modelH01CC53

Diagram of H01CC53

Extends from Pharmacokinetic.Models.PK_1C_enteral.

Information

name:ElagolixEstradiolAndNorethisterone
ATC code:H01CC53
route:oral
compartments:1
dosage:300mg
volume of distribution:120L
clearance:12L/h
other parameters in model implementation

Elagolix, estradiol, and norethisterone are combined in an oral contraceptive and hormone therapy regimen, often studied for the treatment of endometriosis-associated pain and/or uterine fibroids. Elagolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol is a form of estrogen, and norethisterone (also known as norethindrone) is a progestin. The combination is used to modulate hormonal balance, reduce bone loss risk, and mitigate hypoestrogenic symptoms in women taking elagolix.

Pharmacokinetics

Estimated pharmacokinetic parameters for healthy adult women (average age 18-49), based on published monograph pharmacokinetics of the individual components, as there are currently no comprehensive published human PK models for the fixed-dose combination.

References

    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)