modelG01AX17
Extends from Pharmacokinetic.Models.PK_1C.
Information
| name: | Dapivirine | |
| ATC code: | G01AX17 | route: | vaginal |
| compartments: | 1 | |
| dosage: | 25 | mg |
| volume of distribution: | 56.6 | L |
| clearance: | 4.91 | L/h |
| other parameters in model implementation | ||
Dapivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used primarily in the form of a vaginal ring to prevent HIV-1 infection in women. The drug is designed for topical use to achieve high local concentrations and minimal systemic exposure. Dapivirine vaginal rings have received a positive scientific opinion from the European Medicines Agency and are recommended by the World Health Organization for HIV prevention in women.
Pharmacokinetics
Pharmacokinetic parameters reported for healthy adult women, post-menopausal and reproductive age, enrolled in clinical trials assessing dapivirine vaginal ring (25 mg), steady-state achieved after repeated monthly administration.
References
Noguchi, LM, et al., & Beigi, RH (2019). Pharmacokinetics of Dapivirine Transfer into Blood Plasma, Breast Milk, and Cervicovaginal Fluid of Lactating Women Using the Dapivirine Vaginal Ring. Antimicrobial agents and chemotherapy 63(3) –. DOI:10.1128/AAC.01930-18 PUBMED:https://pubmed.ncbi.nlm.nih.gov/30602513
Benítez-Gutiérrez, L, et al., & de Mendoza, C (2018). Treatment and prevention of HIV infection with long-acting antiretrovirals. Expert review of clinical pharmacology 11(5) 507–517. DOI:10.1080/17512433.2018.1453805 PUBMED:https://pubmed.ncbi.nlm.nih.gov/29595351
Bunge, KE, et al., & Squires, KE (2020). Brief Report: Phase IIa Safety Study of a Vaginal Ring Containing Dapivirine in Adolescent Young Women. Journal of acquired immune deficiency syndromes (1999) 83(2) 135–139. DOI:10.1097/QAI.0000000000002244 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31929401
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 |
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)