 2D

Berat 352.346
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean effective half-life of roxadustat is approximately 15 hours in patients with CKD.[L40318]
Volume Distribusi The blood-to-plasma ratio of roxadustat is 0.6. The apparent volume of distribution at steady-state is 24 L.[L40318]
Klirens (Clearance) The apparent total body clearance (CL/F) of roxadustat is 1.1 L/h in patients with CKD not on dialysis and 1.4 L/h in patients with CKD on dialysis.[L40318]

Absorpsi

Roxadustat plasma exposure (AUC and Cmax) increases dose-proportionally within the recommended therapeutic dose range. In a three times per week dosing regimen, steady-state roxadustat plasma concentrations are achieved within one week (three doses) with minimal accumulation. Maximum plasma concentrations (Cmax) are usually achieved at two hours post dose in the fasted state. Administration of roxadustat with food decreased Cmax by 25% but did not alter AUC as compared with the fasted state.L40318

Metabolisme

In vitro, roxadustat is a substrate for CYP2C8 and UGT1A9 enzymes. Roxadustat is primarily metabolized to hydroxy-roxadustat and roxadustat O-glucuronide. Unchanged roxadustat was the major circulating component in human plasma and detectable metabolites in human plasma constituted less than 10% of total drug-related material exposure. No human-specific metabolites were observed L40318 but roxadustat O-glucuronide was detected in human urine sample.A245403

Rute Eliminasi

Following oral administration of radiolabelled roxadustat in healthy subjects, the mean recovery of radioactivity was 96% (50% in feces, 46% in urine). In feces, 28% of the dose was excreted as unchanged roxadustat. Less than 2% of the dose was recovered in urine as unchanged roxadustat.L40318

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food can decrease Cmax but not to a clinically significant extent.

Interaksi Obat

403 Data
Mifepristone The serum concentration of Roxadustat can be increased when it is combined with Mifepristone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Roxadustat.
Phenytoin The metabolism of Roxadustat can be decreased when combined with Phenytoin.
Secobarbital The metabolism of Roxadustat can be increased when combined with Secobarbital.
Rifampin The metabolism of Roxadustat can be decreased when combined with Rifampicin.
Troglitazone The metabolism of Roxadustat can be decreased when combined with Troglitazone.
Bexarotene The metabolism of Roxadustat can be decreased when combined with Bexarotene.
Diltiazem The metabolism of Roxadustat can be decreased when combined with Diltiazem.
Trimethoprim The metabolism of Roxadustat can be decreased when combined with Trimethoprim.
Levothyroxine The metabolism of Roxadustat can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Roxadustat can be decreased when combined with Loratadine.
Quinine The metabolism of Roxadustat can be decreased when combined with Quinine.
Ritonavir The metabolism of Roxadustat can be decreased when combined with Ritonavir.
Medroxyprogesterone acetate The metabolism of Roxadustat can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine The metabolism of Roxadustat can be decreased when combined with Nicardipine.
Efavirenz The metabolism of Roxadustat can be decreased when combined with Efavirenz.
Tamoxifen The serum concentration of Tamoxifen can be increased when it is combined with Roxadustat.
Ketoconazole The metabolism of Roxadustat can be decreased when combined with Ketoconazole.
Irbesartan The metabolism of Roxadustat can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Roxadustat can be decreased when combined with Oxybutynin.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Roxadustat.
Pioglitazone The metabolism of Roxadustat can be decreased when combined with Pioglitazone.
Saquinavir The metabolism of Roxadustat can be decreased when combined with Saquinavir.
Genistein The metabolism of Roxadustat can be decreased when combined with Genistein.
Topiroxostat The metabolism of Roxadustat can be decreased when combined with Topiroxostat.
Abiraterone The metabolism of Roxadustat can be decreased when combined with Abiraterone.
Eltrombopag The metabolism of Roxadustat can be decreased when combined with Eltrombopag.
Teriflunomide The serum concentration of Teriflunomide can be increased when it is combined with Roxadustat.
Enzalutamide The metabolism of Roxadustat can be decreased when combined with Enzalutamide.
Sorafenib The metabolism of Roxadustat can be decreased when combined with Sorafenib.
Erlotinib The metabolism of Roxadustat can be decreased when combined with Erlotinib.
Fluticasone propionate The metabolism of Roxadustat can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Roxadustat can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Roxadustat can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Roxadustat can be decreased when combined with Salmeterol.
Felodipine The metabolism of Roxadustat can be decreased when combined with Felodipine.
Gemfibrozil The metabolism of Roxadustat can be decreased when combined with Gemfibrozil.
Dabrafenib The metabolism of Roxadustat can be decreased when combined with Dabrafenib.
Fluticasone The metabolism of Roxadustat can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Roxadustat can be decreased when combined with Mometasone furoate.
Folic acid The serum concentration of Folic acid can be increased when it is combined with Roxadustat.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Roxadustat.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Roxadustat.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Roxadustat.
Allopurinol The serum concentration of Allopurinol can be increased when it is combined with Roxadustat.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Roxadustat.
Teniposide The serum concentration of Teniposide can be increased when it is combined with Roxadustat.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Roxadustat.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Roxadustat.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Roxadustat.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Roxadustat.
Oxaliplatin The serum concentration of Oxaliplatin can be increased when it is combined with Roxadustat.
Vincristine The serum concentration of Vincristine can be increased when it is combined with Roxadustat.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Roxadustat.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Roxadustat.
Ivermectin The serum concentration of Ivermectin can be increased when it is combined with Roxadustat.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Roxadustat.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Roxadustat.
Clofarabine The serum concentration of Clofarabine can be increased when it is combined with Roxadustat.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Roxadustat.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Roxadustat.
Daunorubicin The serum concentration of Daunorubicin can be increased when it is combined with Roxadustat.
Nitrofurantoin The serum concentration of Nitrofurantoin can be increased when it is combined with Roxadustat.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Roxadustat.
Riluzole The serum concentration of Riluzole can be increased when it is combined with Roxadustat.
Irinotecan The serum concentration of Irinotecan can be increased when it is combined with Roxadustat.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Roxadustat.
Sulfasalazine The serum concentration of Sulfasalazine can be increased when it is combined with Roxadustat.
Donepezil The serum concentration of Donepezil can be increased when it is combined with Roxadustat.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Roxadustat.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Roxadustat.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Roxadustat.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Roxadustat.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Roxadustat.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Roxadustat.
Leflunomide The serum concentration of Leflunomide can be increased when it is combined with Roxadustat.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Roxadustat.
Mitoxantrone The serum concentration of Mitoxantrone can be increased when it is combined with Roxadustat.
Dasatinib The serum concentration of Dasatinib can be increased when it is combined with Roxadustat.
Alvocidib The serum concentration of Alvocidib can be increased when it is combined with Roxadustat.
Camptothecin The serum concentration of Camptothecin can be increased when it is combined with Roxadustat.
Nilotinib The serum concentration of Nilotinib can be increased when it is combined with Roxadustat.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Roxadustat.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Roxadustat.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Roxadustat.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Roxadustat.
Pralatrexate The serum concentration of Pralatrexate can be increased when it is combined with Roxadustat.
Vemurafenib The serum concentration of Vemurafenib can be increased when it is combined with Roxadustat.
Ponatinib The serum concentration of Ponatinib can be increased when it is combined with Roxadustat.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Roxadustat.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Roxadustat.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Roxadustat.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Roxadustat.
Idelalisib The serum concentration of Idelalisib can be increased when it is combined with Roxadustat.
Palbociclib The serum concentration of Palbociclib can be increased when it is combined with Roxadustat.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Roxadustat.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Roxadustat.
Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Roxadustat.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Roxadustat.
Osimertinib The serum concentration of Osimertinib can be increased when it is combined with Roxadustat.

Target Protein

Egl nine homolog 1 EGLN1
Prolyl hydroxylase EGLN2 EGLN2
Prolyl hydroxylase EGLN3 EGLN3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30805897
    Dhillon S: Roxadustat: First Global Approval. Drugs. 2019 Apr;79(5):563-572. doi: 10.1007/s40265-019-01077-1.
  • PMID: 34077510
    Barratt J, Andric B, Tataradze A, Schomig M, Reusch M, Valluri U, Mariat C: Roxadustat for the treatment of anaemia in chronic kidney disease patients not on dialysis: a Phase 3, randomized, open-label, active-controlled study (DOLOMITES). Nephrol Dial Transplant. 2021 Aug 27;36(9):1616-1628. doi: 10.1093/ndt/gfab191.
  • PMID: 18160990
    Ziello JE, Jovin IS, Huang Y: Hypoxia-Inducible Factor (HIF)-1 regulatory pathway and its potential for therapeutic intervention in malignancy and ischemia. Yale J Biol Med. 2007 Jun;80(2):51-60.
  • PMID: 27918992
    Hansson A, Thevis M, Cox H, Miller G, Eichner D, Bondesson U, Hedeland M: Investigation of the metabolites of the HIF stabilizer FG-4592 (roxadustat) in five different in vitro models and in a human doping control sample using high resolution mass spectrometry. J Pharm Biomed Anal. 2017 Feb 5;134:228-236. doi: 10.1016/j.jpba.2016.11.041. Epub 2016 Nov 27.

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Sekuens Gen/Protein (FASTA)

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