Francesca Ferretti1, Marta Boffito1,2. 1. St Stephen's Centre, Chelsea and Westminster Hospital and Foundation Trust. 2. Department of Medicine, Imperial College London, London, UK.
Abstract
PURPOSE OF REVIEW: Rilpivirine is a non-nucleoside reverse transcriptase inhibitor approved for the treatment of HIV in combination with other antiretrovirals (ARV). The development of the long-acting formulation of rilpivirine (RPV-LA) and its use in clinical settings is the subject of this review. RECENT FINDINGS: In 2017, the results of the phase IIb study LATTE2 have been published. This study demonstrated that the combination of RPV-LA with a second long-acting agent (cabotegravir) administered intramuscularly every 4--8 weeks was similar in virologic suppression rates to standard of care ARV treatment. SUMMARY: RPV-LA is an injectable nanoparticle suspension for intramuscular use. Phase I studies in healthy volunteers demonstrated that RPV-LA, administered at doses between 600 and 1200 mg, was well tolerated and effective in maintaining satisfactory drug concentrations in plasma, vaginal secretions and rectal tissue compartments for at least 4 weeks. RPV-LA efficacy was also shown in a phase II clinical trial in HIV infected patients and phase III studies are currently ongoing. Most study participants stated that they would use or continue using injectables, both in HIV treatment and prevention settings. Long-acting injectable ARVs have the potential to improve the convenience of HIV drug regimens.
PURPOSE OF REVIEW: Rilpivirine is a non-nucleoside reverse transcriptase inhibitor approved for the treatment of HIV in combination with other antiretrovirals (ARV). The development of the long-acting formulation of rilpivirine (RPV-LA) and its use in clinical settings is the subject of this review. RECENT FINDINGS: In 2017, the results of the phase IIb study LATTE2 have been published. This study demonstrated that the combination of RPV-LA with a second long-acting agent (cabotegravir) administered intramuscularly every 4--8 weeks was similar in virologic suppression rates to standard of care ARV treatment. SUMMARY: RPV-LA is an injectable nanoparticle suspension for intramuscular use. Phase I studies in healthy volunteers demonstrated that RPV-LA, administered at doses between 600 and 1200 mg, was well tolerated and effective in maintaining satisfactory drug concentrations in plasma, vaginal secretions and rectal tissue compartments for at least 4 weeks. RPV-LA efficacy was also shown in a phase II clinical trial in HIV infectedpatients and phase III studies are currently ongoing. Most study participants stated that they would use or continue using injectables, both in HIV treatment and prevention settings. Long-acting injectable ARVs have the potential to improve the convenience of HIV drug regimens.
Authors: Kurtis Moffatt; Ismaiel A Tekko; Lalitkumar Vora; Fabiana Volpe-Zanutto; Aaron R J Hutton; Jessica Mistilis; Courtney Jarrahian; Nima Akhavein; Andrew D Weber; Helen O McCarthy; Ryan F Donnelly Journal: Pharm Res Date: 2022-10-12 Impact factor: 4.580
Authors: Kevin Melody; Chandra N Roy; Christopher Kline; Mackenzie L Cottrell; Dwayne Evans; Kathleen Shutt; Pleuni S Pennings; Brandon F Keele; Moses Bility; Angela D M Kashuba; Zandrea Ambrose Journal: J Virol Date: 2020-03-31 Impact factor: 6.549