Effects of rifampicin, CYP2B6 and ABCB1 polymorphisms on efavirenz plasma concentration in Chinese patients living with HIV and tuberculosis. (January 2023)

• Record Type: Journal Article
• Authors: Zhang, Li; Meng, Xianmin; Dong, Ping; Qi, Tangkai; Liu, Li; Wang, Bin
• Is Part Of: International journal of STD & AIDS. Volume 34:Number 1(2023)
• Page Start: 37
• Page End: 47
• Publication Date: 2023-01
• Subjects: Efavirenz -- cytochrome P450 2B6 -- ATP-binding cassette sub-family B member 1 -- rifampicin -- human immunodeficiency virus -- plasma concentration; Sexually transmitted diseases -- Periodicals; AIDS (Disease) -- Periodicals; 616.951
• DOI: 10.1177/09564624221134137
• Languages: English
• ISSNs: 0956-4624

Abstract

Background: Tuberculosis (TB) is the leading opportunistic infection of people living with human immunodeficiency virus (HIV; PLWH). Cytochrome P450 (CYP) 2B6 and ATP-binding cassette sub-family B member 1 ( ABCB1 ) are involved in the metabolism and transportation of efavirenz. The study was aimed to investigate the effects of rifampicin, CYP2B6 and ABCB1 polymorphisms on efavirenz exposure in Chinese PLWH co-infected with TB. Method: PLWH were screened according to inclusion and exclusion criteria and divided into HIV group and HIV/TB group. Efavirenz plasma concentration (C0 ) was determined, dose-adjusted concentration (C0 /D) was calculated, and genotypes of CYP2B6 516G>T, 785A>G, and ABCB1 2677G>T, 3435C>T were analyzed. Results: 252 PLWH were enrolled, including 75 co-infected with TB and concomitant with rifampicin. Efavirenz C0 and C0 /D were both higher in HIV group (1.94 μg/mL, 0.2007 (μg/ml)/(mg/kg/d)) compared with HIV/TB group (1.52 μg/mL, 0.1557 (μg/ml)/(mg/kg/d)) ( p = .001). Efavirenz C0 /D was significantly higher in patients with variant genotypes of CYP2B6 516G>T and 785A>G ( p <.001), and was significantly lower in HIV/TB group compared with HIV group among patients with CYP2B6 516 GG, TT, and 785 AA, AG genotypes ( p < .05). Conclusion: Efavirenz exposure is reduced by co-administration with rifampicin, and related to genetic polymorphisms of CYP2B6.