Complete Guide to DTg Pharmacokinetics
Overview
DTg is a Integrase Strand Transfer Inhibitor (INSTI) used in the HIV / Infectious Disease therapeutic area. It is indicated for HIV-1 infection (antiretroviral therapy). Interactive pharmacokinetic simulator for Dolutegravir (DTG, Tivicay) — 1-compartment model with pregnancy and drug interaction effects. Based on Liu et al. 2020 PBPK and Dooley et al. 2015 population PK.
Key Pharmacokinetic Parameters
The following parameters are derived from published Population PK (1-CMT, oral) models for DTg:
| Parameter | Value |
|---|---|
| ka | 2.24 h⁻¹ |
| CL F | 0.901 L/h |
| Cmax | ~3.67 µg/mL (50 mg QD, steady state) |
| Vc F | 17.4 L |
| dose | 50 mg QD or 50 mg BID |
| brand | Tivicay |
| route | Oral |
| t lag | 0.263 h |
| t half | ~14 h |
| Ctrough | ~1.11 µg/mL (50 mg QD) |
| IC90 PA | 0.064 µg/mL (protein-adjusted) |
| protein binding | >98.9% |
| pregnancy 2nd tri | CL/F ↑72% vs non-pregnant |
| pregnancy 3rd tri | CL/F ↑85% vs non-pregnant |
Parameters represent typical population estimates from published literature. Individual values may vary.
Dosing & Administration
DTg is administered via the Oral route. Oral administration involves absorption from the gastrointestinal tract, and bioavailability may be affected by food intake, formulation, and first-pass metabolism.
Dosing recommendations should always follow approved prescribing information. The interactive simulator allows you to explore different dosing scenarios and their impact on drug exposure metrics such as AUC, Cmax, and Ctrough.
Clinical Considerations
In the HIV / Infectious Disease therapeutic area, for the treatment of HIV-1 infection (antiretroviral therapy), understanding the pharmacokinetics of DTg is essential for dose optimization and therapeutic drug monitoring. Key clinical factors that may affect DTg pharmacokinetics include:
- •Body weight and body composition
- •Renal and hepatic function
- •Drug-drug interactions and concomitant medications
- •Age, sex, and genetic polymorphisms
Interactive DTg PK Simulator
Explore DTg pharmacokinetics interactively. Adjust doses, dosing intervals, and patient covariates to visualize concentration-time profiles in real time.
Frequently Asked Questions
What is the half-life of DTg?
The elimination half-life of DTg depends on patient-specific factors. Based on published models, the typical half-life is approximately ~14 h.
How is DTg administered?
DTg is administered via the Oral route. It is indicated for HIV-1 infection (antiretroviral therapy). As a Integrase Strand Transfer Inhibitor (INSTI), dosing regimens should follow approved prescribing information and clinical guidelines.
What are the key PK parameters of DTg?
Key pharmacokinetic parameters for DTg include clearance (CL), volume of distribution (Vd), and elimination half-life. See the PK Parameters section above for specific values from published models.
Can I simulate DTg dosing scenarios for free?
Yes! PKPDBuilder offers a completely free, interactive DTg PK simulator based on published pharmacometric models. No login required. Use it to explore different doses, dosing intervals, and patient covariates.
⚠️ Disclaimer
This guide is for research and educational purposes only. It is not intended for clinical decision-making or patient dosing. Parameters are derived from published literature and represent population estimates. Always consult approved prescribing information for clinical use.