Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. We analyzed the genotypes of CYP2B6 and their contribution to plasma EFV concentrations in 35 EFV-treated patients in International Medical Center of Japan. The mean plasma EFV concentration of patients with CYP2B6 *6/*6 (Q172H and K262R) (25.4+/-7.5 microM, +/-SD, n = 2) was significantly higher than that of patients with genotypes *6 heterozygote (9.9+/-3.3 microM, n = 10) or without alleles *6 (8.0+/-2.6 microM, n = 23) (p < 0.0001). To confirm our result, we further analyzed nine patients (three with high EFV concentrations and arbitrarily selected six with normal EFV concentrations) treated in Osaka National Hospital, and it resulted that the only three patients with the high concentrations were the *6/*6 holder. EFV dose could be decreased in those patients harboring the genotype to reduce toxicity with compromising potency, representing the first step of the Tailor-Made therapy of HIV-1 infection.
Biochemical and biophysical research communications. 2004 Jul 9;319(4):1322-6. doi: 10.1016/j.bbrc.2004.05.116 1959
Homozygous CYP2B6 *6 (Q172H and K262R) correlates with high plasma efavirenz concentrations in HIV-1 patients treated with standard efavirenz-containing regimens
人类CYP2B6*6（Q172H和K262R）纯合子与标准依非韦伦方案治疗的HIV-1患者中高水平血浆依非韦伦浓度相关 翻译改进
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DOI: 10.1016/j.bbrc.2004.05.116 PMID: 15194512
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Keywords：cyp2b6 genotype; efavirenz concentration; hiv-1patients
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期刊名：BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
缩写：BIOCHEM BIOPH RES CO
ISSN：0006-291X
e-ISSN：1090-2104
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