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

General Information of Drug (ID: DMTGU0L)

• Drug Name: H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1669) Drug Info
• Synonyms: CHEMBL412824; H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1669)

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 44316161
  TTD Drug ID: DMTGU0L

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	[2]
Fasitibant chloride	DM563NC	Osteoarthritis	FA00-FA05	Phase 2	[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	[1]
NPC-567	DMAVZ1F	Rhinitis	FA20	Discontinued in Phase 2	[7]
Labradimil	DMSFL76	Brain cancer	2A00	Discontinued in Phase 2	[8]
NPC-17731	DMGVIZY	Asthma	CA23	Terminated	[9]
JSM-10292	DMU5TGC	Pain	MG30-MG3Z	Terminated	[10]

Drug(s) Targeting B1 bradykinin receptor (BDKRB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SSR-240612	DMFNZPY	Rheumatoid arthritis	FA20	Phase 2	[11]
Safotibant	DMKDP57	Diabetic macular edema	9B71.02	Phase 2	[12]
BI 113823	DMUJ1EL	Osteoarthritis	FA00-FA05	Phase 1	[13]
H-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1638)	DM6839G	Discovery agent	N.A.	Investigative	[1]
Des-Arg(9)-[Leu(8)]-BK	DMVX9I0	Depression	6A70-6A7Z	Investigative	[14]
H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1645)	DMDXIS7	Discovery agent	N.A.	Investigative	[1]
JMV1431	DMAR3M2	Discovery agent	N.A.	Investigative	[1]
Ac-Lys-[Leu(8)]-des-Arg(9)-BK	DMIAYTP	Discovery agent	N.A.	Investigative	[15]
NVP-SAA164	DMN90R6	Pain	MG30-MG3Z	Investigative	[16]
Des-Arg10-Kallidin	DMZ5Y94	Discovery agent	N.A.	Investigative	[17]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
B1 bradykinin receptor (BDKRB1)	TTG5QIA	BKRB1_HUMAN	Inhibitor	[1]
B2 bradykinin receptor (BDKRB2)	TTGY8IW	BKRB2_HUMAN	Inhibitor	[1]

References

• [1] 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.
• [2] Bradykinin receptor antagonists--a review of the patent literature 2005-2008. Expert Opin Ther Pat. 2009 Jul;19(7):919-41.
• [3] 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.
• [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] 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.
• [8] 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.
• [9] Antinociceptive profile of the pseudopeptide B2 bradykinin receptor antagonist NPC 18688 in mice. Br J Pharmacol. 1996 Feb;117(3):552-558.
• [10] 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.
• [11] The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 September; 152(2): 280-287.
• [12] The role of kinin receptors in cancer and therapeutic opportunities. Cancer Letters Volume 345, Issue 1, 1 April 2014, Pages 27-38.
• [13] The bradykinin B1 receptor antagonist BI113823 reverses inflammatory hyperalgesia by desensitization of peripheral and spinal neurons. Eur J Pain. 2015 Jan;19(1):132-42.
• [14] Evidence for the participation of kinins in Freund's adjuvant-induced inflammatory and nociceptive responses in kinin B1 and B2 receptor knockout mice. Neuropharmacology. 2001 Dec;41(8):1006-12.
• [15] Non-competitive pharmacological antagonism at the rabbit B(1) receptor. Br J Pharmacol. 2000 Nov;131(5):885-92.
• [16] 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: 659).
• [17] Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8.