The effect of BMS-582949, a P38 mitogen-activated protein kinase (P38 MAPK) inhibitor on arterial inflammation: a multicenter FDG-PET trial

Atherosclerosis. 2015 Jun;240(2):490-6. doi: 10.1016/j.atherosclerosis.2015.03.039. Epub 2015 Mar 28.

Abstract

Objectives: This study evaluated the effect of p38 mitogen-activated protein kinase (p38MAPK) inhibitor, BMS-582949, on atherosclerotic plaque inflammation, using (18)FDG-PET imaging. p38MAPK is an important element of inflammatory pathways in atherothrombosis and its inhibition may lead to reduced inflammation within atherosclerotic plaques.

Methods: Subjects with documented atherosclerosis (n = 72) on stable low-dose statin therapy and having at least one lesion with active atherosclerotic plaque inflammation in either aorta or carotid arteries were randomized to BMS-582949 (100 mg once daily), placebo, or atorvastatin (80 mg once daily), for 12 weeks. Arterial inflammation was assessed using (18)FDG-PET/CT imaging of the carotid arteries and aorta. Uptake of arterial (18)FDG was assessed as target-to-background ratio (TBR): 1) as a mean of all slices of the index vessel, and 2) within active slices of all vessels (AS: which includes only slices with significant inflammation (TBR ≥ 1.6) at the baseline).

Results: Treatment with BMS-582949 did not reduce arterial inflammation relative to placebo, (ΔTBR index: 0.10 [95% CI: -0.11, 0.30], p = 0.34; ΔTBR AS: -0.01 [-0.31, 0.28], p = 0.93) or hs-CRP (median %ΔCRP [IQR]: 33.83% [153.91] vs. 16.71% [133.45], p = 0.61). In contrast, relative to placebo, statin intensification was associated with significant reduction of hs-CRP (%ΔCRP [IQR]: -17.44% [54.68] vs. 16.71% [133.45], p = 0.04) and arterial inflammation in active slices (ΔTBRAS = -0.24 [95% CI: -0.46, -0.01], p = 0.04).

Conclusions: The findings of this study demonstrates that in stable atherosclerosis, 12 weeks of treatment with BMS-582949 did not reduce arterial inflammation or hs-CRP compared to placebo, whereas intensification of statin therapy significantly decreased arterial inflammation.

Trial registration: ClinicalTrials.gov NCT00570752.

Keywords: Atherosclerosis; FDG; Imaging; Inflammation; MAPK.

Publication types

  • Comparative Study
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Aged
  • Anti-Inflammatory Agents / adverse effects
  • Anti-Inflammatory Agents / therapeutic use*
  • Aortic Diseases / blood
  • Aortic Diseases / diagnostic imaging
  • Aortic Diseases / drug therapy*
  • Aortic Diseases / enzymology
  • Atherosclerosis / blood
  • Atherosclerosis / diagnostic imaging
  • Atherosclerosis / drug therapy*
  • Atherosclerosis / enzymology
  • Atorvastatin / therapeutic use
  • Biomarkers / blood
  • C-Reactive Protein / metabolism
  • Carotid Artery Diseases / blood
  • Carotid Artery Diseases / diagnostic imaging
  • Carotid Artery Diseases / drug therapy*
  • Carotid Artery Diseases / enzymology
  • Double-Blind Method
  • Female
  • Fluorodeoxyglucose F18*
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use
  • Inflammation / blood
  • Inflammation / diagnostic imaging
  • Inflammation / drug therapy*
  • Inflammation / enzymology
  • Inflammation Mediators / blood
  • Male
  • Middle Aged
  • Multimodal Imaging
  • Plaque, Atherosclerotic
  • Positron-Emission Tomography*
  • Predictive Value of Tests
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrroles / adverse effects
  • Pyrroles / therapeutic use*
  • Radiopharmaceuticals*
  • Time Factors
  • Tomography, X-Ray Computed
  • Treatment Outcome
  • Triazines / adverse effects
  • Triazines / therapeutic use*
  • United States
  • p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo(1,2-f)(1,2,4)triazine-6-carboxamide
  • Anti-Inflammatory Agents
  • Biomarkers
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Inflammation Mediators
  • Protein Kinase Inhibitors
  • Pyrroles
  • Radiopharmaceuticals
  • Triazines
  • Fluorodeoxyglucose F18
  • C-Reactive Protein
  • Atorvastatin
  • p38 Mitogen-Activated Protein Kinases

Associated data

  • ClinicalTrials.gov/NCT00570752