modelDegarelix

Diagram of Degarelix

Extends from Pharmacolibrary.Drugs.ATC.L.L02BX02.

Information

name:Degarelix
ATC code:L02BX02
route:subcutaneous
compartments:2
dosage:240mg
volume of distribution:19L
clearance:0.88L/h
other parameters in model implementation

Degarelix is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of advanced hormone-dependent prostate cancer in men. It acts by suppressing the production of luteinizing hormone and subsequently testosterone without causing a testosterone surge. Degarelix is currently approved for medical use in many countries for prostate cancer.

Pharmacokinetics

Pharmacokinetic parameters reported in adult males with prostate cancer following subcutaneous administration.

References

  1. Tornøe, CW, et al., & Jonsson, EN (2004). Population pharmacokinetic modeling of a subcutaneous depot for GnRH antagonist degarelix. Pharmaceutical research 21(4) 574–584. DOI:10.1023/b:pham.0000022403.60314.51 PUBMED:https://pubmed.ncbi.nlm.nih.gov/15139513

  2. Tornøe, CW, et al., & Jonsson, EN (2007). Population pharmacokinetic/pharmacodynamic (PK/PD) modelling of the hypothalamic-pituitary-gonadal axis following treatment with GnRH analogues. British journal of clinical pharmacology 63(6) 648–664. DOI:10.1111/j.1365-2125.2006.02820.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/17096678

  3. Tornøe, CW, et al., & Jonsson, EN (2005). Stochastic differential equations in NONMEM: implementation, application, and comparison with ordinary differential equations. Pharmaceutical research 22(8) 1247–1258. DOI:10.1007/s11095-005-5269-5 PUBMED:https://pubmed.ncbi.nlm.nih.gov/16078134

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.VolumeVdp (from PK_2C)VdpPerKg*weightVolume of distribution (m3)
Modelica.Units.SI.SpecificVolumeVdpPerKg (from PK_2C)0.9Volume of distribution peripheral(l/kg)
Pharmacolibrary.Types.Clearancek12 (from PK_2C)1intercompartmental C-P clearance
Pharmacolibrary.Types.Clearancek21 (from PK_2C)1intercompartmental P-C clearance

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)
Interfaces.ConcentrationPort_bperipheralCPort (from PK_2C)
Pharmacolibrary.Types.ConcentrationOutputC_peripheral1 (from PK_2C)

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
Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSymtransfer (from PK_2C)
Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartmentperipheral (from PK_2C)

Revisions

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