Long-acting Injectable Containing Lopinavir Eliminates Reliance on Ritonavir Pharmacokinetic Enhancement
High-extraction protease inhibitors (eg, for human immunodeficiency virus and severe acute respiratory syndrome coronavirus 2) typically require ritonavir to enhance bioavailability by overcoming first-pass metabolism. However, in the long-acting subcutaneous injectable dosage form TLC-ART 101, lopinavir persisted in plasma for 57 days, while ritonavir was detectable for only 3-7 days. The remarkable duration of lopinavir suggests that ritonavir may be unnecessary in long-acting injectable products, potentially reducing side effects and drug-drug interactions.
Authors
- Zachary R. Stephen (ORCID: https://orcid.org/0000-0002-2014-3100)
- Rachel Bender Ignacio (ORCID: https://orcid.org/0000-0001-6167-1447)
- Charles Flexner (ORCID: https://orcid.org/0000-0002-4495-5349)
- Rodney J. Y. Ho (ORCID: https://orcid.org/0000-0001-5960-4288)
- Simone Perazzolo (ORCID: https://orcid.org/0000-0003-4498-7823)
- Edward P. Acosta
Institutions
- Johns Hopkins University (US)
- University of Washington (US)
- Johns Hopkins Medicine (US)
- University of Alabama at Birmingham (US)
- Fred Hutch Cancer Center (US)
Publication Details
- Journal
- The Journal of Infectious Diseases
- Published
- 2025-06-24
- DOI
- https://doi.org/10.1093/infdis/jiaf319
- Citations
- 1
- Primary Topic
- HIV/AIDS drug development and treatment
- Type
- article
- Field-Weighted Citation Impact
- 1.40