Labradimil

Bradykinin B2 Receptor Agonist / Blood Brain Barrier ModulatorRx: ResearchCompound: Investigational

Also known as: bradykinin analog BBB opener, Cereport, RMP-7

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Labradimil (also known as Cereport or RMP-7) is a synthetic bradykinin analog developed to transiently and selectively increase blood-brain barrier permeability, thereby enhancing CNS delivery of chemotherapeutic agents such as carboplatin for brain tumors. Clinical trials in glioblastoma and brain metastases showed mixed results, and the compound did not achieve regulatory approval.

Mechanism of Action

Synthetic analog of bradykinin that transiently opens the blood-brain barrier (BBB) by activating bradykinin B2 receptors on cerebral capillary endothelial cells, increasing paracellular permeability and facilitating delivery of co-administered agents into the CNS.

Routes of Administration

Intravenous

Goals & Uses

  • Improved survival in glioblastomaOncologyLow
  • Enhanced CNS drug deliveryPharmacokinetic AugmentationModerate
  • Brain tumor chemotherapy augmentationOncologyModerate

Contraindications

  • Hypersensitivity to bradykinin analogsAllergy/ImmunologyHigh
  • Severe hypotension or hemodynamic instabilityCardiovascularHigh
  • Active intracranial hemorrhageNeurologicalHigh

Adverse Effects

  • HeadacheNeurologicCommonPain in the head or upper neck
  • HypotensionCardiovascularCommonLow blood pressure
  • Nausea/vomitingGastrointestinalUncommon
  • FlushingVascularCommonWarmth and redness of the skin
  • SeizuresNeurologicalUncommon

Drug Interactions

  • CarboplatinModerate
  • ACE inhibitorsModerate
  • AntihypertensivesModerateMay potentiate hypotensive effects in some contexts

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Pediatric patientsAgeRelative
  • Patients with cardiovascular diseaseComorbidityRelative

Regulatory Status

  • European UnionInvestigationalStudied in European clinical trials for glioblastoma; no marketing authorization granted.
  • United StatesInvestigationalEvaluated in FDA-regulated clinical trials; never approved. IND held during development phase.

Never received FDA or EMA approval. Evaluated in Phase II/III clinical trials during the 1990s–2000s for brain tumor chemotherapy augmentation. Development largely discontinued after pivotal trials failed to demonstrate sufficient clinical benefit.

Evidence & Sources

No sources recorded yet.

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