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

General Information of Drug (ID: DMF8B62)

• Drug Name: Linetastine Drug Info
• Synonyms: Tmk688; UNII-7U248Z56LA; 110501-66-1; TMK-688; 159776-68-8; 7U248Z56LA; Linetastine [INN]; Tmk 688; Linazolast; CCRIS 6902; Linazolast (JAN); YM-257; AC1O5R98; CHEMBL314338; SCHEMBL1614484; [4-[(1E,3E)-5-[2-(4-benzhydryloxypiperidin-1-yl)ethylamino]-5-oxopenta-1,3-dienyl]-2-methoxyphenyl] ethyl carbonate; Carbonic acid, 4-(5-((2-(4-(diphenylmethoxy)-1-piperidinyl)ethyl)amino)-5-oxo-1,3-pentadienyl)-2-methoxyphenyl ethyl ester; D09850; Linazolast; Molecule 26

Indication

Disease Entry	ICD 11	Status	REF
Rhinitis	FA20	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 6439232
  CAS Number: CAS 110501-66-1
  TTD Drug ID: DMF8B62

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 Protein kinase C beta (PRKCB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[14]
RUBOXISTAURIN HYDROCHLORIDE	DMQOCD8	Lymphoma	2A80-2A86	Phase 3	[15]
Sotrastaurin acetate	DME53YS	Renal transplantation	NE84	Phase 2	[16]
LY333531	DMGMC8H	Solid tumour/cancer	2A00-2F9Z	Phase 2	[17]
MS-553	DM7ER9J	Chronic lymphocytic leukaemia	2A82.0	Phase 1	[18]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[19]
RO-320432	DMFZ1YW	N. A.	N. A.	Terminated	[20]
LY-317644	DMM20PI	N. A.	N. A.	Terminated	[21]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[22]
LY-326449	DMN53M4	Discovery agent	N.A.	Investigative	[23]

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	Inhibitor	[2]
Protein kinase C beta (PRKCB)	TTYPXQF	KPCB_HUMAN	Inhibitor	[3]

References

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• [3] Potential new medical therapies for diabetic retinopathy: protein kinase C inhibitors. Am J Ophthalmol. 2002 May;133(5):693-8.
• [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] The oral protein-kinase C beta inhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines. Leuk Lymphoma. 2008 Jul;49(7):1374-83.
• [15] Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-9.
• [16] Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
• [17] Protein kinase C beta inhibition attenuates the progression of experimental diabetic nephropathy in the presence of continued hypertension. Diabetes. 2003 Feb;52(2):512-8.
• [18] ClinicalTrials.gov (NCT03492125) A Study Of The Selective PKC-beta Inhibitor MS- 553. U.S. National Institutes of Health.
• [19] Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins, Bioorg. Med. Chem. Lett. 5(18):2155-2160 (1995).
• [20] Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain, Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994).
• [21] Synthesis of bisindolylmaleimide macrocycles, Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995).
• [22] Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
• [23] (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71.