modelV03AX03
Extends from Pharmacokinetic.Models.PK_1C_enteral.
Information
| name: | Cobicistat | |
| ATC code: | V03AX03 | route: | oral |
| compartments: | 1 | |
| dosage: | 150 | mg |
| volume of distribution: | 2.4 | L |
| clearance: | 1.0 | L/h |
| other parameters in model implementation | ||
Cobicistat is a potent, selective inhibitor of cytochrome P450 3A (CYP3A) enzymes used as a pharmacokinetic enhancer (booster) for certain antiretroviral drugs, particularly HIV-1 protease inhibitors (such as atazanavir, darunavir) and the integrase inhibitor elvitegravir. Cobicistat has no activity against HIV-1 itself and is not used as monotherapy. It is currently approved and used in combination with other antiretrovirals.
Pharmacokinetics
Pharmacokinetic parameters in healthy adult volunteers, mixed sex, single dose under fasting and fed (high fat meal) conditions.
References
Eisenmann, ED, et al., & Baker, SD (2021). Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition. Cancer research communications 1(2) 79–89. DOI:10.1158/2767-9764.crc-21-0076 PUBMED:https://pubmed.ncbi.nlm.nih.gov/34950932
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
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
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.TransferRate | ka (from PK_1C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_1C_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) |
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 |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)