modelB03XA05
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | Roxadustat | |
| ATC code: | B03XA05 | route: | oral |
| compartments: | 2 | |
| dosage: | 100 | mg |
| volume of distribution: | 22.1 | L |
| clearance: | 1.23 | L/h |
| other parameters in model implementation | ||
Roxadustat is an orally administered hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) used primarily for the treatment of anemia associated with chronic kidney disease (CKD). The drug stimulates endogenous erythropoietin production and improves iron metabolism. Roxadustat is approved for clinical use in several countries including China, Japan, and the European Union, but not the United States.
Pharmacokinetics
Pharmacokinetics parameters in healthy adult volunteers and CKD patients; population: mixed males and females aged 18-75.
References
Rekić, D, et al., & Hamrén, B (2021). Pharmacokinetics of Roxadustat: A Population Analysis of 2855 Dialysis- and Non-Dialysis-Dependent Patients with Chronic Kidney Disease. Clinical pharmacokinetics 60(6) 759–773. DOI:10.1007/s40262-020-00974-z PUBMED:https://pubmed.ncbi.nlm.nih.gov/33486718
Shen, ZW, et al., & Lou, Y (2024). Optimizing the dosing regimen of roxadustat in kidney transplant recipients with early post-transplant anemia. Journal of pharmaceutical sciences 113(11) 3344–3353. DOI:10.1016/j.xphs.2024.09.004 PUBMED:https://pubmed.ncbi.nlm.nih.gov/39251067
Alvarez, JC, et al., & Larabi, IA (2024). Hair and dietary supplements testing to identify contamination with roxadustat in an adverse analytical finding. Journal of pharmaceutical and biomedical analysis 239 115915–None. DOI:10.1016/j.jpba.2023.115915 PUBMED:https://pubmed.ncbi.nlm.nih.gov/38091820
Parameters
| Type | Name | Default | Description |
|---|---|---|---|
| Modelica.Units.SI.Mass | weight (from PK_1C) | 75 | patient weight (kg) |
| Modelica.Units.SI.SpecificVolume | VdPerKg (from PK_1C) | 0.9 | Volume of distribution (L/kg) |
| Modelica.Units.SI.MassFraction | F (from PK_1C) | 0.8 | bioavailiability (0-1) |
| Pharmacolibrary.Types.Clearance | Cl (from PK_1C) | 20 | clearance |
| Modelica.Units.SI.Time | adminTime (from PK_1C) | 60 | first administration time (s) |
| Modelica.Units.SI.Time | adminDuration (from PK_1C) | 600 | administration duration (s) |
| Modelica.Units.SI.Time | adminPeriod (from PK_1C) | 8*60*60 | period of administration (default 8 hours)(s) |
| Pharmacolibrary.Types.Mass | adminMass (from PK_1C) | 1000 | administration mass (mg) |
| Integer | adminCount (from PK_1C) | 8 | number of dose administered (1) |
| Pharmacolibrary.Types.Volume | Vd (from PK_1C) | VdPerKg*weight | Volume of distribution (m3) |
| Pharmacolibrary.Types.MassConcentration | Cmin (from PK_1C) | 0.004 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Cmax (from PK_1C) | 0.008 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Ctox_peak (from PK_1C) | 0.012 | toxicity peak level |
| Pharmacolibrary.Types.MassConcentration | Ctox_trough (from PK_1C) | 0.006 | toxicity trough level |
| Pharmacolibrary.Types.Volume | Vdp (from PK_2C) | VdpPerKg*weight | Volume of distribution (m3) |
| Modelica.Units.SI.SpecificVolume | VdpPerKg (from PK_2C) | 0.9 | Volume of distribution peripheral(l/kg) |
| Pharmacolibrary.Types.Clearance | k12 (from PK_2C) | 1 | intercompartmental C-P clearance |
| Pharmacolibrary.Types.Clearance | k21 (from PK_2C) | 1 | intercompartmental P-C clearance |
| Pharmacolibrary.Types.TransferRate | ka (from PK_2C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_2C_enteral) | 600 | delay between oral administration and absorption (default 10min) |
Connectors
| Type | Name | Default | Description |
|---|---|---|---|
| Types.ConcentrationOutput | C_central (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | centralCPort (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | peripheralCPort (from PK_2C) | ||
| Pharmacolibrary.Types.ConcentrationOutput | C_peripheral1 (from PK_2C) |
Components
| Type | Name | Default | Description |
|---|---|---|---|
| Pharmacokinetic.NoPerfusedTissueCompartment | central (from PK_1C) | ||
| Pharmacokinetic.ClearanceDrivenElimination | elim (from PK_1C) | ||
| Sources.PeriodicDose | periodicDose (from PK_1C) | ||
| Modelica.Units.SI.Time | t1_2 (from PK_1C) | elimination half-life | |
| Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSym | transfer (from PK_2C) | ||
| Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartment | peripheral (from PK_2C) |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)