modelEnzalutamide
Extends from Pharmacolibrary.Drugs.ATC.L.L02BB04.
Information
| name: | Enzalutamide | |
| ATC code: | L02BB04 | route: | oral |
| compartments: | 2 | |
| dosage: | 160 | mg |
| volume of distribution: | 110 | L |
| clearance: | 0.56 | L/h |
| other parameters in model implementation | ||
Enzalutamide is a non-steroidal antiandrogen medication approved for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It acts by inhibiting the androgen receptor and is used as an oral therapy in advanced prostate cancer settings.
Pharmacokinetics
Population pharmacokinetic parameters reported for adult male patients with metastatic castration-resistant prostate cancer receiving oral enzalutamide 160 mg once daily.
References
Liu, YM, et al., & Chen, Q (2019). Pharmacokinetics and Safety of Enzalutamide in Healthy Chinese Male Volunteers. Clinical therapeutics 41(2) 261–268. DOI:10.1016/j.clinthera.2018.12.002 PUBMED:https://pubmed.ncbi.nlm.nih.gov/30642613
Lennep, BW, et al., & Morgans, AK (2024). Enzalutamide: Understanding and Managing Drug Interactions to Improve Patient Safety and Drug Efficacy. Drug safety 47(7) 617–641. DOI:10.1007/s40264-024-01415-7 PUBMED:https://pubmed.ncbi.nlm.nih.gov/38607520
George, DJ, et al., & Shore, ND (2023). Impact of Concomitant Prostate Cancer Medications on Efficacy and Safety of Relugolix Versus Leuprolide in Men With Advanced Prostate Cancer. Clinical genitourinary cancer 21(3) 383–392.e2. DOI:10.1016/j.clgc.2023.03.009 PUBMED:https://pubmed.ncbi.nlm.nih.gov/37062659
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)