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. Author manuscript; available in PMC: 2021 Nov 1.
Published in final edited form as: Clin Pharmacokinet. 2020 Nov;59(11):1433–1450. doi: 10.1007/s40262-020-00897-9

Table 4:

Comparison of simulated or predicted and observed PK Parameters

AUC0-t/∞ [mg ·h/L]a
Simulated/
observed (ratio)
Cmax [mg/L]
Simulated/
observed (ratio)
tmax [h]
Simulated/
observed (ratio)
Dolutegravir
Non-pregnant women
 Castellino study [17] 34.0/35.9 (0.95) 2.29/2.53 (0.86) 0.95/0.50 (1.90)
 Dooley study cohort 1 [18] (steady state) 39.0/36.1 (1.08) 2.91/2.65 (1.10) 2.25/1.5 (1.50)
 Dooley study cohort 2 [18] (steady state) 41.1/42.1 (0.98) 2.96/2.91 (1.02) 2.20/2.00 (1.10)
 Ford study [23] (steady state) 63.1/52.5(1. 20) 4.00/3.43 (1.17) 4.25/4.00 (1.06)
 Johnson2014, Cohort 1 (steady state) [24] 65.2/71.9 (0.91) 4.14/4.35 (0.95) 4.30/3.00 (1.43)
 Johnson2014, Cohort2 (steady state) [24] 67.4/71.9 (0.94) 4.30/4.78 (0.90) 4.30/3.50 (1.23)
 Song2012_high_fat [21] 66.1/83.6 (0.79) 2.97/4.19 (0.71) 4.90/5.00 (0.98)
 Song2012_low_fat [21] 59.8/66.7 (0.90) 2.83/3.81 (0.74) 4.00/3.00 (1.33)
 Song2012_moderate_fat [21] 64.7/71.0 (0.91) 2.94/3.86 (0.76) 4.75/4.00 (1.19)
 Song2016_moderate_fat_meal [20] (steady state) 62.2/55.4 (1.12) 3.99/3.83 (1.04) 4.00/3.00 (1.33)
 Song2013 study [19] b 47.2/40.3 (1.17) 1.82/1.90 (0.96) 2.50/3.00 (0.83)
 Weller study [22] 44.1/37.1 (1.19) 1.89/1.84 (1.03) 2.40/2.50 (0.96)
 Wang2019 [25] 63.8/51.62 (1.23) 4.30/3.81(1.13) 4.10/4.00 (1.03)
Pregnant women
 2nd trimester (steady state) 34.70/42.38 (0.82) 2.77/3.00 (0.92) 4.20/2.00 (2.10)
 3rd trimester (steady state) 31.91/47.59 (0.67) 2.57/3.00 (0.86) 4.20/4.00 (1.05)
Raltegravir
Non-pregnant women See OSP GitHub See OSP GitHub See OSP GitHub
 Markowitz2006[75] 8.86/7.96 (1.11) 3.04/2.24 (1.36) 0.80/1.00 (0.80)
 Iwamoto2009[78] 8.66/4.90 (1.77) 3.10/1.28 (2.42) 0.75/1.50 (0.50)
 Rhee2014 [76] 9.13/8.53 (1.07) 3.11/2.22 (1.40) 0.75/2.00 (0.38)
 Wenning2009 [77] 8.99/12.25 (0.73) 3.12/3.82 (0.81) 0.75/1.50 (0.50)
 Brainard2011_fasted b [79] 9.66/6.47 (1.49) 3.42/1.59 (2.15) 0.75/2.00 (0.38)
 Brainard2011_high fat b [79] 8.83/ 11.37 (0.78) 1.48/1.59 (0.93) 2.45/2.00 (1.23)
 Brainard2011_moderate_fat b [79] 8.86/6.44 (1.38) 1.54/0.74 (2.08) 2.20/4.00 (0.55)
 Brainard2011_low_fat b [79] 9.01/3.39 (2.66) 1.76/0.59 (2.98) 1.95/3.50 (0.56)
 Taburet2015_moderate_fat_1 c[80] 8.46/8.24 (1.03) 1.65/2.03 (0.82) 2.20/1.00 (2.20)
 Taburet2015_moderate_fat_2 c [80] 8.95/ 11.00 (0.81) 1.54/2.77 (0.56) 2.20/2.00 (1.10)
Pregnant women
 2nd trimester (steady state) 4.10/3.90 (1.05) 0.834/0.67 (1.22) 2.55/2.00 (1.28)
 3rd trimester (steady state) 3.71/4.44 (0.84) 0.763/0.85 (0.89) 2.50/2.00 (1.25)

Data expressed as geometric mean values unless indicated otherwise.

a

AUC0-t was used in the studies by Dooley et al. [18], Ford et al. [23], Johnson et al. [24], Song et al. [20], Markowitz et al.,[75] Brainard et al.[79] and Taburet et al.[80]; whereas AUC0-∞ was used in the studies by Castellino et al. [17], Song et al. [21], Song et al. [19], Weller et al. [22], Iwamoto et al.[78], Rhee et al.[76] and Wenning et al.[77].

b

Data expressed as arithmetic mean values.

c

Data expressed as median values.

Abbreviations: AUC0-t: area under the concentration-time curve from zero to the time point of the last observed plasma concentration (in case of multiple dose studies, time refers to the time after last dose); AUC0-∞: area under the concentration-time curve from zero to infinity; Cmax: peak plasma concentration; tmax: time at which peak plasma concentration is reached.