BIIB093 (IV glibenclamide): an investigational compound for the prevention and treatment of severe cerebral edema

Expert Opin Investig Drugs. 2019 Dec;28(12):1031-1040. doi: 10.1080/13543784.2019.1681967. Epub 2019 Oct 24.

Abstract

Introduction: Brain swelling due to edema formation is a major cause of neurological deterioration and death in patients with large hemispheric infarction (LHI) and severe traumatic brain injury (TBI), especially contusion-TBI. Preclinical studies have shown that SUR1-TRPM4 channels play a critical role in edema formation and brain swelling in LHI and TBI. Glibenclamide, a sulfonylurea drug and potent inhibitor of SUR1-TRPM4, was reformulated for intravenous injection, known as BIIB093.Areas covered: We discuss the findings from Phase 2 clinical trials of BIIB093 in patients with LHI (GAMES-Pilot and GAMES-RP) and from a small Phase 2 clinical trial in patients with TBI. For the GAMES trials, we review data on objective biological variables, adjudicated edema-related endpoints, functional outcomes, and mortality which, despite missing the primary endpoint, supported the initiation of a Phase 3 trial in LHI (CHARM). For the TBI trial, we review data on MRI measures of edema and the initiation of a Phase 2 trial in contusion-TBI (ASTRAL).Expert opinion: Emerging clinical data show that BIIB093 has the potential to transform our management of patients with LHI, contusion-TBI and other conditions in which swelling leads to neurological deterioration and death.

Keywords: BIIB093; Glibenclamide; SUR1-TRPM4; cerebral edema; contusion; large hemispheric infarction; stroke; traumatic brain injury.

Publication types

  • Review

MeSH terms

  • Administration, Intravenous
  • Animals
  • Brain Edema / prevention & control*
  • Drugs, Investigational / administration & dosage
  • Drugs, Investigational / pharmacology
  • Glyburide / administration & dosage*
  • Glyburide / pharmacology
  • Humans
  • Neuroprotective Agents / administration & dosage*
  • Neuroprotective Agents / pharmacology
  • Severity of Illness Index

Substances

  • Drugs, Investigational
  • Neuroprotective Agents
  • Glyburide