An Animal Model of Abacavir-Induced HLA-Mediated Liver Injury

Toxicol Sci. 2018 Apr 1;162(2):713-723. doi: 10.1093/toxsci/kfy001.

Abstract

Genome-wide association studies indicate that several idiosyncratic adverse drug reactions are highly associated with specific human leukocyte antigen (HLA) alleles. For instance, abacavir, a human immunodeficiency virus reverse transcriptase inhibitor, induces multiorgan toxicity exclusively in patients carrying the HLA-B*57:01 allele. However, the underlying mechanism is unclear due to a lack of appropriate animal models. Previously, we developed HLA-B*57:01 transgenic mice and found that topical application of abacavir to the ears induced proliferation of CD8+ lymphocytes in local lymph nodes. Here, we attempted to reproduce abacavir-induced liver injury in these mice. However, oral administration of abacavir alone to HLA-B*57:01 transgenic mice did not increase levels of the liver injury marker alanine aminotransferase. Considering the importance of innate immune activation in mouse liver, we treated mice with CpG oligodeoxynucleotide, a toll-like receptor 9 agonist, plus abacavir. This resulted in a marked increase in alanine aminotransferase, pathological changes in liver, increased numbers of activated CD8+ T cells, and tissue infiltration by immune cells exclusively in HLA-B*57:01 transgenic mice. These results indicate that CpG oligodeoxynucleotide-induced inflammatory reactions and/or innate immune activation are necessary for abacavir-induced HLA-mediated liver injury characterized by infiltration of CD8+ T cells. Thus, we developed the first mouse model of HLA-mediated abacavir-induced idiosyncratic liver injury. Further investigation will show that the proposed HLA-mediated liver injury model can be applied to other combinations of drugs and HLA types, thereby improving drug development and contributing to the development of personalized medicine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine Transaminase / blood
  • Animals
  • CD8-Positive T-Lymphocytes / drug effects
  • CD8-Positive T-Lymphocytes / immunology
  • Chemical and Drug Induced Liver Injury / etiology
  • Chemical and Drug Induced Liver Injury / genetics
  • Chemical and Drug Induced Liver Injury / immunology*
  • Chemical and Drug Induced Liver Injury / pathology
  • Dideoxynucleosides / toxicity*
  • Disease Models, Animal*
  • HLA-B Antigens / genetics*
  • Hepatocytes / drug effects
  • Hepatocytes / immunology
  • Hepatocytes / pathology
  • Immunity, Innate / drug effects
  • Immunity, Innate / genetics
  • Liver / drug effects*
  • Liver / immunology
  • Liver / pathology
  • Male
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Oligodeoxyribonucleotides / pharmacology
  • Reverse Transcriptase Inhibitors / toxicity*
  • Toll-Like Receptor 9 / agonists

Substances

  • CpG ODN 1826
  • Dideoxynucleosides
  • HLA-B Antigens
  • HLA-B*57:01 antigen
  • Oligodeoxyribonucleotides
  • Reverse Transcriptase Inhibitors
  • Tlr9 protein, mouse
  • Toll-Like Receptor 9
  • Alanine Transaminase
  • abacavir