Brief Report: High Peak Level of Plasma Raltegravir Concentration in Patients With ABCB1 and ABCG2 Genetic Variants. (1st May 2016)

• Record Type: Journal Article
• Authors: Tsuchiya, Kiyoto; Hayashida, Tsunefusa; Hamada, Akinobu; Oka, Shinichi; Gatanaga, Hiroyuki
• Is Part Of: Journal of acquired immune deficiency syndromes. Volume 72:Number 1(2016)
• Publication Date: 2016-05-01
• Subjects: antiretroviral therapy -- raltegravir -- plasma concentrations -- ATP-binding cassette transporter B1 -- ATP-binding cassette transporter G2; AIDS (Disease) -- Periodicals; Acquired Immunodeficiency Syndrome -- Periodicals; AIDS (Disease); Periodicals; 616.9792005
• DOI: 10.1097/QAI.0000000000000893
• Languages: English
• ISSNs: 1525-4135

Abstract

Abstract : Abstract: Raltegravir was recently identified to be a substrate of ATP-binding cassette transporter B1 (ABCB1) and G2 (ABCG2), which are efflux transporters and expressed in the intestines. We analyzed the relations between plasma raltegravir concentrations and single nucleotide polymorphism of ABCB1 and ABCG2 genes. The peak plasma concentration of raltegravir was significantly higher in the patients with ABCB1 4036 AG/GG and ABCG2 421 CA/AA than in other genotype holders ( P = 0.0052), though no difference was identified in trough raltegravir concentrations, which may be explained by reduced expression of efflux transporters in intestine by these genetic variants.