modelJ05AP02
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | Telaprevir | |
| ATC code: | J05AP02 | route: | oral |
| compartments: | 2 | |
| dosage: | 750 | mg |
| volume of distribution: | 252 | L |
| clearance: | 22.8 | L/h |
| other parameters in model implementation | ||
Telaprevir is an oral antiviral drug that acts as a protease inhibitor, specifically inhibiting the NS3/4A protease of hepatitis C virus (HCV). It was used in combination with other agents for the treatment of chronic hepatitis C infection, genotype 1. While it was previously approved, telaprevir has been withdrawn from the market in many countries due to adverse effects and the development of more effective agents.
Pharmacokinetics
Pharmacokinetic model in adult healthy subjects and patients with chronic hepatitis C. Oral administration under fed conditions.
References
Kiang, TK, et al., & Ensom, MH (2013). Telaprevir: clinical pharmacokinetics, pharmacodynamics, and drug-drug interactions. Clinical pharmacokinetics 52(7) 487–510. DOI:10.1007/s40262-013-0053-x PUBMED:https://pubmed.ncbi.nlm.nih.gov/23553423
Gentile, I, et al., & Borgia, G (2014). Dasabuvir: A Non-Nucleoside Inhibitor of NS5B for the Treatment of Hepatitis C Virus Infection. Reviews on recent clinical trials 9(2) 115–123. DOI:10.2174/1574887109666140529222602 PUBMED:https://pubmed.ncbi.nlm.nih.gov/24882169
Klibanov, OM, et al., & Vickery, SB (2011). Telaprevir: a novel NS3/4 protease inhibitor for the treatment of hepatitis C. Pharmacotherapy 31(10) 951–974. DOI:10.1592/phco.31.10.951 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21950642
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)