ArticleNature communications2022
Transformation of dolutegravir into an ultra-long-acting parenteral prodrug formulation.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 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
23 citing papers in PubMed.
- Effect of Alkyl Chain Length on Physicochemical and Pharmacokinetic Performance of Aripiprazole Fatty Acid Prodrugs for Long-Acting Injectable Suspensions.Pharmaceutics · 2026Article
- Brief Report: Breast Milk Transfer and Infant Exposures to Dolutegravir, Tenofovir, and Tenofovir Alafenamide: Results From IMPAACT 2010/VESTED.Journal of acquired immune deficiency syndromes (1999) · 2026Article
- An ultra-long-acting dimeric bictegravir prodrug defined by a short pharmacokinetic tail.Nature communications · 2026Article
- A scalable ultra-long-acting tenofovir phosphonate prodrug sustains HBV suppression.Science advances · 2025Article
- Recent Advances in Antiviral Drug Delivery Strategies.AAPS PharmSciTech · 2025Review
- Advances in HIV Treatment: Long-Acting Antiretrovirals and the Path Toward a Cure.Biomedicines · 2025Article
- CEST MRI detects antiretroviral drug toxicities in the developing mouse brain.Frontiers in pharmacology · 2025Article
- Review
- Solubilization techniques used for poorly water-soluble drugs.Acta pharmaceutica Sinica. B · 2024Review
- Development of an extended action fostemsavir lipid nanoparticle.Communications biology · 2024Article
- Cell Culture Evaluation Hints Widely Available HIV Drugs Are Primed for Success if Repurposed for HTLV-1 Prevention.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Development and validation of an ultra-high performance liquid chromatography-tandem mass spectrometry method to quantify antiretroviral drug concentrations in human plasma for therapeutic monitoring.Journal of pharmaceutical and biomedical analysis · 2024Article
- Drug Nanocrystals: A Delivery Channel for Antiviral Therapies.AAPS PharmSciTech · 2024Review
- Polymer Delivery Systems for Long-Acting Antiretroviral Drugs.Pharmaceutics · 2024Review
- Polymer-prodrug conjugates as candidates for degradable, long-acting implants, releasing the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine.Journal of materials chemistry. B · 2023Article
- Article
- Prodrug approaches for the development of a long-acting drug delivery systems.Advanced drug delivery reviews · 2023Review
- Nanotherapeutic Approaches to Treat COVID-19-Induced Pulmonary Fibrosis.Biotech (Basel (Switzerland)) · 2023Review
- Long-acting dolutegravir formulations prevent neurodevelopmental impairments in a mouse model.Frontiers in pharmacology · 2023Article
- Lenacapavir with Fostemsavir in a Multidrug-Resistant HIV-Infected Hemodialysis Patient.Case reports in infectious diseases · 2023Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
23 authors.
Funding
Abstract
Ultra-long-acting integrase strand transfer inhibitors were created by screening a library of monomeric and dimeric dolutegravir (DTG) prodrug nanoformulations. This led to an 18-carbon chain modified ester prodrug nanocrystal (coined NM2DTG) with the potential to sustain yearly dosing. Here, we show that the physiochemical and pharmacokinetic (PK) formulation properties facilitate slow drug release from tissue macrophage depot stores at the muscle injection site and adjacent lymphoid tissues following single parenteral injection. Significant plasma drug levels are recorded up to a year following injection. Tissue sites for prodrug hydrolysis are dependent on nanocrystal dissolution and prodrug release, drug-depot volume, perfusion, and cell-tissue pH. Each affect an extended NM2DTG apparent half-life recorded by PK parameters. The NM2DTG product can impact therapeutic adherence, tolerability, and access of a widely used integrase inhibitor in both resource limited and rich settings to reduce HIV-1 transmission and achieve optimal treatment outcomes.
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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.