ArticleNature communications2021
Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir.
Article in Nature communications, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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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
19 citing papers in PubMed, 45 citations in OpenAlex.
- An ultra-long-acting dimeric bictegravir prodrug defined by a short pharmacokinetic tail.Nature communications · 2026Article
- The synthesis of indomethacin prodrugs for the formation of nanosuspensions by emulsion templated freeze drying.RSC advances · 2025Article
- Review
- New Therapies and Strategies to Curb HIV Infections with a Focus on Macrophages and Reservoirs.Viruses · 2024Review
- Carrier-Free, Amorphous Verteporfin Nanodrug for Enhanced Photodynamic Cancer Therapy and Brain Drug Delivery.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Recent advances of nanocrystals in cancer theranostics.Nanoscale advances · 2023Review
- Nanotherapeutic Approaches to Treat COVID-19-Induced Pulmonary Fibrosis.Biotech (Basel (Switzerland)) · 2023Review
- Long-acting HIV pre-exposure prophylaxis (PrEP) approaches: recent advances, emerging technologies, and development challenges.Expert opinion on drug delivery · 2022Review
- Real-Life Therapeutic Concentration Monitoring of Long-Acting Cabotegravir and Rilpivirine: Preliminary Results of an Ongoing Prospective Observational Study in Switzerland.Pharmaceutics · 2022Article
- Transformation of dolutegravir into an ultra-long-acting parenteral prodrug formulation.Nature communications · 2022Article
- Analyte recovery in LC-MS/MS bioanalysis: An old issue revisited.Analytica chimica acta · 2022Article
- Non-Viral Vectors for Delivery of Nucleic Acid Therapies for Cancer.Biotech (Basel (Switzerland)) · 2022Review
- Oral antivirals for the prevention and treatment of SARS-CoV-2 infection.AIDS reviews · 2022Article
- Prodrug Therapies for Infectious and Neurodegenerative Diseases.Pharmaceutics · 2022Review
- Evolution of drug delivery systems: From 1950 to 2020 and beyond.Journal of controlled release : official journal of the Controlled Release Society · 2022Article
- Towards the Antiviral Agents and Nanotechnology-Enabled Approaches Against Parvovirus B19.Frontiers in cellular and infection microbiology · 2022Review
- Ultra-long-acting (XLA) antivirals for chronic viral hepatitis.International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases · 2022Article
- Pre-Exposure Prophylaxis for viral infections other than HIV.Le infezioni in medicina · 2022Review
- Rational Design of Thermosensitive Hydrogel to Deliver Nanocrystals with Intranasal Administration for Brain Targeting in Parkinson's Disease.Research (Washington, D.C.) · 2021Article
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
Abstract
A once every eight-week cabotegravir (CAB) long-acting parenteral is more effective than daily oral emtricitabine and tenofovir disoproxil fumarate in preventing human immunodeficiency virus type one (HIV-1) transmission. Extending CAB dosing to a yearly injectable advances efforts for the elimination of viral transmission. Here we report rigor, reproducibility and mechanistic insights for a year-long CAB injectable. Pharmacokinetic (PK) profiles of this nanoformulated CAB prodrug (NM2CAB) are affirmed at three independent research laboratories. PK profiles in mice and rats show plasma CAB levels at or above the protein-adjusted 90% inhibitory concentration for a year after a single dose. Sustained native and prodrug concentrations are at the muscle injection site and in lymphoid tissues. The results parallel NM2CAB uptake and retention in human macrophages. NM2CAB nanocrystals are stable in blood and tissue homogenates. The long apparent drug half-life follows pH-dependent prodrug hydrolysis upon slow prodrug nanocrystal dissolution and absorption. In contrast, solubilized prodrug is hydrolyzed in hours in plasma and tissues from multiple mammalian species. No toxicities are observed in animals. These results affirm the pharmacological properties and extended apparent half-life for a nanoformulated CAB prodrug. The report serves to support the mechanistic design for drug formulation safety, rigor and reproducibility.
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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.