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. 2015 Jun 18;10(6):e0130277. doi: 10.1371/journal.pone.0130277

Table 1. Blood levels of various NNRTIs.

Drug (in vitro EC 50) Author Daily Dose Limitations Measured after intake Measured samples C mean (ng/ml) C max (ng/ml) Number of blood levels > EC50 Ratio EC50 / C mean
EFV Manosuthi 2005 [19] 1x600mg concurrent Rifampicin 12h 42 3020 12210 1 (2.4%) 3.3
(31.5μmol/l = 1x800mg concurrent Rifampicin 12h 42 3390 21310 6 (14.3%) 2.9
9944ng/ml) Marzolini 2001 [20] 1x600mg 14h 171 2188 15230 6 (3.5%) 4.5
Gutierrez 2005 [21] 1x600mg 12h 58 4120 12590 3 (5.2%) 2.4
NVP Ratanasuwan 2012 [22] 2x200mg Post-dose 108 6671 ~25000 0 9.6
(239μmol/l = Nafrialdi 2012 [23] 2x200mg 24 7950 ~15000 0 8.0
63786ng/ml) Wang 2011 [17] 2x200mg CR group 2h 87 6850 ~15000 0 9.3
2x200mg CR group 12h 34 5180 12.3
ETR DeJesus 2010 [24] 1x400mg 4h 20 801 1410 0 48.4
(89.0μmol/l = Kakuda 2009 [25] 2x800mg early formulation 3h 15 935 41.5
38740ng/ml) Gruzdev 2003 [26] 2x900mg early formulation 3h 12 418 92.7
LSV Vourvahis 2012 [27] 1x2400mg healthy volunteers 4h 48 1727 ~3000 0 97.6
(543μmol/l = Vourvahis 2010 [28] 1x750mg healthy volunteers 4h 14 1524 111
168523ng/ml) Vourvahis 2012 [29] 2x1000mg healthy volunteers 4h 16 1328 127
DLV (171μmol/l Justesen 2004 [30] 2x1000mg healthy volunteers 1h 3 14890 24840 0 5.2
= 78072ng/ml) Cheng 1997 [31] 3x400mg 1h 8 12144 6.4
RPV (24.4μmol/l Goebel 2006 [32] 1x150mg 4h 9 922 9.7
= 8941ng/ml) Ford 2013 [33] 1x25mg healthy volunteers 4h 16 148 60.4

Several studies about blood concentrations of NNRTIs in patients are compared to the in vitro EC50 of cytotoxicity against cancer cells. (C mean: mean of all measured blood concentrations in a cohort; C max: highest blood concentration measured in one patient in a cohort)