Pilot study of intravenous glyburide in patients with a large ischemic stroke

Stroke. 2014 Jan;45(1):281-3. doi: 10.1161/STROKEAHA.113.003352. Epub 2013 Nov 5.


Background and purpose: Preclinical and retrospective clinical data indicate that glyburide, a selective inhibitor of sulfonylurea receptor 1-transient receptor potential melastatin 4, is effective in preventing edema and improving outcome after focal ischemia. We assessed the feasibility of recruiting and treating patients with severe stroke while obtaining preliminary information on the safety and tolerability of RP-1127 (glyburide for injection).

Methods: We studied 10 patients with acute ischemic stroke, with baseline diffusion-weighted imaging lesion volumes of 82 to 210 cm3, whether treated with intravenous recombinant tissue-type plasminogen activator, age 18 to 80 years, and time to RP-1127≤10 hours.

Results: Recruitment was completed within 10 months. The mean age was 50.5 years, and baseline diffusion-weighted image lesion volume was 102±23 cm3. There were no serious adverse events related to drug and no symptomatic hypoglycemia. The increase in ipsilateral hemisphere volume was 50±33 cm3. The proportion of 90-day modified Rankin Scale≤4 was 90% (40% modified Rankin Scale, ≤3).

Conclusions: RP-1127 at a dose of 3 mg/d was well tolerated and did not require any dose reductions. A clinical trial of RP-1127 is feasible.

Clinical trial registration: URL: http://www.clinicaltrials.gov. Unique identifier: NCT01268683.

Keywords: acute treatment; brain swelling; cerebral edema; glyburide; hemorrhagic transformation; ischemic stroke.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Blood Glucose / metabolism
  • Brain Edema / drug therapy
  • Brain Edema / etiology
  • Brain Ischemia / drug therapy*
  • Comorbidity
  • Female
  • Fibrinolytic Agents / therapeutic use
  • Glyburide / administration & dosage
  • Glyburide / adverse effects
  • Glyburide / therapeutic use*
  • Humans
  • Hypoglycemia / chemically induced
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / therapeutic use*
  • Injections, Intravenous
  • Magnetic Resonance Imaging
  • Male
  • Middle Aged
  • Patient Safety
  • Pilot Projects
  • Prospective Studies
  • Stroke / drug therapy*
  • Tissue Plasminogen Activator / therapeutic use
  • Treatment Outcome
  • White People
  • Young Adult


  • Blood Glucose
  • Fibrinolytic Agents
  • Hypoglycemic Agents
  • Tissue Plasminogen Activator
  • Glyburide

Associated data

  • ClinicalTrials.gov/NCT01268683