2-HOBA in Systemic Lupus Erythematosus

Purpose

This is a phase II randomized, placebo-controlled, double-blind, cross-over study to determine the effect of isolevuglandin (IsoLG) scavenging by 2-HOBA on blood pressure and immune activation in patients with SLE. 42 patients with stable SLE will be randomized to treatment sequence to receive placebo or 500mg 2-HOBA three times a day for 8 weeks followed by a 4 week washout and then 8 weeks of the other agent. Primary outcome measures include change in 24-hour blood pressure and NETosis. This study will provide mechanistic information on the role of IsoLGs in autoimmune disease-associated hypertension and immune activation.

Condition

  • Systemic Lupus Erthematosus (SLE)

Eligibility

Eligible Ages
Over 18 Years
Eligible Sex
Female
Accepts Healthy Volunteers
No

Inclusion Criteria

  • Written informed consent - Age ≥18 years - Female (biological) - Meeting the 2019 European League Against Rheumatism/ American College of Rheumatology classification criteria for SLE32 - No change in immunosuppressants ≥3 months - Stable prednisone (or equivalent) dose ≤ 20mg/ day for ≥ 1 month - Elevated blood pressure defined as >120 and < or = 160 mmHg systolic or >80 and < or = 110 mmHg diastolic blood pressure at screening visit - No change in anti-hypertensive dose ≥2 weeks - Willingness to stop NSAIDs for ≥2 weeks before and throughout the study - If of childbearing potential, willingness to use effective birth control throughout the study and 4 weeks after completion of the study (examples: condom, diaphragm, oral contraceptive pill, intrauterine device)

Exclusion Criteria

  • Pregnant or breastfeeding - Male (biological) - Active cancer except for non-melanoma skin cancer - Prior diagnosis of liver cirrhosis or the following abnormal liver function studies: AST or ALT >1.5x the upper limit of normal or total bilirubin ≥1.5 mg/dl - Active infection requiring medical intervention - Major surgery in ≤ 3 months - Aspirin allergy - Use of MAO-I - Estimated creatinine clearance <30 ml/min - Known atrial fibrillation - Severe comorbid condition

Study Design

Phase
Phase 2
Study Type
Interventional
Allocation
Randomized
Intervention Model
Crossover Assignment
Primary Purpose
Treatment
Masking
Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor)

Arm Groups

ArmDescriptionAssigned Intervention
Experimental
Placebo First
Placebo for first 8 weeks, then washout for 4 weeks, and then 2-HOBA acetate for 8 weeks
  • Drug: 2-HOBA acetate (2-Hydroxybenzlamine acetate)
    2-HOBA acetate (2-Hydroxybenzlamine acetate) 500mg (provided as two 250mg capsules) three times per day
    Other names:
    • 2-hydroxybenzylamine
    • 2-HOBA
    • salicylamine
    • IUPAC name: 2-(aminomethyl)phenol
  • Drug: Placebo
    Placebo (provided as two capsules) three times per day
    Other names:
    • indentical placebo
Experimental
2-HOBA First
2-HOBA acetate for first 8 weeks, then washout for 4 weeks, and then placebo for 8 weeks
  • Drug: 2-HOBA acetate (2-Hydroxybenzlamine acetate)
    2-HOBA acetate (2-Hydroxybenzlamine acetate) 500mg (provided as two 250mg capsules) three times per day
    Other names:
    • 2-hydroxybenzylamine
    • 2-HOBA
    • salicylamine
    • IUPAC name: 2-(aminomethyl)phenol
  • Drug: Placebo
    Placebo (provided as two capsules) three times per day
    Other names:
    • indentical placebo

Recruiting Locations

Vanderbilt University Medical Center
Nashville, Tennessee 37232
Contact:
Phicharmon Kulapatana
615-936-5747
phicharmon.kulapatana@vumc.org

More Details

Status
Recruiting
Sponsor
Vanderbilt University Medical Center

Study Contact

Phicharmon Kulapatana (study coordinator)
615-936-5747
phicharmon.kulapatana@vumc.org

Detailed Description

Systemic lupus erythematosus (SLE) is an inflammatory autoimmune disease with a markedly increased prevalence of not only hypertension but also resistant hypertension. Hypertension, along with other factors, leads to a 2 to 3-fold increase in risk of cardiovascular disease in SLE. Other than glucocorticoids and immunosuppression, there are few therapeutic options for patients with SLE and none that are known to have a beneficial effect on hypertension and cardiovascular disease; in fact, glucocorticoids have substantial deleterious effects. The increased prevalence of hypertension and its greater severity in SLE patients are unexplained; however, work from our group and others increasingly implicates activation of the immune system in the pathogenesis of hypertension. Moreover, our data suggest that downstream products of oxidative stress, specifically isolevuglandins (IsoLGs), drive immune activation and hypertension. IsoLGs are highly reactive dicarbonyl products of oxidative stress that bind covalently to proteins causing conformational changes rendering them immunogenic and proinflammatory. Two decades of work at Vanderbilt led to the identification of 2-hydroxybenzylamine (2-HOBA) as a highly effective scavenger of reactive dicarbonyls such as IsoLGs. Scavenging reactive dicarbonyls is preferable to using antioxidants because reactive oxygen species are necessary for normal cellular function. In animal models of SLE, hypertension, and atherosclerosis 2-HOBA reduced inflammation, neutrophil extracellular traps (NETosis), blood pressure, and atherosclerosis, and in human phase I clinical studies with healthy volunteers it was well tolerated. This is a mechanistic, proof-of-concept phase II study with a randomized, placebo-controlled, double-blind, cross-over design to determine the effect of IsoLG scavenging by 2-HOBA on blood pressure and immune activation in patients with SLE. 42 patients with stable SLE will be randomized to treatment sequence to receive placebo or 500mg 2-HOBA three times a day for 8 weeks followed by a 4 week washout and then 8 weeks of the other agent. Comparing 2-HOBA and placebo arms, primary outcomes include change in 24-hour blood pressure and immune activation measured by NETosis.