Applications
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HIV with multiple mutations was markedly less resistant to Lopinavir than to Ritonavir. Although the activity of Lopinavir declined significantly against the multiply mutated strains compared with its activity against the baseline strains, the extent of the decline was substantially less than that of Ritonavir. Furthermore, the EC50 value of Lopinavir against HIV with multiple mutations was 10-fold lower than that of Ritonavir.
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Applications
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The Cmax and oral bioavailability of Lopinavir in rats were 0.8 μg/mL and 25%, respectively. At 6th hr, the plasma level of Lopinavir declined below the level of quantitation (0.01 μg/mL). However, co-administration of Lopinavir with Ritonavir (10 mg/kg) maintained the concentrations of Lopinavir in excess of 3 μg/mL with low variability. In addition, the area under the plasma concentration-time curve from 0 ~ 8 hrs for Lopinavir increased 14-fold due to Ritonavir co-administration.
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References:
[1]. Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, McDonald E, Saldivar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.
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