ArticleBritish journal of clinical pharmacology2022
Multiparametric magnetic resonance imaging to characterize cabotegravir long-acting formulation depot kinetics in healthy adult volunteers.
Article in British journal of clinical pharmacology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 31 citations in OpenAlex.
- Population pharmacokinetics of cabotegravir following intramuscular thigh injections in adults with and without HIV.Antimicrobial agents and chemotherapy · 2024Trial
- Virtual Bioequivalence Assessment of Long-acting Injectable Suspensions Using PBPK Modeling: Part 1. Impact of particle Size on Formulation Variability.The AAPS journal · 2026Article
- Mechanistic Modeling of Intramuscular Administration of a Long-acting Injectable Accounting for Tissue Response At the Depot Site.The AAPS journal · 2025Article
- The impact of product quality attributes on in vivo performance of bupivacaine multivesicular liposomes.Drug delivery and translational research · 2025Article
- Leveraging Model Master Files for Long-Acting Injectables.Pharmaceutical research · 2025Article
- Effect of Obesity on the Exposure of Long-acting Cabotegravir and Rilpivirine: A Modeling Study.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2024Article
- Tricaprylin-based drug crystalline suspension for intramuscular long-acting delivery of entecavir with alleviated local inflammation.Bioengineering & translational medicine · 2024Article
- Development of a physiologically-based pharmacokinetic model to simulate the pharmacokinetics of intramuscular antiretroviral drugs.CPT: pharmacometrics & systems pharmacology · 2024Article
- Development of Mechanistic In Vitro-In Vivo Extrapolation to Support Bioequivalence Assessment of Long-Acting Injectables.Pharmaceutics · 2024Article
- Drug Exposure of Long-Acting Cabotegravir and Rilpivirine in Older People With Human Immunodeficiency Virus: A Pharmacokinetic Modeling Study.Open forum infectious diseases · 2024Article
- Population pharmacokinetics of rilpivirine following oral administration and long-acting intramuscular injection in real-world people with HIV.Frontiers in pharmacology · 2024Article
- Demonstration Project of Long-Acting Antiretroviral Therapy in a Diverse Population of People With HIV.Annals of internal medicine · 2023Observational
- Characterization of large volume subcutaneous injections using computed tomography imaging and simultaneous pressure measurements.Frontiers in drug delivery · 2023Article
- A population pharmacokinetic model based on HPTN 077 of long-acting injectable cabotegravir for HIV PrEP.British journal of clinical pharmacology · 2022Article
- Multiparametric magnetic resonance imaging to characterize cabotegravir long-acting formulation depot kinetics in healthy adult volunteers.British journal of clinical pharmacology · 2022Article
- MRI/PET multimodal imaging of the innate immune response in skeletal muscle and draining lymph node post vaccination in rats.Frontiers in immunology · 2022Article
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Authors and funding
20 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimCabotegravir long-acting (LA) intramuscular (IM) injection is being investigated for HIV preexposure prophylaxis due to its potent antiretroviral activity and infrequent dosing requirement. A subset of healthy adult volunteers participating in a Phase I study assessing cabotegravir tissue pharmacokinetics underwent serial magnetic resonance imaging (MRI) to assess drug depot localization and kinetics following a single cabotegravir LA IM targeted injection.
methodsEight participants (four men, four women) were administered cabotegravir LA 600 mg under ultrasonographic-guided injection targeting the gluteal muscles. MRI was performed to determine injection-site location in gluteal muscle (IM), subcutaneous (SC) adipose tissue and combined IM/SC compartments, and to quantify drug depot characteristics, including volume and surface area, on Days 1 (≤2 hours postinjection), 3 and 8. Linear regression analysis examined correlations between MRI-derived parameters and plasma cabotegravir exposure metrics, including maximum observed concentration (C
resultsCabotegravir LA depot locations varied by participant and were identified in the IM compartment (n = 2), combined IM/SC compartments (n = 4), SC compartment (n = 1) and retroperitoneal cavity (n = 1). Although several MRI parameter and exposure metric correlations were determined, total depot surface area on Day 1 strongly correlated with plasma cabotegravir concentration at Days 3 and 8, C
conclusionMRI clearly delineated cabotegravir LA injection-site location and depot kinetics in healthy adults. Although injection-site variability was observed, drug depot surface area correlated with both plasma C
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