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Updated: Feb 20, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Rilpivirine: The Key for Long-term Success
1Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, HIV and PK Research Group, Institute of Biomedicine of Seville (IBiS), University of Seville, CSIC, University Hospital Virgen del Rocío, Sevilla, Spain.
Abstract:
During the past 30 years of antiretroviral therapy, continuous improvements in drug discovery have provided increasingly potent and safer antivirals that have transformed HIV infection in a chronic illness, rarely fatal. Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are frequently used as part of any antiretroviral combination therapy. Side effects and low resistance barrier of fi rst-generation NNRTIs (e.g., nevirapine and efavirenz) have been overcome with rilpivirine (RPV), and the last NNRTI approved for the treatment of HIV infection. The good efficacy, safety profi le, and convenient dosing of RPV account for the unique durability of RPV-based regimens. The advent of new oral fi xed-dose coformulations of RPV (e.g., along with dolutegravir or with tenofovir alafenamide [TAF]/emtricitabine [FTC]) as well as the development of long-acting injectable RPV nanoformulations will further expand its therapeutic landscape, including RPV use in dual maintenance therapy in HIV-infected patients or as pre-exposure prophylaxis in high-risk uninfected individuals.
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