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. Author manuscript; available in PMC: 2019 May 30.
Published in final edited form as: Clin Infect Dis. 2015 Apr 16;61(3):453–463. doi: 10.1093/cid/civ317

Table 3. EFV pharmacokinetic parameters in plasma and breast milk and breastfed infants’ exposure.

Pooled CYP2B6 516GG CYP2B6 516GT CYP2B6 516TT
Preliminary phase pharmacokinetic data n = 117 n = 42 n = 52 n = 23

Maternal plasma EFV conc. (ng/mL) 2310 (632-8880) 1660 (632-3610) 2390 (951-8880) 5400 (1920-8110)
Breast milk EFV conc. (ng/mL) 2280 (475-10800) 1610 (475-5580) 2370 (713-10300) 4070 (995-10800)
Infant plasma EFV conc. (ng/mL) 173 (46.0-4630) 124 (46.0-4630) 164 (48.5-2150) 333 (75.5-1590)

Intensive pharmacokinetic parameters n = 29 n = 10 n = 11 n = 8

Plasma
Cl/F (L/h)a 9.89 (3.39-22.4) 12.2 (9.37-22.4) 10.0 (4.71-20.7) 4.64 (3.39-5.35)
AUC0-24 (ng.h/mL)a 60700 (26800-177000) 49400 (26800-64000) 59700 (29000-128000) 130000 (112000-177000)
Cmax (ng/mL)a 4630 (2050-9760) 3220 (2310-4630) 4750 (2050-6780) 6940 (5560-9760)
Cmin (ng/mL)a 2030 (755-6740) 1640 (861-2310) 1580 (755-4860) 5150 (3830-6740)
Breast milk
AUC0-24 (ng.h/mL)b 68500 (26300-257000) 55000 (29200-105000) 60600 (26300-206000) 105000 (68100-257000)
Cmax (ng/mL)c 5390 (1430-18400) 4020 (2400-8450) 4540 (1430-9220) 8920 (5810-18400)
Cmin (ng/mL)d 1680 (316-9570) 1120 (534-2430) 1500 (316-6070) 2480 (1500-9570)
Time averaged M/P conc. ratio 1.10 (0.57-1.71) 1.22 (0.61-1.71) 1.08 (0.57-1.57) 0.98 (0.59-1.66)
M/P AUC0-24 ratio 1.13 (0.50-1.93) 1.23 (0.71-1.93) 1.18 (0.73-1.73) 0.95 (0.57-1.66)
Infant exposure
Average infant EFV dose (µg/kg/day) 428 (164-1610) 344 (182-656) 379 (164-1290) 656 (426-1610)
Maximum infant EFV dose (µg/kg/day) 809 (215-2760) 603 (360-1270) 681 (215-1380) 1340 (872-2760)
Average EIpaediatrice (%) 2.14 (0.82-8.05) 1.72 (0.91-3.28) 1.90 (0.82-6.45) 3.28 (2.13-8.05)
Maximum EIpaediatrice (%) 4.05 (1.08-13.8) 3.02 (1.80-6.35) 3.41 (1.08-6.90) 6.70 (4.36-13.8)
EImaternale (%) 7.69 (2.04-26.2) 5.73 (3.42-12.1) 6.47 (2.04-13.1) 12.7 (8.28-26.2)
Infant plasma EFV conc. 1f(ng/mL) 173 (27.2-1590) 166.10 (27.3-208) 88.53 (37.7-273) 293 (103-1590)
Infant plasma EFV conc. 2f (ng/mL) 146 (29.9-1130) 133.54 (30.0-223) 85.83 (45.2-313) 342 (113-1130)

Values are presented as median (range).

a, b and c: Significant differences between genotype groups (Kruskal-Wallis test) at 0.001, 0.05, 0.01 and levels, respectively

d

no significant difference between genotype groups (Kruskal-Wallis test)

e

EIpaediatric and EImaternal represent paediatric and maternal dose weight-adjusted exposure indices, respectively (average EIpaediatric was calculated by replacing InfantDosemax with InfantDoseavg in equation 3)

f

Infant plasma EFV conc. 1 and 2 represent infant plasma concentrations 2 h and 8 h after maternal dose, respectively.