Beijing Institute of Liver Disease, Beijing, China ; Beijing Baihuirui Bio-Technologies Inc, Beijing, China.
PLoS One. 2013 Jul 30;8(7):e67606. doi: 10.1371/journal.pone.0067606. Print 2013.
The role of preexisting minority drug-resistance mutations in treatment failure has not been fully understood in chronic hepatitis B patients. To understand mechanisms of drug resistance, we analyzed drug-resistance mutations in 46 treatment-failure patients and in 29 treatment-naïve patients and determined linkage patterns of the drug-resistance mutations in individual viral genomes using a highly sensitive parallel allele-specific sequencing (PASS) method. Lamivudine resistance (LAMr) mutations were predominant in treatment-failure patients, irrespective of the inclusion of LAM in the regimen. The primary LAMr mutations M204V and M204I were detected in 100% and 30% of the treatment-failure patients, respectively. Two secondary LAMr mutations (L180M and V173L) were also found in most treatment-failure patients (87% and 78%, respectively). The linkages containing these three mutations dominated the resistant viruses. Importantly, minority LAMr mutations present in <2% of the viral population were detected in 83% of the treatment-naïve patients. Moreover, the low-frequency same linked LAMr mutations (<0.15%) were detected in 24% of the treatment-naïve patients. Our results demonstrate that the selection of preexisting minority linked LAMr mutations may be an important mechanism for the rapid development of LAM resistance, caution the continuous use of LAM to treat drug-experienced and -naïve hepatitis B patients, and underline the importance of the detection of minority single and linked drug-resistance mutations before initiating antiviral therapy.
在慢性乙型肝炎患者中,先前存在的少数耐药突变在治疗失败中的作用尚未完全阐明。为了了解耐药机制,我们分析了 46 例治疗失败患者和 29 例未治疗患者的耐药突变,并使用高度敏感的平行等位基因特异性测序(PASS)方法确定了个体病毒基因组中耐药突变的连锁模式。拉米夫定耐药(LAMr)突变在治疗失败患者中占主导地位,无论方案中是否包含 LAM。主要的 LAMr 突变 M204V 和 M204I 分别在 100%和 30%的治疗失败患者中被检测到。在大多数治疗失败患者中还发现了两种次要的 LAMr 突变(L180M 和 V173L)(分别为 87%和 78%)。包含这三种突变的连锁在耐药病毒中占主导地位。重要的是,在 83%的未治疗患者中检测到了先前存在的病毒群体中存在的少数 LAMr 突变(<2%)。此外,在 24%的未治疗患者中检测到低频相同连锁的 LAMr 突变(<0.15%)。我们的结果表明,先前存在的少数连锁 LAMr 突变的选择可能是 LAM 耐药迅速发展的一个重要机制,对继续使用 LAM 治疗有经验和无经验的乙型肝炎患者提出了警告,并强调了在开始抗病毒治疗之前检测少数单药和连锁耐药突变的重要性。