Imatinib mesylate (Gleevec) in the treatment of diffuse cutaneous systemic sclerosis: results of a 1-year, phase IIa, single-arm, open-label clinical trial

Ann Rheum Dis. 2011 Jun;70(6):1003-9. doi: 10.1136/ard.2010.143974. Epub 2011 Mar 11.

Abstract

Objective: To assess the safety and effectiveness of imatinib mesylate in the treatment of diffuse cutaneous systemic sclerosis (dcSSc).

Methods: In this phase IIa, open-label, single-arm clinical trial, 30 patients with dcSSc were treated with imatinib 400 mg daily. Patients were monitored monthly for safety assessments. Modified Rodnan skin scores (MRSS) were assessed every 3 months. Pulmonary function testing, chest radiography, echocardiography and skin biopsies were performed at baseline and after 12 months of treatment.

Results: Twenty-four patients completed 12 months of therapy. 171 adverse events (AE) with possible relation to imatinib were identified; 97.6% were grade 1 or 2. Twenty-four serious AE were identified, two of which were attributed to study medication. MRSS decreased by 6.6 points or 22.4% at 12 months (p=0.001). This change was evident starting at the 6-month time point (Δ=-4.5; p<0.001) and was seen in patients with both early and late-stage disease. Forced vital capacity (FVC) improved by 6.4% predicted (p=0.008), and the diffusion capacity remained stable. The improvement in FVC was significantly greater in patients without interstitial lung disease. Health-related quality of life measures improved or remained stable. Blinded dermatopathological analysis confirmed a significant decrease in skin thickness and improvement in skin morphology.

Conclusions: Treatment with imatinib was tolerated by most patients in this cohort. Although AE were common, most were mild to moderate. In this open-label experience, improvements in skin thickening and FVC were observed. Further investigation of tyrosine kinase inhibition for dcSSc in a double-blind randomised placebo controlled trial is warranted. ClinicalTrials.gov, NCT00555581.

Publication types

  • Clinical Trial, Phase II
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Benzamides
  • Biopsy
  • Dermatologic Agents / adverse effects
  • Dermatologic Agents / therapeutic use*
  • Female
  • Humans
  • Imatinib Mesylate
  • Male
  • Middle Aged
  • Piperazines / adverse effects
  • Piperazines / therapeutic use*
  • Protein Kinase Inhibitors / adverse effects
  • Protein Kinase Inhibitors / therapeutic use*
  • Pulmonary Diffusing Capacity / drug effects
  • Pulmonary Fibrosis / diagnostic imaging
  • Pulmonary Fibrosis / physiopathology
  • Pyrimidines / adverse effects
  • Pyrimidines / therapeutic use*
  • Radiography
  • Scleroderma, Diffuse / drug therapy*
  • Scleroderma, Diffuse / pathology
  • Severity of Illness Index
  • Skin / pathology
  • Treatment Outcome
  • Ultrasonography
  • Vital Capacity / drug effects
  • Young Adult

Substances

  • Benzamides
  • Dermatologic Agents
  • Piperazines
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Imatinib Mesylate

Associated data

  • ClinicalTrials.gov/NCT00555581