Antiretroviral Pharmacokinetics in HIV Treatment

Antiretroviral pharmacokinetics examines how drugs used to treat HIV are absorbed, distributed, metabolised and eliminated in the body. Understanding these processes is critical to ensuring effective viral suppression, minimising toxicity and preventing the emergence of drug resistance. Many antiretroviral agents, notably nucleotide and nucleoside reverse transcriptase inhibitors, are administered as prodrugs that require intracellular conversion to active metabolites. Differences in oral bioavailability, plasma half-life and tissue penetration underpin the choice of formulation and dosing regimen. Advances in pharmacokinetic modelling have informed the development of tenofovir disoproxil fumarate and tenofovir alafenamide, highlighting trade-offs between systemic exposure and intracellular activation. Moreover, long-acting injectable and implantable delivery systems are under investigation to enhance adherence and broaden global access. Therapeutic drug monitoring and point-of-care assays are emerging as tools to tailor therapy to individual patient profiles, address variability in drug exposure and support safer lifelong treatment across diverse populations.

Research from Nature Portfolio

No recent Nature Portfolio content available.

Antiretroviral Pharmacokinetics in HIV Treatment publication trend

The graph below shows the total number of articles in antiretroviral pharmacokinetics in hiv treatment across all publications each year (not limited to Nature Index journals).

Technical terms

Bioavailability: The proportion of an administered dose that reaches the systemic circulation.

Prodrug: An inactive compound converted in the body to its pharmacologically active form.

Area under the curve (AUC): A measure of total drug exposure over time.

Cmax: The peak plasma concentration achieved after drug administration.

Therapeutic drug monitoring (TDM): Measurement of drug levels to guide individualised dosing.

References

1. Development and In-House Validation of an Enzyme-Linked Immunosorbent Assay and a Lateral Flow Immunoassay for the Dosage of Tenofovir in Human Saliva. Biosensors (2023).
2. Pharmacokinetic Feasibility of Stability-Enhanced Solid-State (SESS) Tenofovir Disoproxil Free Base Crystal. Pharmaceutics (2023).
3. A Review and Clinical Understanding of Tenofovir: Tenofovir Disoproxil Fumarate versus Tenofovir Alafenamide. Journal of the International Association of Providers of AIDS Care (JIAPAC) (2020).