Labradimil
Also known as: bradykinin analog BBB opener, Cereport, RMP-7
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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
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.
Frequently Asked Questions
What is Labradimil?
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.
What is Labradimil used for?
Labradimil is educationally associated with: Improved survival in glioblastoma, Enhanced CNS drug delivery, Brain tumor chemotherapy augmentation. Educational only — not medical advice.
How is Labradimil administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Labradimil?
Reported adverse effects include: Headache, Hypotension, Nausea/vomiting, Flushing, Seizures. This list is not exhaustive — consult a qualified clinician.
Who should avoid Labradimil?
Recorded contraindications: Hypersensitivity to bradykinin analogs, Severe hypotension or hemodynamic instability, Active intracranial hemorrhage. Consult a qualified clinician before use.