modelJ05AR09

Diagram of J05AR09

Extends from Pharmacokinetic.Models.PK_1C_enteral.

Information

name:EmtricitabineTenofovirDisoproxilElvitegravirAndCobicistat
ATC code:J05AR09
route:oral
compartments:1
dosage:200mg
volume of distribution:83.6L
clearance:25.3L/hr
other parameters in model implementation

This fixed-dose combination consists of emtricitabine (a nucleoside reverse transcriptase inhibitor), tenofovir disoproxil fumarate (a nucleotide reverse transcriptase inhibitor), elvitegravir (an integrase inhibitor), and cobicistat (a pharmacokinetic enhancer/booster). The combination is used as a complete regimen for the treatment of HIV-1 infection in adults and adolescents. It is widely approved and used as a single-tablet regimen to improve adherence and reduce pill burden in HIV therapy.

Pharmacokinetics

Pharmacokinetic parameters have been reported in healthy adult subjects after oral administration of the fixed-dose combination tablet (once daily). PK parameters reflect values at steady-state.

References

  1. Ogbuagu, O (2016). Rilpivirine, emtricitabine and tenofovir alafenamide: single-tablet combination for the treatment of HIV-1 infection in selected patients. Expert review of anti-infective therapy 14(12) 1113–1126. DOI:10.1080/14787210.2016.1255551 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27797606

  2. Yamada, H, et al., & Irie, S (2018). Effects of a Nutritional Protein-Rich Drink on the Pharmacokinetics of Elvitegravir, Cobicistat, Emtricitabine, Tenofovir Alafenamide, and Tenofovir Compared With a Standard Meal in Healthy Japanese Male Subjects. Clinical pharmacology in drug development 7(2) 132–142. DOI:10.1002/cpdd.365 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28581645

Parameters

TypeNameDefaultDescription
Modelica.Units.SI.Massweight (from PK_1C)75patient weight (kg)
Modelica.Units.SI.SpecificVolumeVdPerKg (from PK_1C)0.9Volume of distribution (L/kg)
Modelica.Units.SI.MassFractionF (from PK_1C)0.8bioavailiability (0-1)
Pharmacolibrary.Types.ClearanceCl (from PK_1C)20clearance
Modelica.Units.SI.TimeadminTime (from PK_1C)60first administration time (s)
Modelica.Units.SI.TimeadminDuration (from PK_1C)600administration duration (s)
Modelica.Units.SI.TimeadminPeriod (from PK_1C)8*60*60period of administration (default 8 hours)(s)
Pharmacolibrary.Types.MassadminMass (from PK_1C)1000administration mass (mg)
IntegeradminCount (from PK_1C)8number of dose administered (1)
Pharmacolibrary.Types.VolumeVd (from PK_1C)VdPerKg*weightVolume of distribution (m3)
Pharmacolibrary.Types.MassConcentrationCmin (from PK_1C)0.004minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCmax (from PK_1C)0.008minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCtox_peak (from PK_1C)0.012toxicity peak level
Pharmacolibrary.Types.MassConcentrationCtox_trough (from PK_1C)0.006toxicity trough level
Pharmacolibrary.Types.TransferRateka (from PK_1C_enteral)0.016666666666666666first order absorption rate
Modelica.Units.SI.TimeTlag (from PK_1C_enteral)600delay between oral administration and absorption (default 10min)

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)

Components

TypeNameDefaultDescription
Pharmacokinetic.NoPerfusedTissueCompartmentcentral (from PK_1C)
Pharmacokinetic.ClearanceDrivenEliminationelim (from PK_1C)
Sources.PeriodicDoseperiodicDose (from PK_1C)
Modelica.Units.SI.Timet1_2 (from PK_1C)elimination half-life

Revisions

  • 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)