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

General Information of Drug (ID: DM3H90W)

• Drug Name: KC-11404 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Terminated	[1]

• Cross-matching ID: TTD Drug ID: DM3H90W

Molecule-Related Drug Atlas

Drug(s) Targeting Arachidonate 5-lipoxygenase (5-LOX)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zileuton	DMVRIC2	Allergic asthma	CA23.0	Approved	[2]
Diethylcarbamazine	DM1TJ8F	Elephantiasis		Approved	[3]
Silymarin	DMXBYQR	N. A.	N. A.	Phase 4	[4]
3,4-Dihydroxycinnamic Acid	DMVZL26	Thrombocytopenia	3B64	Phase 4	[5]
Avastin+/-Tarceva	DMA86FL	Non-small-cell lung cancer	2C25.Y	Phase 3	[6]
ABT-761	DM3FIC2	Asthma	CA23	Phase 3	[7]
Tenidap	DMHQRYE	Rheumatoid arthritis	FA20	Phase 3	[8]
FPL-62064	DMGF8MZ	Inflammation	1A00-CA43.1	Phase 3	[9]
Flobufen	DMPSG4D	Rheumatoid arthritis	FA20	Phase 3	[10]
Darbufelone	DMYVKM5	Asthma	CA23	Phase 2/3	[11]

Drug(s) Targeting Platelet-activating factor receptor (PTAFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ticlopidine	DMO946V	Acute coronary syndrome	BA41	Approved	[12]
RUPATADINE	DMBPN7T	N. A.	N. A.	Phase 4	[13]
ISRAPAFANT	DMP61YB	Asthma	CA23	Phase 3	[14]
CMI-392	DM1NCUY	Psoriasis vulgaris	EA90	Phase 2	[15]
Lexipafant	DMZ2YBE	Nerve injury	ND56.4	Phase 2	[16]
YM-264	DMAZNVX	Sepsis	1G40-1G41	Phase 2	[17]
Dersalazine	DMH96JW	Inflammatory bowel disease	DD72	Phase 2	[18]
60P002	DMHBN8X	Dengue	1D20-1D2Z	Phase 2	[19]
PegCNTF	DMW7VGZ	Obesity	5B81	Phase 1	[20]
FOROPAFANT	DML1DGP	Asthma	CA23	Discontinued in Phase 3	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Arachidonate 5-lipoxygenase (5-LOX)	TT2J34L	LOX5_HUMAN	Modulator	[1]
Platelet-activating factor receptor (PTAFR)	TTQL5VC	PTAFR_HUMAN	Modulator	[1]

References

• [1] Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995 Feb 17;38(4):669-85.
• [2] 5-lipoxygenase inhibitor zileuton attenuates ischemic brain damage: involvement of matrix metalloproteinase 9. Neurol Res. 2009 Oct;31(8):848-52.
• [3] Inhibition of leukotriene formation by diethylcarbamazine modifies the acid-base balance in the rabbits with blast injuries of the lungs. Vojnosanit Pregl. 1999 May-Jun;56(3):243-7.
• [4] Anti-inflammatory and anti-arthritic activities of silymarin acting through inhibition of 5-lipoxygenase. Phytomedicine. 2000 Mar;7(1):21-4.
• [5] Phenidone protects the nigral dopaminergic neurons from LPS-induced neurotoxicity. Neurosci Lett. 2008 Nov 7;445(1):1-6.
• [6] Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity. J Med Chem. 1997 Nov 7;40(23):3773-80.
• [7] Treatment with 5-lipoxygenase inhibitor VIA-2291 (Atreleuton) in patients with recent acute coronary syndrome. Circ Cardiovasc Imaging. 2010 May;3(3):298-307.
• [8] The in vitro free radical scavenging activity of tenidap, a new dual cyclo-oxygenase and 5-1ipoxygenase inhibitor. Mediators Inflamm. 1992;1(2):141-3.
• [9] FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.
• [10] Pharmacological profile of the novel potent antirheumatic 4-(2',4'-difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid. Arzneimittelforschung. 1997 May;47(5):648-52.
• [11] Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9.
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [13] Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
• [14] Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor. J Biol Chem. 2010 Feb 19;285(8):5931-40.
• [15] Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20.
• [16] Lexipafant and acute pancreatitis: a critical appraisal of the clinical trials.Eur J Surg.2002;168(4):215-9.
• [17] Effects of YM264, a novel PAF antagonist, on puromycin aminonucleoside-induced nephropathy in the rat. Biochem Biophys Res Commun. 1991 Apr 30;176(2):781-5.
• [18] The intestinal anti-inflammatory effect of dersalazine sodium is related to a down-regulation in IL-17 production in experimental models of rodent colitis. Br J Pharmacol. 2012 February; 165(3): 729-740.
• [19] Clinical pipeline report, company report or official report of 60 Degrees Pharmaceuticals.
• [20] Sch 37370: a new drug combining antagonism of platelet-activating factor (PAF) with antagonism of histamine. Agents Actions Suppl. 1991;34:313-21.
• [21] Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist. J Pharmacol Exp Ther. 1991 Oct;259(1):44-51.