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Genome-wide Association Study of Methotrexate-Induced Liver Injury in Rheumatoid Arthritis Patients

  • Frank Eektimmerman
  • , Jesse J. Swen
  • , Alfons A. den Broeder
  • , Johanna M. W. Hazes
  • , Fina S. Kurreeman
  • , Suzanne M. M. Verstappen
  • , Nisha Nair
  • , Andrzej Pawlik
  • , Mike T. Nurmohamed
  • , Vita Dolžan
  • , Stefan Böhringer
  • , Cornelia F. Allaart
  • , Henk-Jan Guchelaar*
  • *Corresponding author for this work
  • Leiden University
  • Canisius Wilhelmina Hospital
  • St. Martin Clinic
  • Erasmus University Rotterdam
  • University of Manchester
  • Manchester University NHS Foundation Trust
  • Pomeranian Medical University in Szczecin
  • Rheumatology Amsterdam Rheumatology and Immunology Center
  • University of Ljubljana

Research output: Contribution to journalArticleAcademicpeer-review

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Abstract

Hepatotoxicity is a serious adverse drug reaction related to methotrexate (MTX). However, the cause of drug-induced liver injury (DILI) is still unclear and unpredictable. Genetic risk factors may predispose for MTX-DILI. Therefore, we conducted a nested case-control genome-wide association study to explore genetic risk factors associated with MTX-DILI. Seven international groups contributed blood samples and data of patients with rheumatoid arthritis who used MTX. MTX-DILI was defined as an alanine aminotransferase (ALT) level of at least three times the upper limit of normal (ULN), to increase contrast controls ALT levels did not raise above two times the ULN. Per study site, control subjects and patients with MTX-DILI (ratio 3:1) were matched for age, gender, and duration of MTX use. Patients were genotyped using Illumina GSA MD-24v1-0 and data were imputed using the 1000 Genomes reference panel. Single-nucleotide polymorphisms (SNPs) were analyzed using an additive genetic model, corrected for sex, country, and age. A P-value of ≤ 5 × 10−8 was considered significant, whereas a P-value of ≤ 5 × 10−6 was considered suggestive. A total of 108 MTX-DILI cases and 311 controls were included for association analysis. None of the SNPs were significantly associated with MTX-DILI. However, we found seven suggestive genetic variants associated with MTX-DILI (P-values 7.43 × 10−8 to 4.86 × 10−6). Of those, five SNPs were in the intronic protein-coding regions of FTCDNL1, BCOR, FGF14, RBMS3, and PFDN4/DOK5. Investigation of candidates SPATA9 (rs72783407), PLCG2 (rs60427389), RAVER2 (rs72675408), JAK1 (rs72675451), PTPN2 (rs2476601), MTHFR C677T (rs1801133), and into the HLA region did not show significant findings. No genetic variants associated with MTX-DILI were found, whereas suggestive SNPs need further investigation.
Original languageEnglish
Pages (from-to)916-923
Number of pages8
JournalClinical pharmacology and therapeutics
Volume113
Issue number4
Early online date2023
DOIs
Publication statusPublished - Apr 2023

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