Infectious Diseases Department, Hospital Carlos III, Madrid, Spain.
AIDS. 2013 Jan 2;27(1):81-5. doi: 10.1097/QAD.0b013e3283584500.
Rilpivirine (RPV) is the latest approved nonnucleoside reverse transcriptase inhibitor (NNRTI). It displays in-vitro activity extending over other NNRTI-resistant HIV strains. There is scarce information about the rate of RPV resistance-associated mutations (RAMs) in patients failing other NNRTIs.
RPV RAMs were examined in plasma samples collected from HIV patients that had recently failed NNRTI-based regimens at 22 clinics in Spain.
Resistance tests from a total of 1064 patients failing efavirenz (EFV) (54.5%), nevirapine (NVP) (40%) or etravirine (ETR) (5.5%) were examined. The prevalence of RPV RAMs was K101E (9.1%), K101P (1.4%), E138A (3.9%), E138G (0.3%), E138K (0.3%), E138Q (0.8%), V179L (0.2%), Y181C (21.8%), Y181I (0.5%), Y181V (0.2%), H221Y (8.3%), F227C (0.1%) and M230L (1.5%). K101E/M184I was seen in 1%. E138K/M184I were absent. Mutations L100I and V108I were significantly more frequent in patients failing EFV than NVP (7.9 vs. 0.2 and 12.2 vs. 7.3%, respectively). Conversely, Y181C, Y181I, V106A, H221Y and F227L were more prevalent following NVP than EFV failures. Using the Spanish resistance interpretation algorithm, 206 genotypes (19.3%) from patients failing NNRTI (NVP 52%, EFV 40.8% and ETR 7.8%) were considered as RPV resistant. In patients with ETR failure, cross-resistance to RPV was seen in 27.6%, mainly as result of Y181C (81.3%), V179I (43.8%), V90I (31.3%) and V108I (18.8%).
RPV resistance is overall recognized in nearly 20% of patients failing other NNRTIs. It is more common following ETR (27.6%) or NVP (25%) failures than EFV (14.5%). E138 mutants are rarely seen in this context.
利匹韦林（RPV）是最新批准的非核苷类逆转录酶抑制剂（NNRTI）。它在体外具有针对其他 NNRTI 耐药 HIV 株的活性。关于其他 NNRTI 失败患者中 RPV 耐药相关突变（RAMs）的发生率，信息很少。
在西班牙 22 家诊所收集了最近 NNRTI 方案失败的 HIV 患者的血浆样本，对 RPV RAMs 进行了检测。
对来自共 1064 例失败的依非韦伦（EFV）（54.5%）、奈韦拉平（NVP）（40%）或依曲韦林（ETR）（5.5%）的患者的耐药性检测结果进行了检查。检测到 RPV RAMs 为 K101E（9.1%）、K101P（1.4%）、E138A（3.9%）、E138G（0.3%）、E138K（0.3%）、E138Q（0.8%）、V179L（0.2%）、Y181C（21.8%）、Y181I（0.5%）、Y181V（0.2%）、H221Y（8.3%）、F227C（0.1%）和 M230L（1.5%）。检测到 1%的 K101E/M184I。未检测到 E138K/M184I。与 NVP 相比，L100I 和 V108I 在 EFV 失败患者中更为常见（分别为 7.9%比 0.2%和 12.2%比 7.3%）。相反，与 EFV 失败相比，Y181C、Y181I、V106A、H221Y 和 F227L 在 NVP 失败患者中更为常见。使用西班牙耐药性解释算法，对来自 NNRTI（NVP 52%、EFV 40.8%和 ETR 7.8%）失败的 206 种基因型（19.3%），认为对 RPV 具有耐药性。在 ETR 失败的患者中，对 RPV 的交叉耐药性见于 27.6%，主要是由于 Y181C（81.3%）、V179I（43.8%）、V90I（31.3%）和 V108I（18.8%）。
在其他 NNRTI 失败的患者中，总体上发现 RPV 耐药率接近 20%。与 EFV（14.5%）相比，它在 ETR（27.6%）或 NVP（25%）失败中更为常见。在此背景下，很少检测到 E138 突变。
