2022
DOI: 10.21203/rs.3.rs-1255147/v1
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Pathways for Dolutegravir Transformation from a Daily Oral to a Once-a-Year Parenteral Medicine

Abstract: An “ultra” long-acting (LA) integrase strand transfer inhibitor was created by screening a library of monomeric and dimeric dolutegravir (DTG) prodrug nanoformulations. This led, to the best of our knowledge, a “first in class” 18-carbon chain modified prodrug nanocrystal (coined as NM2DTG). Ideal physiochemical and pharmacokinetic (PK) properties facilitated slow drug release from tissue macrophage prodrug depot stores for up to one year after a single intramuscular injection. Both the muscle injection site a… Show more

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“…Indeed, pre-exposure prophylaxis has shown its benefit in the prevention of viral acquisition in uninfected individuals engaged in high-risk behaviors 54 . Recent advances in chemical pharmacology have led to the emergence of ultra-long-acting (XLA) antiviral formulations that may provide drug exposure for several months or up to 1 year [55][56][57][58][59] . The advent of these medicines might transform the way to confront new COVID-19 surges.…”
Section: Long-acting Antiviral Formulationsmentioning
confidence: 99%
“…Indeed, pre-exposure prophylaxis has shown its benefit in the prevention of viral acquisition in uninfected individuals engaged in high-risk behaviors 54 . Recent advances in chemical pharmacology have led to the emergence of ultra-long-acting (XLA) antiviral formulations that may provide drug exposure for several months or up to 1 year [55][56][57][58][59] . The advent of these medicines might transform the way to confront new COVID-19 surges.…”
Section: Long-acting Antiviral Formulationsmentioning
confidence: 99%