Once daily maraviroc 300 mg or 150 mg in combination with ritonavir-boosted darunavir 800/100 mg.
Once daily maraviroc 300 mg or 150 mg in combination with ritonavir-boosted darunavir 800/100 mg.
复制标题
每天一次，马拉韦罗 300 毫克或 150 毫克，与利托那韦增强的达芦那韦 800/100 毫克组合。
DOI：
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发表时间：
2012
影响因子：
5.2
通讯作者：
Stephen Taylor
中科院分区：
文献类型：
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作者：
C. Okoli;M. Siccardi;Sathish Thomas;N. Dufty;Kirstin Khonyongwa;J. Ainsworth;John Watson;Roseanne Cook;K. Gandhi;G. Hickinbottom;A. Owen;Stephen Taylor
目标
描述马拉韦罗150或300毫克每日一次与达鲁那韦/利托那韦800/100毫克配伍的药代动力学。
方法
对服用马拉韦罗的HIV感染者的病例进行了回顾。接受马拉韦罗治疗至少5周的患者分为：(I)每日两次服用300毫克马拉韦罗，同时服用替诺福韦245毫克/恩曲他滨200毫克；(Ii)每日服用马拉韦罗300毫克，每日服用达鲁那韦/利托那韦800/100毫克；(Iii)每日服用马拉韦罗150毫克，每日服用达鲁那韦/利托那韦800/100毫克。分别于服药后2、12、24小时采集C(谷值)和C(峰值)数据。
结果
研究对象为66名患者，共提供115份样本。每日服用300 mg马拉韦罗与替诺福韦245 mg/200 mg恩曲他滨(n=9)，每日服用300 mg马拉韦罗与达鲁那韦/利托那韦(n=29)，中位数(IQR)C(峰值)分别为378(350-640)ng/mL，728(378-935)ng/mL，每日服用150 mg马拉韦克(n=2；P=0.24)。达鲁那韦/利托那韦(n=34)、替诺福韦/恩曲他滨(n=12)、马拉韦罗组(n=34)和马拉韦罗组(n=17；P=0.001)的中位数(IQR)C(谷值)分别为46(33-61)ng/mL和43(35-55)ng/mL。黑人患者(n=34)马拉韦罗C谷值为61(45~110)ng/m L，白人患者(n=29)为49(42~70)ng/m L(P=0.04)。黑人患者(n=20)C峰值为800(397~1060)ng/mL，白人患者(n=20)C峰值为387(336~723)ng/mL，P=0.02。
结论
与马拉韦罗300毫克与替诺福韦245毫克/恩曲他滨200毫克相比，每天服用一次马拉韦罗300毫克和800/100毫克达鲁那韦/利托那韦的耐受性很好，具有良好的药代动力学。与白人患者相比，黑人患者的C(谷值)和C(峰值)分别高出24%和107%。
OBJECTIVES
To describe the pharmacokinetics of maraviroc when dosed at 150 or 300 mg once daily with 800/100 mg of darunavir/ritonavir.
METHODS
A retrospective case-note review of HIV-infected adults taking maraviroc was conducted. Patients on a maraviroc-based regimen for a minimum of 5 weeks were grouped as receiving: (i) 300 mg of maraviroc twice daily with 245 mg of tenofovir/200 mg of emtricitabine; (ii) 300 mg of maraviroc once daily with 800/100 mg of darunavir/ritonavir once daily; and (iii) 150 mg of maraviroc once daily with 800/100 mg of darunavir/ritonavir once daily. C(trough) and C(peak) data were collected at 2, 12 or 24 h post-dose.
RESULTS
Sixty-six patients were included, providing 115 samples. The median (IQR) C(peak) was 378 (350-640) ng/mL for 300 mg of maraviroc twice daily with 245 mg of tenofovir/200 mg of emtricitabine (n=9), 728 (378-935) ng/mL for 300 mg of maraviroc once daily with darunavir/ritonavir (n=29) and 364 (104-624) ng/mL for 150 mg of maraviroc once daily with darunavir/ritonavir (n=2; P=0.24). The median (IQR) C(trough) was 46 (33-61) ng/mL for 300 mg of maraviroc twice daily with 245 mg of tenofovir/200 mg of emtricitabine (n=12), 70 (49-97) ng/mL for 300 mg of maraviroc once daily with darunavir/ritonavir (n=34) and 43 (35-55) ng/mL for 150 mg of maraviroc once daily with darunavir/ritonavir (n=17; P=0.001). The maraviroc C(trough) in black patients (n=34) was 61 (45-110) ng/mL and in white patients (n=29) it was 49 (42-70) ng/mL (P=0.04). The C(peak) in black patients (n=20) was 800 (397-1060) ng/mL versus 387 (336-723) ng/mL in white patients (n=20; P=0.02).
CONCLUSIONS
Once daily coadministration of 300 mg of maraviroc with 800/100 mg of darunavir/ritonavir was well tolerated and had favourable pharmacokinetics when compared with 300 mg of maraviroc twice daily with 245 mg of tenofovir/200 mg of emtricitabine. A 24% higher C(trough) and 107% higher C(peak) was seen in black patients compared with white patients.