ArticleAntimicrobial agents and chemotherapy2010
Pharmacokinetics and disposition of rilpivirine (TMC278) nanosuspension as a long-acting injectable antiretroviral formulation.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 77 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
77 citing papers in PubMed, 186 citations in OpenAlex.
- A scalable ultra-long-acting tenofovir phosphonate prodrug sustains HBV suppression.Science advances · 2025Article
- Cryo-EM Structure of HIV-1 Reverse Transcriptase withACS infectious diseases · 2025Article
- Novel pH-Responsive Structural Rearrangement of Myristic Acid-Conjugated Quetiapine Nanosuspension for Enhanced Long-Acting Delivery Performance.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Lipid nanocarrier targeting activated macrophages for antiretroviral therapy of HIV reservoir.Nanomedicine (London, England) · 2023Article
- Development and Evaluation of Dissolving Microarray Patches for Co-administered and Repeated Intradermal Delivery of Long-acting Rilpivirine and Cabotegravir Nanosuspensions for Paediatric HIV Antiretroviral Therapy.Pharmaceutical research · 2023Article
- A Retrospective Analysis of Preclinical and Clinical Pharmacokinetics from Administration of Long-Acting Aqueous Suspensions.Pharmaceutical research · 2023Article
- A SWOT analysis of nano co-crystals in drug delivery: present outlook and future perspectives.RSC advances · 2023Review
- Nano drug-delivery systems for management of AIDS: liposomes, dendrimers, gold and silver nanoparticles.Nanomedicine (London, England) · 2023Review
- Effect of Dispersion Medium on Pharmacokinetic Profile of Rotigotine Crystalline Suspension following Subcutaneous Injection.Pharmaceutics · 2022Article
- A Holistic Review of the Preclinical Landscape for Long-Acting Anti-infective Drugs Using HIV as a Paradigm.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2022Review
- Long-acting HIV pre-exposure prophylaxis (PrEP) approaches: recent advances, emerging technologies, and development challenges.Expert opinion on drug delivery · 2022Review
- Leveraging the therapeutic, biological, and self-assembling potential of peptides for the treatment of viral infections.Journal of controlled release : official journal of the Controlled Release Society · 2022Review
- Approved HIV reverse transcriptase inhibitors in the past decade.Acta pharmaceutica Sinica. B · 2022Review
- Transformation of tenofovir into stable ProTide nanocrystals with long-acting pharmacokinetic profiles.Nature communications · 2021Article
- Biodegradable polymeric solid implants for ultra-long-acting delivery of single or multiple antiretroviral drugs.International journal of pharmaceutics · 2021Article
- A review of existing strategies for designing long-acting parenteral formulations: Focus on underlying mechanisms, and future perspectives.Acta pharmaceutica Sinica. B · 2021Review
- Injectable Antiretroviral Drugs: Back to the Future.Viruses · 2021Review
- Mechanistic Modeling of Maternal Lymphoid and Fetal Plasma Antiretroviral Exposure During the Third Trimester.Frontiers in pediatrics · 2021Article
- Development and Comparison of Intramuscularly Injected Long-acting Testosterone Undecanoate Nano-/Microcrystal Suspensions with Three Different Particle Size.Iranian journal of pharmaceutical research : IJPR · 2021Article
- Long-acting approaches for delivery of antiretroviral drugs for prevention and treatment of HIV: a review of recent research.Expert opinion on drug delivery · 2020Review
17 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The next-generation human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitor rilpivirine (TMC278) was administered in rats and dogs as single intramuscular (IM) or subcutaneous (SC) injections, formulated as a 200-nm nanosuspension. The plasma pharmacokinetics, injection site concentrations, disposition to lymphoid tissues, and tolerability were evaluated in support of its potential use as a once-monthly antiretroviral agent in humans. Rilpivirine plasma concentration-time profiles showed sustained and dose-proportional release over 2 months in rats and over 6 months in dogs. The absolute bioavailability approached 100%, indicating a complete release from the depot, in spite of rilpivirine concentrations still being high at the injection site(s) 3 months after administration in dogs. For both species, IM administration was associated with higher initial peak plasma concentrations and a more rapid washout than SC administration, which resulted in a stable plasma-concentration profile over at least 6 weeks in dogs. The rilpivirine concentrations in the lymph nodes draining the IM injection site exceeded the plasma concentrations by over 100-fold 1 month after administration, while the concentrations in the lymphoid tissues decreased to 3- to 6-fold the plasma concentrations beyond 3 months. These observations suggest uptake of nanoparticles by macrophages, which generates secondary depots in these lymph nodes. Both SC and IM injections were generally well tolerated and safe, with observations of a transient inflammatory response at the injection site. The findings support clinical investigations of rilpivirine nanosuspension as a long-acting formulation to improve adherence during antiretroviral therapy and for preexposure prophylaxis.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.