Rhee Soo-Yon, Boehm Michael, Tarasova Olga, Di Teodoro Giulia, Abecasis Ana B, Sönnerborg Anders, Bailey Alexander J, Kireev Dmitry, Zazzi Maurizio, Shafer Robert W
Department of Medicine, Stanford University, Stanford, CA 94305, USA.
Institute of Virology, Faculty of Medicine and University Hospital of Cologne, University of Cologne, 50935 Cologne, Germany.
Pathogens. 2022 May 5;11(5):546. doi: 10.3390/pathogens11050546.
Ritonavir-boosted atazanavir is an option for second-line therapy in low- and middle-income countries (LMICs). We analyzed publicly available HIV-1 protease sequences from previously PI-naïve patients with virological failure (VF) following treatment with atazanavir. Overall, 1497 patient sequences were identified, including 740 reported in 27 published studies and 757 from datasets assembled for this analysis. A total of 63% of patients received boosted atazanavir. A total of 38% had non-subtype B viruses. A total of 264 (18%) sequences had a PI drug-resistance mutation (DRM) defined as having a Stanford HIV Drug Resistance Database mutation penalty score. Among sequences with a DRM, nine major DRMs had a prevalence >5%: I50L (34%), M46I (33%), V82A (22%), L90M (19%), I54V (16%), N88S (10%), M46L (8%), V32I (6%), and I84V (6%). Common accessory DRMs were L33F (21%), Q58E (16%), K20T (14%), G73S (12%), L10F (10%), F53L (10%), K43T (9%), and L24I (6%). A novel nonpolymorphic mutation, L89T occurred in 8.4% of non-subtype B, but in only 0.4% of subtype B sequences. The 264 sequences included 3 (1.1%) interpreted as causing high-level, 14 (5.3%) as causing intermediate, and 27 (10.2%) as causing low-level darunavir resistance. Atazanavir selects for nine major and eight accessory DRMs, and one novel nonpolymorphic mutation occurring primarily in non-B sequences. Atazanavir-selected mutations confer low-levels of darunavir cross resistance. Clinical studies, however, are required to determine the optimal boosted PI to use for second-line and potentially later line therapy in LMICs.
利托那韦增强的阿扎那韦是低收入和中等收入国家(LMICs)二线治疗的一种选择。我们分析了先前接受阿扎那韦治疗后病毒学失败(VF)的初治患者公开可用的HIV-1蛋白酶序列。总体而言,共鉴定出1497例患者的序列,其中包括27项已发表研究中报告的740例以及为本分析汇总的数据集里的757例。共有63%的患者接受了增强的阿扎那韦治疗。共有38%的患者感染的是非B亚型病毒。共有264条(18%)序列具有蛋白酶抑制剂耐药性突变(DRM),定义为具有斯坦福HIV耐药数据库突变惩罚分数。在具有DRM的序列中,9种主要DRM的流行率>5%:I50L(34%)、M46I(33%)、V82A(22%)、L90M(19%)、I54V(16%)、N88S(10%)、M46L(8%)、V32I(6%)和I84V(6%)。常见的辅助DRM有L33F(21%)、Q58E(16%)、K20T(14%)、G73S(12%)、L10F(10%)、F53L(10%)、K43T(9%)和L24I(6%)。一种新的非多态性突变L89T出现在8.4%的非B亚型序列中,但仅出现在0.4%的B亚型序列中。这264条序列中,有3条(1.1%)被解释为导致高水平、14条(5.3%)导致中等水平、27条(10.2%)导致低水平的达芦那韦耐药。阿扎那韦会筛选出9种主要和8种辅助DRM,以及一种主要出现在非B亚型序列中的新的非多态性突变。阿扎那韦选择的突变导致低水平的达芦那韦交叉耐药。然而,需要进行临床研究以确定在LMICs中用于二线及可能后续治疗的最佳增强蛋白酶抑制剂。