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Long-acting Injectable Containing Lopinavir Eliminates Reliance on Ritonavir Pharmacokinetic Enhancement
Simone Perazzolo1, Charles W Flexner2, Zachary R Stephen1
1Department of Pharmaceutics, University of Washington, Seattle, Washington, USA.
Abstract:
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.
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