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Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. In an approach to evade the first-pass metabolism and efflux of LVR, peptide prodrugs of LVR [valine–valine–lopinavir (VVL) and glycine–valine–lopinavir (GVL)] were synthesized. Prodrugs were identified with 1 H and 13 C NMR spectra and LC/MS/MS...
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