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

General Information of Drug (ID: DM563NC)

• Drug Name: Fasitibant chloride Drug Info
• Synonyms: MEN-16132; Bradykinin B2 antagonist (inflammation), Menarini; MEN-11270 analogs, Menarini

Indication

Disease Entry	ICD 11	Status	REF
Osteoarthritis	FA00-FA05	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11535140
  TTD Drug ID: DM563NC

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]
DELTIBANT	DM5CB8U	Sepsis	1G40-1G41	Phase 2	[4]
Anatibant	DMG7IEN	Traumatic brain injury	NA07.Z	Phase 2	[5]
DM199	DM0157T	Cerebral ischemia	8B11	Phase 2	[6]
BRADYKININ	DM4R6UV	N. A.	N. A.	Phase 1	[7]
NPC-567	DMAVZ1F	Rhinitis	FA20	Discontinued in Phase 2	[8]
Labradimil	DMSFL76	Brain cancer	2A00	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	Antagonist	[2]

References

• [1] ClinicalTrials.gov (NCT01091116) A Locally Injected Bradykinin Antagonist for TReatment of OSteoarthritiS. U.S. National Institutes of Health.
• [2] 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.
• [3] Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.
• [4] 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.
• [5] 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.
• [6] Pharmacological effects of recombinant human tissue kallikrein on bradykinin B2 receptors. Pharmacol Res Perspect. 2015 Mar;3(2):e00119.
• [7] 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.
• [8] 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.
• [9] 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.
• [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.