Drug General Information
Drug ID
D0G0IZ
Former ID
DCL000146
Drug Name
Labradimil
Synonyms
Cereport; Lobradimil; Receptor mediated permeabilizer; RMP 7; DRG-0182; RMP-7; N2-((S)-2-(L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-L-prolinamido)-3-(p-methoxyphenyl)propyl)-L-arginine; (S-(R*,R*))-L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-3-(2-thienyl)-L-alanylglycyl-L-seryl-N-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-L-prolinamide
Drug Type
Small molecular drug
Indication Brain cancer [ICD9: 191, 225.0; ICD10:C71, D33] Discontinued in Phase 2 [541821], [546212]
Therapeutic Class
Anticancer Agents
Company
Alkermes
Structure
Download
2D MOL

3D MOL

Formula
C49H75N15O12S
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
InChIKey
IDXCXSCCZNCXCL-XMADEQCMSA-N
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) B2 bradykinin receptor Target Info Agonist [535614], [537315]
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Endocrine and other factor-regulated calcium reabsorption
Chagas disease (American trypanosomiasis)
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Pathway Interaction Database Direct p53 effectors
Validated transcriptional targets of deltaNp63 isoforms
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
G alpha (i) signalling events
WikiPathways ACE Inhibitor Pathway
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Nifedipine Activity
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 541821(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 672).
Ref 546212Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006912)
Ref 535614Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity. Brain Res. 2002 Nov 29;956(2):211-20.
Ref 537315Metabolically stable bradykinin B2 receptor agonists enhance transvascular drug delivery into malignant brain tumors by increasing drug half-life. J Transl Med. 2009 May 13;7:33.

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