Labradimil
DRACPC ID DRACPC0067
Active Ingredients Labradimil
Description A synthetic analog of bradykinin. Lobradimil is a potent, specific bradykinin B-2 receptor agonist that stimulates B-2 receptors expressed on the surface of brain capillary endothelial cells, thereby reversibly increasing the permeability of the blood-brain barrier (BBB). Compared to bradykinin, this agent possesses enhanced receptor selectivity, greater plasma stability, and a longer half-life.
Synonyms Cereport; DRG-0182; L-Prolinamide, L-Arginyl-L-prolyl-trans-4- hydroxy-L-prolyl-3-(2- thienyl)-L-alanylglycl -L-seryl-N-(2-((4-((aminoiminomethyl)amino)-1- -carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-, (S-(R*,R*)); RMP-7; Labradimil; Lobradimil
Type Small Molecule
Disease Brain cancer
Classification
Bradykinin agonists Peptide and derivative
Structure Information
Molecular Formula C49H75N15O12S
Molecular Weight 1098.3
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S,4R)-1-[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-thiophen-2-ylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-methoxyphenyl)propyl]amino]-5-(diaminomethylideneamino)pentanoic acid
InChI InChI=1S/C49H75N15O12S/c1-76-31-14-12-28(13-15-31)21-29(24-57-34(47(74)75)9-3-17-56-49(53)54)59-43(70)37-10-4-18-62(37)45(72)36(27-65)61-41(68)35(23-32-7-6-20-77-32)60-40(67)25-58-42(69)39-22-30(66)26-64(39)46(73)38-11-5-19-63(38)44(71)33(50)8-2-16-55-48(51)52/h6-7,12-15,20,29-30,33-39,57,65-66H,2-5,8-11,16-19,21-27,50H2,1H3,(H,58,69)(H,59,70)(H,60,67)(H,61,68)(H,74,75)(H4,51,52,55)(H4,53,54,56)/t29-,30+,33-,34-,35-,36-,37-,38-,39-/m0/s1
InChI_Key IDXCXSCCZNCXCL-XMADEQCMSA-N
SMILES O=C(O)[C@@H](NC[C@@H](NC([C@H]1N(C([C@@H](NC([C@@H](NC(CNC([C@H]2N(C([C@H]3N(C([C@@H](N)CCC/N=C(N)\N)=O)CCC3)=O)C[C@H](O)C2)=O)=O)CC4=CC=CS4)=O)CO)=O)CCC1)=O)CC5=CC=C(OC)C=C5)CCC/N=C(N)\N
External Codes
PubChem CID 6918284
DrugBank Accession Number DB06549
NCI Thesaurus Code C1606
UNII 2MK663C346 GSRS
CAS 159768-75-9
Drug approval
Drug indication
Investigated for use/treatment in brain cancer and pediatric indications.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00005602 | Phase I Study of Concurrent Cereport and Carboplatin With Radiation Therapy for Children With Newly-Diagnosed Brain Stem Gliomas | Brain and Central Nervous System Tumors | Phase 1 | Treatment |
| NCT00001502 | Pediatric Phase I Trial of RMP-7 and Carboplatin in Brain Tumors | Brain Neoplasms; Glioma; Medulloblastoma | Phase 1 | Treatment |
| NCT00019422 | A Phase II Trial of Intravenous Cereport (RMP-7) and Carboplatin in Childhood Brain Tumors | Brain and Central Nervous System Tumors | Phase 2 | Treatment |
| NCT00002316 | Phase I Study to Evaluate the Safety and Tolerance of RMP-7 Administered With Amphotericin B to Patients With HIV Infection and Cryptococcal Meningitis | Meningitis, Cryptococcal; HIV Infections | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
