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

General Information of Drug (ID: DMS9BDQ)

• Drug Name: Tipelukast Drug Info
• Synonyms: Asthma therapy, MediciNova; KCA-757; MN-001

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Phase 2	[1]
Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[2]

• Cross-matching ID:
  PubChem CID: 9893228
  CAS Number: CAS 125961-82-2
  TTD Drug ID: DMS9BDQ

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	[4]
Diethylcarbamazine	DM1TJ8F	Elephantiasis		Approved	[5]
Silymarin	DMXBYQR	N. A.	N. A.	Phase 4	[6]
3,4-Dihydroxycinnamic Acid	DMVZL26	Thrombocytopenia	3B64	Phase 4	[7]
Avastin+/-Tarceva	DMA86FL	Non-small-cell lung cancer	2C25.Y	Phase 3	[8]
ABT-761	DM3FIC2	Asthma	CA23	Phase 3	[9]
Tenidap	DMHQRYE	Rheumatoid arthritis	FA20	Phase 3	[10]
FPL-62064	DMGF8MZ	Inflammation	1A00-CA43.1	Phase 3	[11]
Flobufen	DMPSG4D	Rheumatoid arthritis	FA20	Phase 3	[12]
Darbufelone	DMYVKM5	Asthma	CA23	Phase 2/3	[13]

Drug(s) Targeting Phosphodiesterase 3 (PDE3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cilostazol	DMZMSCT	Intermittent claudication	BD40.00	Approved	[14]
Oxtriphylline	DMLHSE3	Cough	MD12	Approved	[14]
Ibudilast	DM4LSPN	Castleman's disease	4B2Y	Approved	[15]
Enoximone	DMQVZJD	Congestive heart failure	BD10	Approved	[16]
Olprinone	DMWBQKU	Heart failure	BD10-BD13	Approved	[17]
Inamrinone Lactate	DMRMFP4	Cardiac disease	BA00-BE2Z	Approved	[18]
Milrinone	DM8TUPF	Congestive heart failure	BD10	Approved	[14]
Tofisopam	DMTGNWU	Hyperuricaemia	5C55.Y	Phase 2	[19]
RPL-554	DMLD4VQ	Allergic rhinitis	CA08.0	Phase 2	[20]
Org-30029	DMDZ4R2	Heart failure	BD10-BD13	Phase 2	[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	[3]
Phosphodiesterase 3 (PDE3)	TTZCG4L	NOUNIPROTAC	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT02503657) Safety and Tolerability Study in Subjects With Idiopathic Pulmonary Fibrosis (IPF).
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Company report (MediciNova)
• [4] 5-lipoxygenase inhibitor zileuton attenuates ischemic brain damage: involvement of matrix metalloproteinase 9. Neurol Res. 2009 Oct;31(8):848-52.
• [5] 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.
• [6] Anti-inflammatory and anti-arthritic activities of silymarin acting through inhibition of 5-lipoxygenase. Phytomedicine. 2000 Mar;7(1):21-4.
• [7] Phenidone protects the nigral dopaminergic neurons from LPS-induced neurotoxicity. Neurosci Lett. 2008 Nov 7;445(1):1-6.
• [8] Simple analogues of anthralin: unusual specificity of structure and antiproliferative activity. J Med Chem. 1997 Nov 7;40(23):3773-80.
• [9] Treatment with 5-lipoxygenase inhibitor VIA-2291 (Atreleuton) in patients with recent acute coronary syndrome. Circ Cardiovasc Imaging. 2010 May;3(3):298-307.
• [10] 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.
• [11] FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor. Agents Actions. 1990 Jun;30(3-4):432-42.
• [12] 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.
• [13] 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.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [15] Therapeutic targeting of 3',5'-cyclic nucleotide phosphodiesterases: inhibition and beyond. Nat Rev Drug Discov. 2019 Oct;18(10):770-796.
• [16] In vitro and in vivo effects of the phosphodiesterase-III inhibitor enoximone on malignant hyperthermia-susceptible swine. Anesthesiology. 2003 Apr;98(4):944-9.
• [17] Olprinone: a phosphodiesterase III inhibitor with positive inotropic and vasodilator effects. Cardiovasc Drug Rev. 2002 Fall;20(3):163-74.
• [18] Effects of amrinone on hepatic ischemia-reperfusion injury in rats. J Hepatol. 2002 Jul;37(1):31-8.
• [19] The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25.
• [20] Efficacy and safety of RPL554, a dual PDE3 and PDE4 inhibitor, in healthy volunteers and in patients with asthma or chronic obstructive pulmonary disease: findings from four clinical trials.Lancet Respir Med.2013 Nov;1(9):714-27.
• [21] Effects of the positive inotropic agent Org 30029 on developed force and aequorin light transients in intact canine ventricular myocardium. Circ Res. 1993 Mar;72(3):597-606.