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

General Information of Drug (ID: DMKFTZA)

• Drug Name: BayCysLT2 Drug Info
• Synonyms: CysLT2cpd

Indication

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

• Cross-matching ID:
  PubChem CID: 53394034
  CAS Number: CAS 712313-33-2
  TTD Drug ID: DMKFTZA

Molecule-Related Drug Atlas

Drug(s) Targeting Leukotriene CysLT1 receptor (CYSLTR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Montelukast	DMD157S	Allergic asthma	CA23.0	Approved	[3]
Zafirlukast	DMHNQOG	Asthma	CA23	Approved	[4]
Pranlukast	DMYHDCA	Allergic rhinitis	CA08.0	Approved	[5]
Cinalukast	DMFIC0M	Asthma	CA23	Approved	[6]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[7]
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[8]
Masilukast	DMDTI0L	Asthma	CA23	Phase 2	[9]
LM-1507.NA	DMW6VA0	Asthma	CA23	Phase 2	[10]
Iralukast	DMQ3RWN	Asthma	CA23	Phase 2	[11]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[12]

Drug(s) Targeting Leukotriene CysLT2 receptor (CYSLTR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY-X-7195	DM2XE80	Asthma	CA23	Phase 2	[8]
AS-35	DMC2WI7	Asthma	CA23	Discontinued in Phase 2	[13]
DS-4574	DM8GZWC	Asthma	CA23	Discontinued in Phase 2	[14]
Sulukast	DMBSLZV	Asthma	CA23	Discontinued in Phase 2	[15]
ICI-198615	DM0195G	Asthma	CA23	Terminated	[16]
MDL-43291	DMBIDQX	Asthma	CA23	Terminated	[17]
LY-290154	DMPZ7AO	Asthma	CA23	Terminated	[18]
FPL-55712	DMF1CDK	Asthma	CA23	Terminated	[19]
LTE4	DMCPB0Q	Discovery agent	N.A.	Investigative	[20]
LTC4	DM702WR	Discovery agent	N.A.	Investigative	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene CysLT1 receptor (CYSLTR1)	TTGKOY9	CLTR1_HUMAN	Antagonist	[2]
Leukotriene CysLT2 receptor (CYSLTR2)	TT0PZR5	CLTR2_HUMAN	Antagonist	[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: 6196).
• [2] Synthesis of cysteinyl leukotrienes in human endothelial cells: subcellular localization and autocrine signaling through the CysLT2 receptor. FASEB J. 2011 Oct;25(10):3519-28.
• [3] Protective potential of montelukast against hepatic ischemia/reperfusion injury in rats. J Surg Res. 2010 Mar;159(1):588-94.
• [4] Inhibitory effects of zafirlukast on respiratory bursts of human neutrophils. Drugs Exp Clin Res. 2002;28(4):133-45.
• [5] Beneficial effects of leukotriene receptor antagonists in the prevention of cedar pollinosis in a community setting. J Investig Allergol Clin Immunol. 2009;19(3):195-203.
• [6] Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast. J Allergy Clin Immunol. 1997 Feb;99(2):210-5.
• [7] Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol Int. 2006 Dec;55(4):403-10.
• [8] The effect of a novel leukotriene C4/D4 antagonist, BAY-x-7195, on experimental allergic reactions. Prostaglandins. 1995 Nov-Dec;50(5-6):269-85.
• [9] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [10] Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma. Biochem Pharmacol. 2002 Apr 15;63(8):1537-46.
• [11] Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro. Br J Pharmacol. 1998 Feb;123(3):590-8.
• [12] In vitro pharmacologic profile of YM158, a new dual antagonist for LTD4 and TXA2 receptors. J Pharmacol Exp Ther. 1998 Nov;287(2):633-9.
• [13] Inhibition of radiolabeled leukotriene-binding by AS-35 in guinea pig lung membrane fraction. Jpn J Pharmacol. 1992 Apr;58(4):357-64.
• [14] Inhibitory effect of DS-4574, a mast cell stabilizer with peptidoleukotriene receptor antagonism, on gastric acid secretion in rats. Eur J Pharmacol. 1994 Apr 1;255(1-3):229-34.
• [15] The pharmacological evaluation of LY 170680, a novel leukotriene D4 and E4 antagonist in the guinea-pig. Br J Pharmacol. 1989 Sep;98(1):259-67.
• [16] Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Biochem Pharmacol. 1992 Oct 6;44(7):1411-5.
• [17] Conformationally restricted leukotriene receptor antagonists: [(octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]ace tic acids. Pharmacology. 1990;40(5):271-6.
• [18] DOI: 10.1021/op060036x
• [19] Effect of the leukotriene receptor antagonists FPL 55712, LY 163443, and MK-571 on the elimination of cysteinyl leukotrienes in the rat. Br J Pharmacol. 1991 Apr;102(4):865-70.
• [20] Differential signaling of cysteinyl leukotrienes and a novel cysteinyl leukotriene receptor 2 (CysLT agonist, N-methyl-leukotriene C in calcium reporter and beta arrestin assays. Mol Pharmacol. 2011 Feb;79(2):270-8.
• [21] Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol Pharmacol. 2000 Dec;58(6):1601-8.