The DOI matches its Crossref record; 23 of the 23 references it cites were found in a registry or an index.
Formulation and pharmacology of long-acting rilpivirine
Abstract
PURPOSE OF REVIEW: Rilpivirine (RPV), a nonnucleoside reverse transcriptase inhibitor, is a potent antiretroviral (ARV) effective for HIV treatment at 25 mg daily oral dose. Its physio-chemical and pharmacological properties enable formulation of RPV as a long-acting injectable nanosuspension. This review summarizes these properties supporting the potential of intermittent parenteral administration of rilpivirine long acting (RPV LA) in both treatment and prevention of HIV-1 infection. RECENT FINDINGS: RPV is unusual among ARVs in that its stability and solubility enable aqueous suspensions with high drug loading, so that injection volumes can be minimized. Such innovative nanosuspensions are well tolerated in animals and humans after intramuscular injection and provide sustained drug concentrations in systemic circulation. The pharmacological findings support further investigations of RPV LA injections every 4 or 8 weeks, both as a single agent for potential preexposure prophylaxis and as two-drug all-injectable maintenance therapy with cabotegravir long acting. SUMMARY: By building on expertise with long-acting injectable antipsychotic agents, RPV has been formulated as an agent for infrequent intramuscular dosing, in addition to its conventional oral tablet forms. The advantages of adherence to a regimen of intermittent injections may be significant.
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“Specifically, nanoparticles of two antiretrovirals, cabotegravir and rilpivirine, are being actively pursued in the clinic.”
From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [17]
In the citing paper
“Cabotegravir 16 and rilpivirine 17 were chosen owing to their efficacy at low oral doses and low water solubility.”
From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [17]
Citations
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Huang, Y., Guo, X., Wu, Y., Chen, X., Feng, L., Xie, N., & Shen, G. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01745-z · Cited by 537
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Metadata
- Authors
- Williams, P. E., Crauwels, H. M., & Basstanie, E. D.
- Affiliations
- Janssen (Belgium) (BE)
- Corresponding author
- Williams, Peter E.
- ORCID
- Crauwels, Herta M.
- Venue
- Current Opinion in HIV and AIDS
- Published
- 2015-07
- Volume
- 10
- Issue
- 4
- Pages
- 233-238
- ISSN
- 1746-630X (ISSN-L)
- OpenAlex
- W2395339327
- Cited by
- 86
- References
- 23
- Citations by year
- 2026: 3 · 2025: 6 · 2024: 7 · 2023: 9 · 2022: 8 · 2021: 10 · 2020: 5 · 2019: 14 · 2018: 10 · 2017: 9 · 2016: 4 · 2015: 1
- FWCI
- 6.22
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Opinion in HIV and AIDS (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Infectious Diseases › HIV/AIDS drug development and treatment
- Health Sciences › Medicine › Infectious Diseases › HIV/AIDS Research and Interventions
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- rilpivirine, long-acting injectables, nanoparticle suspensions, HIV-1, non-nucleoside reverse transcriptase inhibitors, antiretroviral therapy, pre-exposure prophylaxis, cabotegravir, intramuscular injection, drug formulation, pharmacokinetics, drug solubility and stability
- MeSH terms
- Rilpivirine, Humans, HIV-1, HIV Infections, Reverse Transcriptase Inhibitors, Anti-HIV Agents
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