Labradimil
From PeptidePlaza, the free peptide reference · Entry #1116 · Metabolic · Sources fetched 2026-09-11 · Editorial standards
Labradimil (also known as Lobradimil, Cereport, labradimilum, Receptor mediated permeabilizer) is a metabolic research peptide. Labradimil is a synthetic bradykinin B2 receptor agonist that has been investigated for its ability to increase the permeability of the blood-brain barrier.
Labradimil, also known as Lobradimil or Cereport, is a synthetic peptide that functions as a bradykinin B2 receptor agonist. Its primary mechanism of action involves increasing the permeability of the blood-brain barrier, a property that has led to its investigation in various central nervous system conditions. Labradimil has been studied in clinical trials for Central Nervous System Neoplasms, reaching Phase 2, and for Medulloblastoma, Cryptococcal Meningitis, Brain Neoplasms, and Paraganglioma, all reaching Phase 1. Research on labradimil has focused on its role in enhancing transvascular drug delivery into malignant brain tumors and its potential to modulate tight junctions for improved drug bioavailability.
1 Mechanism of action
Bradykinin B2 receptor agonist (agonist)
Primary targets: Bradykinin B2 receptor
2 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
2.1 Indicated / studied for
- Central Nervous System Neoplasms
- Medulloblastoma
- Meningitis, Cryptococcal
- Brain Neoplasms
- Paraganglioma
3 Chemical and physical properties
| CAS number | 159768-75-9 |
|---|---|
| Molar mass | 1098.3 g/mol |
| Purity (typical) | Not independently verified |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
| Receptors / targets | Bradykinin B2 receptor |
4 Research studies (8)
- The development of the bradykinin agonist labradimil as a means to increase the permeability of the blood-brain barrier: from concept to clinical evaluation
Clinical pharmacokinetics (2001) · Review - Gateways to clinical trials
Methods and findings in experimental and clinical pharmacology (2007) - Metabolically stable bradykinin B2 receptor agonists enhance transvascular drug delivery into malignant brain tumors by increasing drug half-life
Journal of translational medicine (2009) - Cyclooxygenase activity in bradykinin-induced dermal extravasation. A study in mice and humans
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie (2020) - Recent progress in tight junction modulation for improving bioavailability
Expert opinion on drug discovery (2014) · Review - Bradykinin modulation of tumor vasculature: II. activation of nitric oxide and phospholipase A2/prostaglandin signaling pathways synergistically modifies vascular physiology and morphology to enhance delivery of chemotherapeutic agents to tumors
The Journal of pharmacology and experimental therapeutics (2001) - A unified in vitro test system for the assessment of tight junction modulators
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V (2019) - Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity
Brain research (2002)
5 Safety and risk profile
5.1 Regulatory status
Labradimil is currently classified as Phase 2 clinical trials. It has no approved human indication in the United States; availability elsewhere does not imply demonstrated safety or efficacy.
6 Frequently asked questions
- What is Labradimil?
- Labradimil is a synthetic peptide that acts as a bradykinin B2 receptor agonist. It is also known by the names Lobradimil and Cereport. It has been studied for its ability to increase the permeability of the blood-brain barrier.
- How does Labradimil work?
- Labradimil functions as an agonist for the bradykinin B2 receptor. This action is associated with its ability to increase the permeability of the blood-brain barrier, which can facilitate the delivery of other drugs to the central nervous system.
- What is Labradimil studied for?
- Labradimil has been studied in clinical trials for conditions such as Central Nervous System Neoplasms, Medulloblastoma, Cryptococcal Meningitis, Brain Neoplasms, and Paraganglioma. Its potential to enhance drug delivery to the brain is a key area of research.
- What is the regulatory status of Labradimil?
- Labradimil has reached Phase 2 in clinical trials for Central Nervous System Neoplasms and Phase 1 for several other indications, including Medulloblastoma and Brain Neoplasms.
7 References
- Labradimil — compound summary PubChem. View source
- Labradimil — molecule record ChEMBL. View source
- Labradimil — published literature (9 records) PubMed. View source
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