Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMSFL76)

• Drug Name: Labradimil Drug Info
• 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

Indication

Disease Entry	ICD 11	Status	REF
Brain cancer	2A00	Discontinued in Phase 2	[1]

• Therapeutic Class: Anticancer Agents
• Cross-matching ID:
  PubChem CID: 6918284
  CAS Number: CAS 159768-75-9
  TTD Drug ID: DMSFL76

Molecule-Related Drug Atlas

Drug(s) Targeting B2 bradykinin receptor (BDKRB2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Icatibant	DMQPTOZ	Hereditary angioedema	4A00.14	Approved	[3]
Fasitibant chloride	DM563NC	Osteoarthritis	FA00-FA05	Phase 2	[4]
DELTIBANT	DM5CB8U	Sepsis	1G40-1G41	Phase 2	[5]
Anatibant	DMG7IEN	Traumatic brain injury	NA07.Z	Phase 2	[6]
DM199	DM0157T	Cerebral ischemia	8B11	Phase 2	[7]
BRADYKININ	DM4R6UV	N. A.	N. A.	Phase 1	[8]
NPC-567	DMAVZ1F	Rhinitis	FA20	Discontinued in Phase 2	[9]
NPC-17731	DMGVIZY	Asthma	CA23	Terminated	[10]
JSM-10292	DMU5TGC	Pain	MG30-MG3Z	Terminated	[11]
CP-0597	DMS23JX	Asthma	CA23	Terminated	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
B2 bradykinin receptor (BDKRB2)	TTGY8IW	BKRB2_HUMAN	Agonist	[2]

References

• [1] URL: 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).
• [2] Metabolically 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.
• [3] Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.
• [4] Fasitibant chloride, a kinin B receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166(4):1403-10.
• [5] CP-0127, a novel potent bradykinin antagonist, increases survival in rat and rabbit models of endotoxin shock. Agents Actions Suppl. 1992;38 ( Pt 3):413-20.
• [6] Inhibition of bradykinin B2 receptors before, not after onset of experimental subarachnoid hemorrhage prevents brain edema formation and improves functional outcome. Crit Care Med. 2009 Jul;37(7):2228-34.
• [7] Pharmacological effects of recombinant human tissue kallikrein on bradykinin B2 receptors. Pharmacol Res Perspect. 2015 Mar;3(2):e00119.
• [8] Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists. J Med Chem. 2000 Jun 15;43(12):2382-6.
• [9] cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
• [10] Antinociceptive profile of the pseudopeptide B2 bradykinin receptor antagonist NPC 18688 in mice. Br J Pharmacol. 1996 Feb;117(3):552-558.
• [11] Binding characteristics of [3H]-JSM10292: a new cell membrane-permeant non-peptide bradykinin B2 receptor antagonist. Br J Pharmacol. 2012 Oct;167(4):839-53.
• [12] CP-0597, a selective bradykinin B2 receptor antagonist, inhibits brain injury in a rat model of reversible middle cerebral artery occlusion. Stroke. 1997 Jul;28(7):1430-6.