Interleukin-6 blockade raises LDL via reduced catabolism rather than via increased synthesis: a cytokine-specific mechanism for cholesterol changes in rheumatoid arthritis

Ann Rheum Dis. 2017 Nov;76(11):1949-1952. doi: 10.1136/annrheumdis-2017-211708. Epub 2017 Sep 15.

Abstract

Objectives: Patients with rheumatoid arthritis (RA) have reduced serum low-density lipoprotein cholesterol (LDL-c), which increases following therapeutic IL-6 blockade. We aimed to define the metabolic pathways underlying these lipid changes.

Methods: In the KALIBRA study, lipoprotein kinetic studies were performed on 11 patients with severe active RA at baseline and following three intravenous infusions of the IL-6R blocker tocilizumab. The primary outcome measure was the fractional catabolic rate (FCR) of LDL.

Results: Serum total cholesterol (4.8 vs 5.7 mmol/L, p=0.003), LDL-c (2.9 vs 3.4 mmol/L, p=0.014) and high-density lipoprotein cholesterol (1.23 vs 1.52 mmol/L, p=0.006) increased following tocilizumab therapy. The LDL FCR fell from a state of hypercatabolism to a value approximating that of the normal population (0.53 vs 0.27 pools/day, p=0.006). Changes in FCR correlated tightly with changes in serum LDL-c and C-reactive protein but not Clinical Disease Activity Index.

Conclusions: Patients with RA have low serum LDL-c due to hypercatabolism of LDL particles. IL-6 blockade normalises this catabolism in a manner associating with the acute phase response (and thus hepatic IL-6 signalling) but not with RA disease activity as measured clinically. We demonstrate that IL-6 is one of the key drivers of inflammation-driven dyslipidaemia.

Keywords: cardiovascular disease; cytokines; lipids; rheumatoid arthritis.

Publication types

  • Evaluation Study

MeSH terms

  • Antibodies, Monoclonal, Humanized / pharmacokinetics*
  • Antirheumatic Agents / pharmacokinetics*
  • Arthritis, Rheumatoid / blood*
  • Arthritis, Rheumatoid / drug therapy*
  • C-Reactive Protein / analysis
  • Cholesterol / blood
  • Cholesterol, HDL / blood
  • Cholesterol, LDL / blood*
  • Female
  • Humans
  • Interleukin-6 / antagonists & inhibitors
  • Interleukin-6 / metabolism*
  • Kinetics
  • Male
  • Middle Aged
  • Severity of Illness Index
  • Treatment Outcome

Substances

  • Antibodies, Monoclonal, Humanized
  • Antirheumatic Agents
  • Cholesterol, HDL
  • Cholesterol, LDL
  • IL6 protein, human
  • Interleukin-6
  • C-Reactive Protein
  • Cholesterol
  • tocilizumab