title: Drug susceptibility to etravirine and darunavir among Human Immunodeficiency Virus Type 1-derived pseudoviruses in treatment-experienced patients with HIV/AIDS in South Korea.
abstract: BACKGROUND
  In South Korea, about 20 types of antiretroviral drugs are used in the treatment of patients with human immunodeficiency virus/acquired immune deficiency syndrome. Since 2010, raltegravir, etravirine, and darunavir have been spotlighted as new drugs for highly active antiretroviral therapy (HAART)-experienced adults with resistant HIV-1 in South Korea. In this study, we investigated potential susceptibility of pseudoviruses derived from treatment-experienced Korean patients to etravirine vs efavirenz and to darunavir vs amprenavir and indinavir using a modified single-round assay.
  
  
  METHODS
  Pseudoviruses derived from nine treatment-experienced patients infected with HIV-1 were investigated by comparison with the wild-type strain pNL4-3. The 50% inhibitory concentration (IC50) values were calculated and drug susceptibility was compared. The intensity of genotypic drug resistance was classified based on the 'SIR' interpretation of the Stanford data base.
  
  
  RESULTS
  Drug susceptibility was generally higher for etravirine and darunavir compared with efavirenz, amprenavir, and indinavir in pseudoviruses derived from treatment-experienced patients. Pseudoviruses derived from patients KRB4025 and KRB8014, who exhibited long-term use of protease inhibitors, showed an outside of tested drug concentration, especially for amprenavir and indinavir. However, they exhibited a lower fold-change in resistance to darunavir.
  
  
  CONCLUSIONS
  Etravirine and darunavir have been used in HAART since 2010 in South Korea. Therefore, these antiretroviral drugs together with other newly introduced antiretroviral drugs are interesting for the optimal treatment of patients with treatment failure. This study may help to find a more effective HAART in the case of HIV-1 infected patients that have difficulty being treated.
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. jh5246@korea.kr.
authors: Oh-Kyung
authors: OK
authors: Kwon
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. sungskim@korea.kr.
authors: Sung Soon
authors: SS
authors: Kim
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. jerhee001@korea.kr.
authors: Jee Eun
authors: JE
authors: Rhee
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. keemeekyung@gmail.com.
authors: Mee-Kyung
authors: MK
authors: Kee
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. mina0827@korea.kr.
authors: Mina
authors: M
authors: Park
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. ohyell0630@korea.kr.
authors: Hye-Ri
authors: HR
authors: Oh
authors: Department of Immunology and Pathology, Division of AIDS, Korea National Institute of Health, Osong, Republic of Korea. juyeon.choi.hb@gmail.com.
authors: Ju-Yeon
authors: JY
authors: Choi
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy / Q000821:virology*; D019380:Anti-HIV Agents / Q000494:pharmacology* / Q000627:therapeutic use; D023241:Antiretroviral Therapy, Highly Active; D000069454:Darunavir / Q000494:pharmacology* / Q000627:therapeutic use; D024882:Drug Resistance, Viral; D005838:Genotype; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology*; D015497:HIV-1 / Q000235:genetics*; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D009154:Mutation; D009570:Nitriles; D010641:Phenotype; D011498:Protein Precursors / Q000235:genetics; D011724:Pyridazines / Q000494:pharmacology* / Q000627:therapeutic use; D011743:Pyrimidines; D011995:Recombination, Genetic; D056910:Republic of Korea; D054301:gag Gene Products, Human Immunodeficiency Virus / Q000235:genetics; D054302:pol Gene Products, Human Immunodeficiency Virus / Q000235:genetics
chemical_list: D019380:Anti-HIV Agents; D009570:Nitriles; D011498:Protein Precursors; D011724:Pyridazines; D011743:Pyrimidines; D054301:gag Gene Products, Human Immunodeficiency Virus; D054302:pol Gene Products, Human Immunodeficiency Virus; C091950:pr160 gag-pol precursor protein, Human immunodeficiency virus 1; C451734:etravirine; D000069454:Darunavir