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The promise and pitfalls of long-acting injectable agents for HIV prevention
Open accessAbstract
PURPOSE OF REVIEW: Preexposure prophylaxis for HIV prevention is highly effective when taken as prescribed. Adherence to required dosing regimens for protection may pose challenges. Long-acting agents for HIV prevention may have the potential to improve adherence via favorable pharmacokinetics supportive of infrequent dosing. This review focuses on the potential benefits and considerations for the study and use of 2 long-acting injectable agents, cabotegravir (GSK1265744LA, CAB LA) and rilpivirine (TMC278LA, RPV LA), for use as chemoprophylaxis for HIV prevention. RECENT FINDINGS: Oral RPV is United States Food and Drug Administration approved for HIV treatment (in combination with other antiretrovirals). Both CAB LA and RPV LA are currently in phase 2a safety/tolerability/pharmacokinetic studies in anticipation and support of future efficacy evaluation. Both agents have favorable pharmacokinetics, and use is complicated by injection site reactions. SUMMARY: Long-acting injectable formulations, if safe and well tolerated, may improve pharmacokinetic coverage of exposures to HIV infection. Complexities around safety, tolerability, and starting/stopping protocols require careful consideration.
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“Dwindling amounts of drug released during the terminal phase of the release period may lead to a 'long pharmacologic tail' 20 , a period of slowly declining drug levels.”
From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [20]
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References 17 · Cited by 110
Metadata
- Authors
- Landovitz, R. J., Kofron, R., & McCauley, M.
- Affiliations
- University of California, Los Angeles (US)
- Family Health International 360 (US)
- Corresponding author
- Landovitz, Raphael J.
- Venue
- Current Opinion in HIV and AIDS
- Published
- 2016-01
- Volume
- 11
- Issue
- 1
- Pages
- 122-128
- ISSN
- 1746-630X (ISSN-L)
- PMC
- PMC4747082
- OpenAlex
- W2418956875
- Cited by
- 110
- References
- 17
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 8 · 2023: 3 · 2022: 7 · 2021: 21 · 2020: 11 · 2019: 15 · 2018: 19 · 2017: 17 · 2016: 5
- FWCI
- 10.66
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Current Opinion in HIV and AIDS (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- eScholarship (California Digital Library) (submittedVersion)
- Funders
- National Institute of Mental Health (P30MH058107)
- National Institute of Allergy and Infectious Diseases (U01AI068619, UM1AI068619, UM1AI068613, UM1AI068617)
- Topics
- Health Sciences › Medicine › Infectious Diseases › HIV/AIDS Research and Interventions
- Health Sciences › Medicine › Infectious Diseases › HIV/AIDS drug development and treatment
- Health Sciences › Medicine › Epidemiology › HIV, Drug Use, Sexual Risk
- Keywords
- long-acting injectable antiretrovirals, HIV pre-exposure prophylaxis, cabotegravir, rilpivirine, medication adherence, pharmacokinetics, injection site reactions, tolerability, HIV prevention
- MeSH terms
- Rilpivirine, Delayed-Action Preparations, Humans, Injections, United States, HIV Infections, Clinical Trials, Phase II as Topic, Disease Transmission, Infectious, Chemoprevention, Anti-HIV Agents, Pre-Exposure Prophylaxis
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