modelJ05AX29
Extends from Pharmacokinetic.Models.PK_2C_enteral.
Information
| name: | Fostemsavir | |
| ATC code: | J05AX29 | route: | oral |
| compartments: | 2 | |
| dosage: | 600 | mg |
| volume of distribution: | 189 | L |
| clearance: | 17.9 | L/h |
| other parameters in model implementation | ||
Fostemsavir is an antiretroviral medication used for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection for whom an otherwise suppressive antiretroviral regimen is not available. It is a prodrug of temsavir, which acts as an attachment inhibitor binding to gp120 on HIV-1, preventing virus attachment and entry into host CD4+ cells. Fostemsavir is FDA- and EMA-approved.
Pharmacokinetics
Population pharmacokinetics of temsavir (the active moiety of fostemsavir) in HIV-1-infected adults, following oral administration of fostemsavir 600 mg twice daily.
References
Magee, M, et al., & Moore, K (2021). Effect of Renal and Hepatic Impairment on the Pharmacokinetics of Temsavir, the Active Moiety of Fostemsavir. Journal of clinical pharmacology 61(7) 939–953. DOI:10.1002/jcph.1810 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33368327
Beran, C, et al., & Sahloff, EG (2024). A Narrative Review of Novel Agents for Managing Heavily Treatment-Experienced People Living With HIV. The Journal of pharmacy technology : jPT : official publication of the Association of Pharmacy Technicians 40(4) 194–201. DOI:10.1177/87551225241259894 PUBMED:https://pubmed.ncbi.nlm.nih.gov/39157636
Landry, I, et al., & Bertz, RJ (2016). Model-Based Phase 3 Dose Selection for HIV-1 Attachment Inhibitor Prodrug BMS-663068 in HIV-1-Infected Patients: Population Pharmacokinetics/Pharmacodynamics of the Active Moiety, BMS-626529. Antimicrobial agents and chemotherapy 60(5) 2782–2789. DOI:10.1128/AAC.02503-15 PUBMED:https://pubmed.ncbi.nlm.nih.gov/26902761
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)